- Vibrational spectra of chloroacetamide and three deuterated analogues in the crystalline state
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The IR and Raman Spectra of α-chloroacetamide CH2ClCONH2 and three deuterated analogues CH2ClCOND2, CD2ClCONH2 and CD2ClCOND2, in the crystalline state have been studied.A complete interpretation of the spectra has been worked out on the basis of spectral comparison and of the normal coordinate analysis of the four analogues.
- Mido, Yoshiyuki,Yanagida, Akiyo,Garcia, M. Victoria
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Read Online
- Triazole-estradiol analogs: A potential cancer therapeutic targeting ovarian and colorectal cancer
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1,2,3-triazoles have continuously shown effectiveness as biologically active systems towards various cancers, and when used in combination with steroid skeletons as a carrier, which can act as a drug delivery system, allows for a creation of a novel set of analogs that may be useful as a pharmacophore leading to a potential treatment option for cancer. A common molecular target for cancer inhibition is that of the Epidermal Growth Factor Receptor/Mitogen Activated Protein Kinase pathways, as inhibition of these proteins is associated with a decrease in cell viability. Estradiol-Triazole analogs were thus designed using a molecular modeling approach. Thirteen of the high scoring analogs were then synthesized and tested in-vitro on an ovarian cancer cell line (A2780) and colorectal cancer cell line (HT-29). The most active compound, Fz25, shows low micromolar activity in both the ovarian (15.29 ± 2.19 μM) and colorectal lines (15.98 ± 0.39 μM). Mechanism of action studies proved that Fz25 moderately arrests cells in the G1 phase of the cell cycle, specifically inhibiting STAT3 in both cell lines. Additionally, Fz57 shows activity in the colorectal line (24.19 ± 1.37 μM). Inhibition studies in both cell lines show inhibition against various proteins in the EGFR pathway, namely EGFR, STAT3, ERK, and mTOR. To further study their effects as therapeutics, Fz25 and Fz57 were studied against drug efflux proteins, which are associated with drug resistance, and were found to inhibit the ABC transporter P-glycoprotein. We can conclude that these estradiol-triazole analogs provide a key for future studies targeting protein inhibition and drug resistance in cancer.
- Alotaibi, Faez,Halaweish, Fathi,Halaweish, Hossam,Iram, Surtaj,Kasten, Abigail,Kyeremateng, Jennifer,Ostlund, Trevor
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- Amide bond formation in aqueous solution: Direct coupling of metal carboxylate salts with ammonium salts at room temperature
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Herein, we report a green, expeditious, and practically simple protocol for direct coupling of carboxylate salts and ammonium salts under ACN/H2O conditions at room temperature without the addition of tertiary amine bases. The water-soluble coupling reagent EDC·HCl is a key component in the reaction. The reaction runs smoothly with unsubstituted/substituted ammonium salts and provides a clean product without column chromatography. Our reaction tolerates both carboxylate (which are unstable in other forms) and amine salts (which are unstable/volatile when present in free form). We believe that the reported method could be used as an alternative and suitable method at the laboratory and industrial scales. This journal is
- Nielsen, John,Tung, Truong Thanh
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supporting information
p. 10073 - 10080
(2021/12/10)
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- Synthesis method of diethyl cyanomethylphosphonate
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The invention discloses a synthesis method of diethyl cyanomethylphosphonate. The synthesis method comprises the following steps: carrying out an esterification reaction on chloroacetic acid and ethanol to obtain ethyl chloroacetate; reacting the ethyl chloroacetate with ammonia water to generate chloroacetamide; adding phosphorus pentoxide into the chloroacetamide, performing heating dehydration,distilling out chloroacetonitrile while heating, and finally performing reduced pressure distillation to enable the chloroacetonitrile to be completely distilled out; transferring the chloroacetonitrile into a synthesis reaction kettle, adding a catalyst tetrabutylammonium iodide, heating, dropwise adding triethyl phosphite, and controlling the internal temperature for a reaction to obtain a crude product; and transferring the crude product into a high-purity rectifying tower, and performing purification to respectively rectify triethyl phosphite and diethyl cyanomethylphosphonate.
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Paragraph 0016-0017; 0020-0021; 0024-0025; 0028-0029
(2020/05/01)
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- A Heterogeneous Ruthenium dmso Complex Supported onto Silica Particles as a Recyclable Catalyst for the Efficient Hydration of Nitriles in Aqueous Medium
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In the present work, we describe an efficient method for the covalent anchoring of a Ru-dmso complex onto two types of supports: mesoporous silica particles (SP) and silica coated magnetic particles (MSNP). First, we have prepared and characterized the molecular complexes containing the bidentate pyridylpyrazole ligands pypz-Me and pypz-CH2COOEt, with the formula [RuIICl2(pypz-R)(dmso)2] (R = Me, 1; CH2COOEt, 2). Complex 2 was anchored onto the silica supports, yielding the heterogeneous systems SP@2 and MSNP@2 which were fully characterized by IR, UV-vis, SEM, TEM, TGA, and XPS techniques. Hydration of representative nitriles has been tested with the molecular complexes and their SP@2 and MSNP@2 heterogeneous counterparts, in aqueous medium under neutral conditions. The heterogeneous catalysts display high yields and excellent selectivity values. Both systems can be reused throughout several cycles for benzonitrile and acrylonitrile substrates, without any significant loss in reactivity. The MSNP@2 material can be easily recovered by a magnet, facilitating its reusability.
- Manrique, Ester,Ferrer, Ingrid,Lu, Changyong,Fontrodona, Xavier,Rodríguez, Montserrat,Romero, Isabel
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p. 8460 - 8470
(2019/07/03)
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- Effective Synthesis of 3,4-Diaryl-isoxazole-5-carboxamides and their Antiproliferative Properties
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A simple scalable procedure for the synthesis of 3,4-diaryl-isoxazole-5-carboxamides 6 under mild conditions from readily available material was developed. The targeted compounds 6, structural analogues of heat shock protein inhibitors, were obtained by the rearrangement of intermediate 3,4-diaryl-5-carboxamido-isoxazoline N-oxides 5. In contrast to carboxamido-isoxazoline oxides 5, base-catalyzed recyclization of 3,4-diaryl-5-(ethoxycarbonyl)isoxazoline N-oxides 9c unexpectedly yielded 5-hydroxy-1,2-oxazin-6-ones 17c instead of ethyl 3,4-diaryl-isoxazole-5-carboxylates 10. Crystal and molecular structure of 4-(2,5-dimethoxy-3,4-methylenedioxyphenyl)-5-hydroxy-3-phenyl-6H-1,2-oxazin-6-one 17c was established by single-crystal X-ray diffraction study. In a phenotypic sea urchin embryo assay, carboxamide 6f showed moderate antimitotic antitubulin activity compared to 5-unsubstituted 3,4-diarylisoxazoles 15, which featured strong microtubule destabilizing effect.
- Maksimenko, Anna S.,Kislyi, Victor P.,Chernysheva, Natalia B.,Strelenko, Yuri A.,Zubavichus, Yan V.,Khrustalev, Victor N.,Semenova, Marina N.,Semenov, Victor V.
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p. 4260 - 4270
(2019/07/12)
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- Corresponding amine nitrile and method of manufacturing thereof
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The invention relates to a manufacturing method of nitrile. Compared with the prior art, the manufacturing method has the characteristics of significantly reduced using amount of an ammonia source, low environmental pressure, low energy consumption, low production cost, high purity and yield of a nitrile product and the like, and nitrile with a more complex structure can be obtained. The invention also relates to a method for manufacturing corresponding amine from nitrile.
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Paragraph 0138; 0139; 0140; 0145; 0146
(2018/05/07)
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- Phosphinous Acid-Assisted Hydration of Nitriles: Understanding the Controversial Reactivity of Osmium and Ruthenium Catalysts
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The synthesis and catalytic behavior of the osmium(II) complexes [OsCl2(η6-p-cymene)(PR2OH)] [R=Me (2 a), Ph (2 b), OMe (2 c), OPh (2 d)] in nitrile hydration reactions is presented. Among them, the best catalytic results were obtained with the phosphinous acid derivative [OsCl2(η6-p-cymene)(PMe2OH)] (2 a), which selectively provided the desired primary amides in excellent yields and short times at 80 °C, employing directly water as solvent, and without the assistance of any basic additive (TOF values up to 200 h?1). The process was successful with aromatic, heteroaromatic, aliphatic, and α,β-unsaturated organonitriles, and showed a high functional group tolerance. Indeed, complex 2 a represents the most active and versatile osmium-based catalyst for the hydration of nitriles reported so far in the literature. In addition, it exhibits a catalytic performance similar to that of its ruthenium analogue [RuCl2(η6-p-cymene)(PMe2OH)] (4). However, when compared to 4, the osmium complex 2 a turned out to be faster in the hydration of less-reactive aliphatic nitriles, whereas the opposite trend was generally observed with aromatic substrates. DFT calculations suggest that these differences in reactivity are mainly related to the ring strain associated with the key intermediate in the catalytic cycle, that is, a five-membered metallacyclic species generated by intramolecular addition of the hydroxyl group of the phosphinous acid ligand to the metal-coordinated nitrile.
- González-Fernández, Rebeca,Crochet, Pascale,Cadierno, Victorio,Menéndez, M. Isabel,López, Ramón
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p. 15210 - 15221
(2017/10/12)
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- Chlorophosphines as auxiliary ligands in ruthenium-catalyzed nitrile hydration reactions: Application to the preparation of β-ketoamides
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The catalytic hydration of nitriles into amides, in water under neutral conditions, has been studied using a series of arene-ruthenium(ii) complexes containing commercially available chlorophosphines as auxiliary ligands, i.e. compounds [RuCl2(η6-p-cymene)(PR2Cl)] (R = aryl, heteroaryl or alkyl group). In the reaction medium, the coordinated chlorophosphines readily undergo hydrolysis to generate the corresponding phosphinous acids PR2OH, which are well-known "cooperative" ligands for this catalytic transformation. Among the complexes employed, best results were obtained with [RuCl2(η6-p-cymene){P(4-C6H4F)2Cl}]. Performing the catalytic reactions at 40 °C with 2 mol% of this complex, a large variety of organonitriles could be selectively converted into the corresponding primary amides in high yields and relatively short times. The application of [RuCl2(η6-p-cymene){P(4-C6H4F)2Cl}] in the preparation of synthetically useful β-ketoamides is also presented.
- González-Fernández, Rebeca,González-Liste, Pedro J.,Borge, Javier,Crochet, Pascale,Cadierno, Victorio
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p. 4398 - 4409
(2016/07/06)
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- Bis(allyl)-ruthenium(IV) complexes with phosphinous acid ligands as catalysts for nitrile hydration reactions
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Several mononuclear ruthenium(iv) complexes with phosphinous acid ligands [RuCl2(η3:η3-C10H16)(PR2OH)] have been synthesized (78-86% yield) by treatment of the dimeric precursor [{RuCl(μ-Cl)(η3:η3-C10H16)}2] (C10H16 = 2,7-dimethylocta-2,6-diene-1,8-diyl) with 2 equivalents of different aromatic, heteroaromatic and aliphatic secondary phosphine oxides R2P(O)H. The compounds [RuCl2(η3:η3-C10H16)(PR2OH)] could also be prepared, in similar yields, by hydrolysis of the P-Cl bond in the corresponding chlorophosphine-Ru(iv) derivatives [RuCl2(η3:η3-C10H16)(PR2Cl)]. In addition to NMR and IR data, the X-ray crystal structures of representative examples are discussed. Moreover, the catalytic behaviour of complexes [RuCl2(η3:η3-C10H16)(PR2OH)] has been investigated for the selective hydration of organonitriles in water. The best results were achieved with the complex [RuCl2(η3:η3-C10H16)(PMe2OH)], which proved to be active under mild conditions (60 °C), with low metal loadings (1 mol%), and showing good functional group tolerance.
- Tomás-Mendivil, Eder,Francos, Javier,González-Fernández, Rebeca,González-Liste, Pedro J.,Borge, Javier,Cadierno, Victorio
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p. 13590 - 13603
(2016/09/04)
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- A simple method for the synthesis of furfuryl ketones and furylacetic acid derivatives
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A simple preparative method has been developed for the synthesis of aryl(furfuryl) ketones, amides, and furylacetic acid esters, based on radical alkylation of furan derivatives at the α-position with O-ethyl(phenacyl)xanthogenates and phenacyl iodides in the presence of Fenton's reagent (H2O2/FeSO4·7H2O) in DMSO. The range of applicability and mechanisms for the formation of major and side products have been considered.
- Chalikidi, Petrakis N.,Nevolina, Tatyana A.,Uchuskin, Maxim G.,Abaev, Vladimir T.,Butin, Alexander V.
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p. 621 - 629
(2015/10/12)
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- Exploring rhodium(I) complexes [RhCl(COD)(PR3)] (COD = 1,5-cyclooctadiene) as catalysts for nitrile hydration reactions in water: The aminophosphines make the difference
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Several rhodium(I) complexes, [RhCl(COD)(PR3)], containing potentially cooperative phosphine ligands, have been synthesized and evaluated as catalysts for the selective hydration of organonitriles into amides in water. Among the different phosphines screened, those of general composition P(NR 2)3 led to the best results. In particular, complex [RhCl(COD){P(NMe2)3}] was able to promote the selective hydration of a large range of nitriles in water without the assistance of any additive, showing a particularly high activity with heteroaromatic and heteroaliphatic substrates. Employing this catalyst, the antiepileptic drug rufinamide was synthesized in high yield by hydration of 4-cyano-1-(2,6- difluorobenzyl)-1H-1,2,3-triazole. For this particular transformation, complex [RhCl(COD){P(NMe2)3}] resulted more effective than related ruthenium catalysts.
- Tomas-Mendivil, Eder,Garcia-Alvarez, Rocio,Vidal, Cristian,Crochet, Pascale,Cadierno, Victorio
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p. 1901 - 1910
(2014/06/24)
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- An efficient ruthenium(iv) catalyst for the selective hydration of nitriles to amides in water under mild conditions
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A Ru(iv) catalyst able to promote the selective hydration of nitriles to amides in water, at low metal loadings and under mild conditions, is presented. This journal is the Partner Organisations 2014.
- Tomás-Mendivil, Eder,Suárez, Francisco J.,Díez, Josefina,Cadierno, Victorio
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supporting information
p. 9661 - 9664
(2014/08/18)
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- Investigation of binap-based hydroxyphosphine arene-ruthenium(II) complexes as catalysts for nitrile hydration
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The binap-based hydroxyphosphine-(η6-arene)-ruthenium(ii) complexes [RuX{η6:κ1(P)-PPh2-binaphthyl}{PPh2(OH)}][OTf] (X = OTf (4), Cl (5)) have been evaluated as potential catalysts for the selective hydration of nitriles to primary amides. The triflate derivative 4 proved to be the most active, being able to hydrate a large variety of aromatic, heteroaromatic, α,β-unsaturated and aliphatic nitriles in pure water at 100°C. The utility of complex 4 to promote the catalytic rearrangement of aldoximes has also been demonstrated. In addition, insights about the role played by the hydroxyphosphine ligand PPh2(OH) during the catalytic reactions are given.
- Toms-Mendivil, Eder,Menndez-Rodrguez, Luca,Francos, Javier,Crochet, Pascale,Cadierno, Victorio
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p. 63466 - 63474
(2015/02/19)
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- Synthesis and antitumor activity evaluation of pyrimidine analogues bearing urea moiety
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A series of 4-anilino-6-phenylpyrimidines containing urea moiety were synthesized and the structures of all products were confirmed by 1H NMR, 13C NMR and HRMS. The antiproliferative activities of these compounds were evaluated against three human tumor cell lines (MGC-803, MCF-7 and EC-109) by applying the MTT assay method. compounds 4a, 4b and 6a showed the most effective activity, among which, 6a was more cytotoxic than 5-fluorouracil against all tested human cancer cell lines with IC50 values ranging from 1.80 to 2.72 μmol·L-1. A series of 4-anilino-6-phenylpyrimidines containing urea moiety were synthesized. The antiproliferative activities of these compounds were evaluated against three human tumor cell lines (MGC-803, MCF-7 and EC-109) by applying the MTT assay method. compounds 4a, 4b and 6a showed most effective activity, among which, 6a was more cytotoxic than 5-fluorouracil against all tested three human cancer cell lines with IC50 values ranging from 1.80 to 2.72 μmol·L-1. Copyright
- Shao, Kunpeng,Zhang, Xuyao,Zhang, Xiaosong,Xue, Dengqi,Ma, Liying,Zhang, Qiurong,Liu, Hongmin
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p. 443 - 447
(2014/06/10)
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- Thiazolyl-phosphine hydrochloride salts: Effective auxiliary ligands for ruthenium-catalyzed nitrile hydration reactions and related amide bond forming processes in water
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A series of water-soluble N-protonated thiazolyl-phosphine hydrochloride salts have been synthesized and coordinated to the ruthenium(ii) fragment [RuCl2(η6-p-cymene)]. The resulting complexes were evaluated as potential catalysts for the selective hydration of nitriles to primary amides in environmentally friendly aqueous medium. The best results in terms of activity were achieved when tris(5-(2-aminothiazolyl))phosphine trihydrochloride was used as ligand. Using the Ru(ii) complex 9 derived from this salt (3 mol%), the catalytic reactions proceeded cleanly in pure water at 100 °C without the assistance of any additive, affording the desired amides in high yields (>78%) after short reaction periods (0.5-7 h). The process was operative with both aromatic, heteroaromatic, α,β-unsaturated and aliphatic nitriles, and tolerated several functional groups. The utility of 9 in promoting the formation of primary amides in water by catalytic rearrangement of aldoximes and direct coupling of aldehydes with NH2OH·HCl has also been demonstrated.
- Garcia-Alvarez, Rocio,Zablocka, Maria,Crochet, Pascale,Duhayon, Carine,Majoral, Jean-Pierre,Cadierno, Victorio
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p. 2447 - 2456
(2013/09/12)
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- Ru(ii) complexes containing dmso and pyrazolyl ligands as catalysts for nitrile hydration in environmentally friendly media
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The synthesis of two Ru-dmso complexes containing the ligands 2-(3-pyrazolyl)pyridine (pypz-H), and pyrazole (pz-H), [RuIICl 2(pypz-H)(dmso)2], (2) and [RuIICl 2(pz-H)(dmso)3], (3), has been described. Both complexes have been fully characterized in solution through 1H-NMR and UV-Vis techniques and also in the solid state through monocrystal X-ray diffraction analysis. The redox properties of both complexes have also been studied by means of cyclic voltammetry. Exposure of 2 to visible light in acetonitrile produces a substitution of one dmso ligand by a solvent molecule generating a new complex, [RuIICl2(MeCN)(pypz-H)(dmso)] (4). Also, UV-visible spectroscopy points out that complex 2 presents a thermal and photochemical substitution of dmso ligands in aqueous solution. Finally, the reactivity of complexes 2 and 3 has been tested with regard to the hydration of nitriles using water as a single solvent, displaying good efficiency and selectivity for the corresponding amide derivatives. In general, better performance is achieved with complex 3. Reuse of these catalysts in water and glycerol has been explored for the first time in ruthenium-mediated nitrile hydration catalysis.
- Ferrer, íngrid,Rich, Jordi,Fontrodona, Xavier,Rodríguez, Montserrat,Romero, Isabel
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p. 13461 - 13469
(2013/09/23)
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- Natural kaolin supported sulfuric acid as an efficient catalyst for selective hydrolysis of nitriles to amides
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The natural kaolin supported sulfuric acid as an efficient catalyst for selective hydrolysis of nitriles to amides was investigated. The nitrile (4 mmol) was dissolved in water (10 mL) in the presence of kaolin and refluxed for 24 h. The crude product was extracted with ethyl acetate in 55-80% yields after completion of the reaction (monitored by TLC). Careful neutralization of all reaction mixtures were carried out to pH = 7 for exact monitoring of reaction for possible formation of carboxylic acid. The products were characterized by IR and 1H NMR spectroscopy and also their melting points are compared with authentic samples. The disappearance of one strong and sharp absorption band (CN stretching band), and the appearance of two NH2 stretching bands in 3370 and 3320 cm-1 and carboxamide stretching in 1650 cm-1 in the IR spectra, were evidence for the formation of primary amides.
- Gordi, Zinat,Eshghi, Hossein
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experimental part
p. 715 - 718
(2011/10/08)
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- Process for Hair Dyeing Comprising Application of Composite Pigment
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Disclosed is a process for dyeing of keratin-containing fibers comprising treating the fibers with at least one functionalized particle comprising on the surface an organic chromophore which is bound via a bridge member, wherein the particles are based on SiO2, Al2O3 or mixtures thereof, and the functionalized particles carry a positive charge.
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- Synthesis and evaluation of antitubercular activity of glycosyl thio- and sulfonyl acetamide derivatives
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A series of glycosyl thioacetamide and glycosyl sulfonyl acetamide derivatives have been prepared following a convenient reaction protocol and evaluated for their antitubercular activity against Mycobacterium tuberculosis H37Rv. Amongst 32 compounds evaluated 3 compounds were effective in inhibiting mycobacterial growth at MIC of 6.25 μg/mL, 6 compounds at MIC of 3.125 μg/mL and 1 compound at MIC of 1.56 μg/mL. All active compounds were found nontoxic in Vero cell lines and mice bone marrow macrophages.
- Ghosh, Samir,Tiwari, Pallavi,Pandey, Shashi,Misra, Anup Kumar,Chaturvedi, Vinita,Gaikwad, Anil,Bhatnagar, Shalini,Sinha, Sudhir
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experimental part
p. 4002 - 4005
(2009/04/06)
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- A facile hydration of nitriles into amides by Al2O3/MeSO3H (AMA)
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A new and practical method for the conversion of nitriles to amides by employing the A12O3/MeSO3H (AMA) is described.
- Sharghi, Hashem,Sarvari, Mona Hosseini
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p. 207 - 212
(2007/10/03)
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- Hair cosmetic, aminocarboxylic acid amide and method for producing the same
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A hair cosmetic which can impart, to hairs, flexibility, smoothness and oily feeling when the hairs are wetted and smoothness, softness and combing easiness after the hairs are dried are provided, the hair cosmetic comprising an amine represented by the formula (I): Formula (I) (wherein R1 represents a C8-40 alkyl group or alkenyl group or a group represented by the formula R5O—(AO)n—CmH2m— (R5 represents a C8-40 alkyl group or alkenyl group having 8 to 40 carbon atoms, A represents a C2-3 alkylene group, n denotes a number from 0 to 30 in average and m denotes an integer of 2 or 3), R2 represents a C1-5 alkylene group, R3 represents H, a C1-24 alkyl group, alkenyl group or hydroxyalkyl group or a C6-28 aryl group or arylalkyl group, R4 represents H, a C1-5 alkyl group, alkylene group or hydroxyalkyl group or a C6-28 aryl group or arylalkyl group, p denotes an integer from 1 to 3, q and r denote integers from 0 to 2 and p+q+r is equal to 3. Also, the amine (I) can be produced with high selectivity and highly economically by reacting a primary amine with an aminocarboxylic acid to run amidation. An amine represented by the formula (1), its salt or quaternary ammonium salt are also provided: Formula (1)
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- Method of treating cancer
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The present invention relates to methods of treating cancer using a combination of a compound which is a PSA conjugate and a compound which is a inhibitor of prenyl-protein transferase, which methods comprise administering to said mammal, either sequentially in any order or simultaneously, amounts of at least two therapeutic agents selected from a group consisting of a compound which is a PSA conjugate and a compound which is a inhibitor of prenyl-protein transferase. The invention also relates to methods of preparing such compositions.
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- Synthesis, spectral studies and anti-inflammatory activity of glycolamide esters of niflumic acid as potential prodrugs
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In order to reduce the gastric irritation caused by direct contract mechanism of the carboxylic acid group, a series of glycolamide esters of niflumic (CAS 4394-00-7) (1) have been prepared as biolabile prodrugs by reacting appropriate 2-chloroacetamides with niflumic acid. The required 2-chloroacetamides were obtained by the condensation of chloroacetyl chloride and corresponding amine. Their structures were confirmed by UV, IR and 1H NMR spectra. Selected compounds were evaluated for anti-inflammatory activity in carrageenan induced paw oedema in rats at the doses of 45, 90 and 150 mg/kg b.w. Prodrugs showed comparable anti-inflammatory activity (67.1-79.4%) at 150 mg/kg b.w. with respect to niflumic acid (70.3%) at 45 mg/kg b.w., indicating moderate release of niflumic acid in vivo. The highest activity was observed with diethylamine (4) and pyrrolidine (9) derivatives.
- Gadad, Andanappa K.,Bhat, Shailija,Tegeli, Varsha S.,Redasani, Vivek V.
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p. 817 - 821
(2007/10/03)
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- α-and β-amino acid hydroxyethlamino sulfonamides useful as retroviral protease inhibitors
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α- and β-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
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- Inhibitors of prenyl-protein transferase
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The present invention comprises piperazinone-containing compounds which inhibit prenyl-protein transferases, including famesyl-protein transferase and geranylgeranyl-protein transferase type I. Such therapeutic compounds are useful in the treatment of cancer.
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- Inhibitors of prenyl-protein transferase
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The present invention comprises piperazinone-containing compounds, which may be useful as inhibitors of prenyl-protein transferases, including farnesyl-protein transferase and geranylgeranyl-protein transferase type I. Such therapeutic compounds are useful in the treatment of cancer.
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- INHIBITORS OF PRENYL-PROTEIN TRANSFERASE
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The present invention is directed to compounds which inhibit prenyl-protein transferases, farnesyl-protein transferase and geranylgeranyl-protein transferase type I, and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and geranylgeranyl-protein transferase type I and the prenylation of the oncogene protein RAS.
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- Pyrazolopyrimidines as therapeutic agents
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The present invention provides compounds of Formula I, including pharmaceutically acceptable salts and/or prodrugs thereof, where G, R2, and R3 are defined as described herein.
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- Antimicrobial wipes which provide improved residual benefit versus gram positive bacteria
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The present invention relates to an antimicrobial wipe comprising a porous or absorbent sheet impregnated with an antimicrobial cleansing composition, wherein the antimicrobial cleansing composition comprises from about 0.001% to about 5.0%, by weight of the antimicrobial cleansing composition, of an antimicrobial active; from about 0.05% to about 10%, by weight of the antimicrobial cleansing composition, of an anionic surfactant; from about 0.1% to about 10%, by weight of the antimicrobial cleansing composition, of a proton donating agent; and from about 3% to about 99.85%, by weight of the antimicrobial cleansing composition, water; wherein the composition is adjusted to a pH of from about 3.0 to about 6.0; wherein the antimicrobial cleansing composition has a Gram Positive Residual Effectiveness Index of greater than about 0.5; and wherein the antimicrobial cleansing composition has a Mildness Index of less than about 0.3. The invention also encompasses methods for cleansing skin and providing residual effectiveness versus Gram positive bacteria using these products.
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- Inhibitors of prenyl-protein transferase
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The present invention is directed to peptidomimetic piperazine-containing macrocyclic compounds which inhibit a prenyl-protein transferase (FTase) and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
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- A new synthesis of 1,2,4-triazolin-5-ones: Application to the convergent synthesis of an NK1 antagonist
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Chlorotriazolinone 4 has been synthesised in a single step via the novel condensation of semicarbazide hydrochloride with orthoester 8. Alkylation of secondary amine 3 with compound 4 proceeds in 99% yield to afford the target NK1 antagonist 1. (C) 2000 Published by Elsevier Science Ltd.
- Cowden,Wilson,Bishop,Cottrell,Davies,Dolling
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p. 8661 - 8664
(2007/10/03)
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- Synthesis of benzo fused heterocyclic sulfonyl chlorides
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A process for preparing a benzo fused heterocyclic sulfonyl halide comprising reacting a benzo fused heterocyclic compound with an SO3 complex in the presence of a water immiscible, non-reactive solvent, at a temperature of from about 0 DEG C. to about 75 DEG C., cooling, if necessary, to a temperature of from about -25 DEG C. to about 65 DEG C. and then adding oxalyl halide.
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- Piperidine derivatives
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The present invention relates to compounds of the formula wherein X is -O- or -CH2-; Y is -C(O)-, -(CH2)n- or -N(CH3)-; n is 1 or 2 or X and Y taken together are -CH=CH-Z is -NH-, -CH2-, -O- or =CH-; A1 is a group B is -(CH2)m-; m is 0, 1 or 2; R1 and R2 are each independently hydrogen or lower alkyl; R3 is hydrogen or halogen; R4 is hydrogen or hydroxy and the dotted line is (-CH2-CH2-)n, and n' is 0 or 1 and to pharmaceutically acceptable acid addition salts thereof. The compounds of the present invention are antagonists of the OFQ receptor. Consequently they will be useful in the treatment of memory and attention deficits, psychiatric, neurological and physiological disorders, especially, but not limited to, amelioration of symptoms of anxiety and stress disorders, depression, memory loss due to Alzheimer's disease or other dementias, epilepsy and convulsions, acute and/or chronic pain conditions, symptoms of addictive drug withdrawal, control of water balance, Na+ excretion and arterial blood pressure disorders and metabolic disorders such as obesity.
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- Azulene derivatives
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The invention provides novel azulene derivatives of general formula I wherein R1 to R6 have the significance given in the description, as well as their tautomers, enantiomers, diastereomers, racemates and physiologically compatible salts or esters and substances which are hydrolyzed or metabolized in vivo to compounds of formula I. The invention is also concerned with a process and intermediates for the manufacture of the above compounds, pharmaceutical compositions which contain such compounds as well as the use of these compounds in the treatment of inflammatory conditions.
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- Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
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PCT No. PCT/US94/09139 Sec. 371 Date Jan. 24, 1996 Sec. 102(e) Date Jan. 24, 1996 PCT Filed Aug. 23, 1994 PCT Pub. No. WO95/06030 PCT Pub. Date Mar. 2, 1995The invention relates to sulfonamide-containing hydroxyethylamine protease inhibitor compounds, their process of making, composition and method of use for inhibiting retroviral proteases such as human immunodeficiency virus.
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- alpha - and beta -amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
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alpha - and beta -amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
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- Mild, rinse-off antimicrobial liquid cleansing compositions containing salicyclic acid
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The present invention relates to a rinse-off antimicrobial cleansing composition comprising from about 0.1% to about 5.0%, by weight of the cleansing composition, of an antimicrobial active; from about 6% to about 16%, by weight of the cleansing composition, of an anionic surfactant, wherein at least about 67% of the anionic surfactant is selected from the group consisting of Class A surfactants, Class C surfactants, and mixtures thereof, wherein the ratio of Class A surfactant to Class C is from about 100:0 to about 1.5:1; from about 2% to about 4%, by weight of the cleansing composition, of a proton donating agent having a Biological Activity Index, Z, of greater than about 0.75, wherein the proton donating agent is such that the composition is essentially free of C4-C20 alkyl fatty acid, and wherein from about 0.15% to about 2%, by weight of the cleansing composition, of the proton donating agent is salicylic acid; a mildness enhancing agent selected from the group consisting of from about 20% to about 70%, by weight of the anionic surfactant, of a mildness enhancing cosurfactant; from about 0.1% to about 1.0%, by weight of the cleansing composition, of a mildness enhancing polymer; and mixtures thereof, and from about 35% to about 95.75%, by weight of the cleansing composition, of water; wherein the composition is adjusted to a pH of greater than about 3 and less than about 6. The invention also encompasses methods for cleansing skin and providing residual effectiveness versus Gram negative bacteria using these products.
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- Selective conversion of nitriles to amides by Amberlyst A-26 supported hydroperoxide
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A mild, efficient and selective conversion of nitriles to amides is achieved by employing Amberlyst A-26 supported hydroperoxide, which is prepared in situ from hydrogen peroxide and Amberlyst A-26 (OH- form). Nitriles and dinitriles are transformed to their corresponding amides and diamides, respectively. Reactions proceed within 0.5-5 hr upon addition of a catalytic amount of Amberlyst A 26(OH-) to a methanolic solution of nitrile and hydrogen peroxide (35%), at room temperature.
- Mansour Lakouraj,Bahrami
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p. 974 - 975
(2007/10/03)
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- AMINO ACID HYDROXYETHYLAMINO SULFONAMIDE RETROVIRAL PROTEASE INHIBITORS
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Described herein is a retroviral protease inhibiting compound of the formula: STR1 or a pharmaceutically acceptable salt, prodrug or ester thereof.
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- INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE
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The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras
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- INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE
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The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras
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- Mild, rinse-off antimicrobial liquid cleansing compositions which provide residual benefit versus gram negative bacteria
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The present invention relates to a rinse-off antimicrobial cleansing composition comprising from about 0.001% to about 5% of an antimicrobial active, from about 1% to about 80% of an anionic surfactant, from about 0.1% to about 12% of a proton donating agent; and from about 3% to about 98.899% of water, wherein the composition is adjusted to a pH of from about 3.0 to about 6.0, wherein the rinse-off antimicrobial cleansing composition has a Gram Negative Residual Effectiveness Index of greater than about 0.3, and wherein the rinse-off antimicrobial cleansing composition has a Mildness Index of greater than 0.3. The invention also encompasses methods for cleansing skin and providing residual effectiveness versus Gram negative bacteria using these products.
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- Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
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Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
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- β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
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α- and β-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
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- A facile hydration of nitriles by dimethyldioxirane
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A new and practical method for the conversion of nitriles to amides by employing the dimethyldioxirane, which is prepared in situ from acetone and oxone, is described.
- Bose, D. Subhas,Baquer, Syed M.
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p. 3119 - 3123
(2007/10/03)
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- Preparation process of aminoacetamide derivative
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Disclosed herein are novel processes for preparing aminoacetamide derivatives, wherein: (1) a secondary amine is reacted with a 2-haloacetamide in the presence or absence of at least one solvent selected from water, lower alcohols, aromatic solvents and acetic acid esters; (2) an N-benzylideneamine derivative is reacted with dimethyl sulfate or diethyl sulfate to form a secondary amine, and this secondary amine is then reacted with a 2-haloacetamide; and (3) a primary amine is reacted with benzaldehyde to form an N-benzylideneamine derivative, this product is then reacted with dimethyl sulfate or diethyl sulfate to form a secondary amine, and this secondary amine is further reacted with a 2-haloacetamide. The 2-aminoacetamide derivatives are useful as intermediates for the preparation of novel antibiotics.
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- Arylalkyl-amines and -amides having anticonvulsant and neuroprotective properties
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There is provided a method of treatment of neurological disorders, such as epilepsy, stroke and cerebral ischaemia, which comprises the administration of a compound of Formula I: STR1 wherein, Ar1 and Ar2, which may be the same or different, independently represent phenyl or phenyl substituted by one or more of amino, nitro, halogen, hydroxy, C1 to 6 alkoxy, C1 to 6 alkyl or cyano; R1 represents hydrogen, C1 to 6 alkyl, C1 to 6 alkoxycarbonyl; R2 represents hydrogen or COCH2 NH2 ; R3 represents hydrogen or C1 to 6 alkyl; in addition, when R2 represents hydrogen either one or both of Ar1 and Ar2 may also represent 2-, 3- or 4-pyridinyl and R1 may also represent trihalomethyl; or a pharmaceutically acceptable salt thereof. Some of the compounds of formula I are novel, and these are also provided, together with pharmaceutical compositions containing the novel compounds.
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