- Design and synthesis of thiourea derivatives with sulfur-containing heterocyclic scaffolds as potential tyrosinase inhibitors
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Tyrosinase is a key enzyme during the production of melanins in plants and animals. A class of novel N-aryl-N′-substituted phenylthiourea derivatives (3a-i, 6a-k) were designed, synthesized and their inhibitory effects on the diphenolase activity of mushroom tyrosinase were evaluated. The results showed some 4,5,6,7-tetrahydro-2-[[(phenylamino)thioxomethyl]amino]-benzo[b]thiophene-3-carboxylic acid derivatives (3a-i) exhibited moderate inhibitory potency on diphenolase activity of tyrosinase. When the scaffold of 4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid was replaced with 2-(1,3,4-thiadiazol-2-yl)thio acetic acid, the inhibitory activity of compounds (6a-k) against tyrosinase was improved obviously; especially, the inhibitory activity of compound 6h (IC50 = 6.13 μM) is significantly higher than kojic acid (IC50 = 33.3 μM). Moreover, the analysis on inhibition mechanism revealed that compound 6h might plays the role as a noncompetitive inhibitor.
- Liu, Pingping,Shu, Chen,Liu, Lujie,Huang, Qingchun,Peng, Yanqing
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- The discovery of a highly selective 5,6,7,8-Tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one SIRT2 Inhibitor that is Neuroprotective in an in vitro Parkinson's Disease Model
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Sirtuins, NAD+-dependent histone deacetylases (HDACs), have recently emerged as potential therapeutic targets for the treatment of a variety of diseases. The discovery of potent and iso-form-selective inhibitors of this enzyme family should pro
- Di Fruscia, Paolo,Zacharioudakis, Emmanouil,Liu, Chang,Moniot, Sébastien,Laohasinnarong, Sasiwan,Khongkow, Mattaka,Harrison, Ian F.,Koltsida, Konstantina,Reynolds, Christopher R.,Schmidtkunz, Karin,Jung, Manfred,Chapman, Kathryn L.,Steegborn, Clemens,Dexter, David T.,Sternberg, Michael J.E.,Lam, Eric W.-F.,Fuchter, Matthew J.
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- Physicochemical properties of novel methyl 2-{(E)-[(2-hydroxynaphthalen-1-yl)methylidene] amino}-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxylate as turn-off fluorometric chemosensor for detection Fe3 + ion
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Schiff base (HATC) was synthesized by the reaction of 2-hydroxy-1-naphthaldehyde with methyl 2-amino-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxylate. Structure of HATC was confirmed by the EI-MA, IR, 1H NMR, 13C NMR and elemental analysis. Photophysical and physicochemical studies of the HATC such as oscillator strength, extinction coefficient, transition dipole moment, fluorescence quantum yield and stokes shift was investigated in different solvents on the basis of polarities. The observed bathochromic absorbance, emission band and different parameter's on changing the polarity of the solvents. HATC interact with the various metal ions were also studied by spectrofluorophotometer. Schiff base used as on- off type fluorescent chemosensor for sensitive and selective detection of Fe3 + ion. Complexation stoichiometry and mechanism of quenching were determined from Benesi–Hildebrand and Stern-Volmer plot.
- Khan, Salman A.,Asiri, Abdullah M.
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- A simple synthesis of alkyl 2-aminobenzo[ b ]thiophene-3-carboxylates via an unexpected dehydrogenation of alkyl 2-amino-4,5,6,7-tetrahydrobenzo[ b ]thiophene-3-carboxylates
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A simple method for the preparation of alkyl 2-aminobenzo[b]thiophene-3-carboxylates is described. Alkyl 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylates, generated from the Gewald three-component reaction between cyclohexanones, alkyl cyanoacet
- Adib, Mehdi,Bayanati, Maryam,Soheilizad, Mehdi,Ghazvini, Helia Janatian,Tajbakhsh, Mahmood,Amanlou, Massoud
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- Microwave-assisted synthesis of 2-aminothiophene derivatives via improved gewald reactions
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In this paper, a new and efficient method was developed to prepare 2-aminothiophene derivatives through improved Gewald reaction. Thirty-one final products were synthesized under microwave radiation for 30 min with 57%-95% isolated yields. All the product
- Ruan, Bankang,Zhang, Zhiyan,Huang, Lei,Xu, Chao,Li, Luolan
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p. 2007 - 2018
(2021/09/29)
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- Design, Synthesis, and Structure-Activity Relationship of N-Aryl- N′-(thiophen-2-yl)thiourea Derivatives as Novel and Specific Human TLR1/2 Agonists for Potential Cancer Immunotherapy
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The previous virtual screening of ten million compounds yielded two novel nonlipopeptide-like chemotypes as TLR2 agonists. Herein, we present the chemical optimization of our initial hit, 1-phenyl-3-(thiophen-2-yl)urea, which resulted in the identification of SMU-C80 (EC50 = 31.02 ± 1.01 nM) as a TLR2-specific agonist with a 370-fold improvement in bioactivity. Mechanistic studies revealed that SMU-C80, through TLR1/2, recruits the adaptor protein MyD88 and triggers the NF-κB pathway to release cytokines such as TNF-α and IL-1β from human, but not murine, cells. To the best of our knowledge, it is the first species-specific TLR1/2 agonist reported until now. Moreover, SMU-C80 increased the percentage of T, B, and NK cells ex vivo and activated the immune cells, which suppressed cancer cell growth in vitro. In summary, we obtained a highly efficient and specific human TLR1/2 agonist that acts through the MyD88 and NF-κB pathway, facilitating cytokine release and the simultaneous activation of immune cells that in turn affects the apoptosis of cancer cells.
- Chen, Zhipeng,Zhang, Lina,Yang, Junjie,Zheng, Lu,Hu, Fanjie,Duan, Siqin,Nandakumar, Kutty Selva,Liu, Shuwen,Yin, Hang,Cheng, Kui
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supporting information
p. 7371 - 7389
(2021/06/28)
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- Room temperature synthesis and characterization of novel Bi(III) complex with 2-amino-3-carbomethoxy-4,5,6,7-tetrahydrobenzo[b]thiophene as potential antimicrobial agent
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A novel bismuth(III) complex with 2-amino-3-carbomethoxy-4,5,6,7-tetrahydrobenzo[b]thiophene (ACTT) as a ligand have been synthesized. The novel complex was characterized on the basis of its IR, NMR, elemental analysis and MS spectral data. It was found that the ligand behaves as a monodentate chelating agent and bonds to the metal ion through the nitrogen atom of the amino group to form the [BiIII(ACTT)6]Cl3 complex. The new complex compound displayed significant antimicrobial activity (MIC = 8-32 μg/mL) against Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Shigella flexneri, Candida albicans, Candida tropicalis and Cryptococcus neoformans.
- Djeukoua, Sorel Kamal Dimo,Doungmo, Giscard,Ekom, Steve Endeguele,Fondjo, Emmanuel Sopbué,Kuiate, Jules Roger,Siéwé, Désire André,Simon, Peter F. W.,Tamokou, Jean-de-Dieu,Tsopmo, Appolinnaire,Walters, Mallory E.
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p. 203 - 211
(2020/03/30)
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- Chromium (III) complex of 2-amino-3-carbomethoxy-4,5,6,7-tetrahydrobenzo[B] thiophene: synthesis, characterization and antimicrobial activity
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A new chromium (III) coordination compound of 2-amino-3-carbomethoxy-4,5,6,7-tetrahydrobenzo[b]thiophene (ACTT) (3) with Cr(NO3)3.9H2O in methanol at room temperature for 48 hours has been prepared. The composition of the new complex compound (4) has been confirmed by a number of instrumental methods including IR, NMR, MS and elemental analysis. It was found that the ACTT ligand behaves as bidentate chelating agent and coordinates to the central metal ion through the nitrogen atom of the amino-group and the oxygen atom of the carbonyl function of the ester group. The results showed that in the coordination sphere of the complex, the metal ion is coordinated by three chelating ACTT ligands. In the structure of the cation core [Cr(ACTT)3]3+, the three ACTT ligands are linked to the chromium ion through three Cr-N and three Cr-O bonds forming a square bipyramidal geometry. The metal complex and the ACTT ligand were screened for their antimicrobial activities against several strains of bacteria (Staphylococcus aureus ATCC25923, Escherichia coli S2 (1), Bacillus subtilis, Staphylococcus aureus, Pseudomonas aeruginosa ATCC27853, Shigella flexneri SDINT) and fungi (Candida albicans ATCC10231, Candida tropicalis PK233, Cryptococcus neoformans H99). The chromium complex showed promising antimicrobial activity against the microorganisms with minimum inhibitory values between 4 and 16 μg/mL.
- Dimo, Kamal Sorel Djeukoua,Doungmo, Giscard,Ekom, Steve Endeguele,Fondjo, Emmanuel Sopbué,Kuiate, Jules-Roger,Siéwé, Désire André,Simon, Peter F. W.,Tamokou, Jean-De-Dieu,Tsopmo, Appolinnaire,Walters, Mallory E.
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p. 4908 - 4913
(2020/11/16)
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- In vitro and in vivo evaluation of the antimalarial MMV665831 and structural analogs
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Antimalarial candidates possessing novel mechanisms of action are needed to control drug resistant Plasmodium falciparum. We were drawn to Malaria Box compound 1 (MMV665831) by virtue of its excellent in vitro potency, and twelve analogs were prepared to probe its structure–activity relationship. Modulation of the diethyl amino group was fruitful, producing compound 25, which was twice as potent as 1 against cultured parasites. Efforts were made to modify the phenolic Mannich base functionality of 1, to prevent formation of a reactive quinone methide. Homologated analog 28 had reduced potency relative to 1, but still inhibited growth with EC50 ≤ 200 nM. Thus, the antimalarial activity of 1 does not derive from quinone methide formation. Chemical stability studies on dimethyl analog 2 showed remarkable hydrolytic stability of both the phenolic Mannich base and ethyl ester moieties, and 1 was evaluated for in vivo efficacy in P. berghei-infected mice (40 mg/kg, oral). Unfortunately, no reduction in parasitemia was seen relative to control. These results are discussed in the context of measured plasma and hepatocyte stabilities, with reference to structurally-related, orally-efficacious antimalarials.
- Carlier, Paul R.,Ding, Sha,Fike, Katherine R.,Klemba, Michael
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supporting information
(2020/07/03)
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- Synthesis of urea analogues bearing N-alkyl-N’-(thiophen-2-yl) scaffold and evaluation of their innate immune response to toll-like receptors
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Previous high throughput virtual screening of 10 million-compound and following cell based validation led to the discovery of a novel, nonlipopeptide-like chemotype ZINC 6662436, as toll-like receptor 2 (TLR2) agonists. In this report, compounds belonging
- Chen, Zhipeng,Cen, Xiaohong,Yang, Junjie,Lin, Zhiman,Liu, Meihuan,Cheng, Kui
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- Synthesis of novel 2-(1-adamantanylcarboxamido)thiophene derivatives. Selective cannabinoid type 2 (CB2) receptor agonists as potential agents for the treatment of skin inflammatory disease
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A set of CB2R ligands, based on the thiophene scaffold, was synthesized and evaluated in in vitro assays. Compounds 8c-i, k, l, bearing the 3-carboxylate and 2-(adamantan-1-yl)carboxamido groups together with apolar alkyl/aryl substituents at 5-position or at 4- and 5-positions of the thiophene ring possess high CB2R affinity at low nanomolar concentration, good receptor selectivity, and agonistic functional activity. The full agonist 8g, showing the best balance between receptor affinity and selectivity, was tested in vitro in an experimental model of allergic contact dermatitis and proved to be able to block the release of MCP-2 in HaCaT cells at 10 μM concentration.
- Mugnaini, Claudia,Rabbito, Alessandro,Brizzi, Antonella,Palombi, Nastasja,Petrosino, Stefania,Verde, Roberta,Di Marzo, Vincenzo,Ligresti, Alessia,Corelli, Federico
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p. 239 - 251
(2018/10/24)
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- Subtle modifications to a thieno[2,3-d]pyrimidine scaffold yield negative allosteric modulators and agonists of the dopamine D2 receptor
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We recently described a structurally novel series of negative allosteric modulators (NAMs) of the dopamine D2 receptor (D2R) based on thieno[2,3-d]pyrimidine 1, showing it can be structurally simplified to reveal low molecular weight, fragment-like NAMs that retain robust negative cooperativity, such as 3. Herein, we report the synthesis and functional profiling of analogues of 3, placing specific emphasis on examining secondary and tertiary amino substituents at the 4-position, combined with a range of substituents at the 5/6-positions (e.g. aromatic/aliphatic carbocycles). We identify analogues with diverse pharmacology at the D2R including NAMs with sub-μM affinity (9h) and, surprisingly, low efficacy partial agonists (9d and 9i).
- Fyfe, Tim J.,Kellam, Barrie,Mistry, Shailesh N.,Scammells, Peter J.,Lane, J. Robert,Capuano, Ben
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p. 474 - 490
(2019/03/07)
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- Development of thieno- and benzopyrimidinone inhibitors of the Hedgehog signaling pathway reveals PDE4-dependent and PDE4-independent mechanisms of action
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From a high content in vivo screen for modulators of developmental patterning in embryonic zebrafish, we previously identified eggmanone (EGM1, 3) as a Hedgehog (Hh) signaling inhibitor functioning downstream of Smoothened. Phenotypic optimization studies for in vitro probe development utilizing a Gli transcription-linked stable luciferase reporter cell line identified EGM1 analogs with improved potency and aqueous solubility. Mechanistic profiling of optimized analogs indicated two distinct scaffold clusters: PDE4 inhibitors able to inhibit downstream of Sufu, and PDE4-independent Hh inhibitors functioning between Smo and Sufu. Each class represents valuable in vitro probes for elucidating the complex mechanisms of Hh regulation.
- Hempel, Jonathan E.,Cadar, Adrian G.,Hong, Charles C.
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supporting information
p. 1947 - 1953
(2016/04/05)
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- Syntheses and biological evaluation of 2-amino-3-acyl- tetrahydrobenzothiophene derivatives; Antibacterial agents with antivirulence activity
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Developing new compounds targeting virulence factors (e.g., inhibition of pilus assembly by pilicides) is a promising approach to combating bacterial infection. A high-throughput screening campaign of a library of 17500 small molecules identified 2-amino-3-acyl-tetrahydrobenzothiophene derivatives (hits 2 and 3) as novel inhibitors of pili-dependent biofilm formation in a uropathogenic Escherichia coli strain UTI89. Based on compounds 2 and 3 as the starting point, we designed and synthesized a series of structurally related analogs and investigated their activity against biofilm formation of E. coli UTI89. Systematic structural modification of the initial hits provided valuable information on their SARs for further optimization. In addition, small structural changes to the parent molecules resulted in low micromolar inhibitors (20-23) of E. coli biofilm development without an effect on bacterial growth. The hit compound 3 and its analog 20 were confirmed to prevent pili formation in a hemagglutination (HA) titer assay and electron microscopy (EM) measurements. These findings suggest that 2-amino-3-acyl-tetrahydrobenzothiophenes may serve as a new class of compounds for further elaboration as antibacterial agents with antivirulence activity.
- The Dang, Hung,Chorell, Erik,Uvell, Hanna,Pinkner, Jerome S.,Hultgren, Scott J.,Almqvist, Fredrik
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p. 1942 - 1956
(2014/03/21)
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- Effect of substituents and encapsulation on the catalytic activity of copper(II) complexes of two tridentate Schiff base ligands based on thiophene: Benzyl alcohol and phenol oxidation reactions
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Encapsulation of Cu(II) complexes of methyl-2-(2-hydroxybenzylideneamino)- 4,5,6,7-tetrahydrobenzo[b]-thiophene-3-carboxylate (HL1) and 2-ethyl-4-methyl 5-(2-hydroxybenzylideneamino)-3-methylthiophene-2,4- dicarboxylate (HL2) in the supercages of zeolite NaY was performed by the flexible ligand method. The neat and encapsulated complexes were characterized by physicochemical and spectroscopic methods and employed as catalysts for oxidation of benzyl alcohol and phenol. The encapsulated complexes were both more reactive and stable as catalysts than the corresponding free complexes. The encapsulated complexes could be reused several times. Complexes of HL2 were more reactive than those of HL1, probably due to the electron-withdrawing effect of the CO2Et group.
- Mobinikhaledi, Akbar,Zendehdel, Mojgan,Safari, Parvin
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p. 431 - 442
(2014/05/20)
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- A simple synthesis of alkyl 2-aminobenzo[ b ]thiophene-3-carboxylates via an unexpected dehydrogenation of alkyl 2-amino-4,5,6,7-tetrahydrobenzo[ b ]thiophene-3-carboxylates
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A simple method for the preparation of alkyl 2-aminobenzo[b]thiophene-3-carboxylates is described. Alkyl 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylates, generated from the Gewald three-component reaction between cyclohexanones, alkyl cyanoacetates and sulfur, undergo dehydrogenation in benzonitrile under an air atmosphere to afford alkyl 2-aminobenzo[b]thiophene-3-carboxylates in good to excellent yields.
- Adib, Mehdi,Bayanati, Maryam,Soheilizad, Mehdi,Ghazvini, Helia Janatian,Tajbakhsh, Mahmood,Amanlou, Massoud
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p. 2918 - 2922
(2015/01/09)
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- Synthesis and pharmacological characterization of 2-(acylamino)thiophene derivatives as metabolically stable, orally effective, positive allosteric modulators of the GABAB receptor
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Two recently reported hit compounds, COR627 and COR628, underpinned the development of a series of 2-(acylamino)thiophene derivatives. Some of these compounds displayed significant activity in vitro as positive allosteric modulators of the GABAB receptor by potentiating GTPγS stimulation induced by GABA at 2.5 and 25 μM while failing to exhibit intrinsic agonist activity. Compounds were also found to be effective in vivo, potentiating baclofen-induced sedation/hypnosis in DBA mice when administered either intraperitoneally or intragastrically. Although displaying a lower potency in vitro than the reference compound GS39783, the new compounds 6, 10, and 11 exhibited a higher efficacy in vivo: combination of these compounds with a per se nonsedative dose of baclofen resulted in shorter onset and longer duration of the loss of righting reflex in mice. Test compounds showed cytotoxic effects at concentrations comparable to or higher than those of GS39783 or BHF177.
- Mugnaini, Claudia,Pedani, Valentina,Casu, Angelo,Lobina, Carla,Casti, Alberto,MacCioni, Paola,Porcu, Alessandra,Giunta, Daniela,Lamponi, Stefania,Solinas, Maurizio,Dragoni, Stefania,Valoti, Massimo,Colombo, Giancarlo,Castelli, Maria Paola,Gessa, Gian Luigi,Corelli, Federico
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p. 3620 - 3635
(2013/06/27)
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- TRICYCLIC PROTEASOME ACTIVITY ENHANCING COMPOUNDS
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Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies.
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Page/Page column 47-48
(2012/02/05)
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- Synthesis of some novel methyl- and ethyl-2-aminothiophene-3-carboxylate and related Schiff-bases
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Methyl- and ethyl-2-amino thiophene-3-carboxylate derivatives 1(a-h) were synthesized by a simple one-pot condensation reaction of the ketone, elemental sulphur and methyl- or ethylcyanoacetate in the presence of morpholine as a catalyst. Further reaction of these compounds with salicylaldehyde gave related Schiff-bases, 2(a-e). Yields of products following recrystallization from ethanol were in the range of 70-85 %. 1H NMR and IR spectra and elemental analysis data were used to identification of these compounds.
- Mobinikhaledi,Kalhor,Taheri
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experimental part
p. 7399 - 7404
(2012/07/17)
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- 1,4-Thienodiazepine-2,5-diones via MCR (I): Synthesis, Virtual Space and p53-Mdm2 Activity
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1,4-Thienodiazepine-2,5-diones have been synthesized via the Ugi-Deprotection-Cyclization (UDC) approach starting from Gewald 2-aminothiophenes in a convergent and versatile manner. The resulting scaffold is unprecedented, cyclic, and peptidomimetic with four points of diversity introduced from readily available starting materials. In addition to eighteen synthesized and characterized compounds, a virtual compound library was generated and evaluated for chemical space distribution and drug-like properties. A small focused compound library of 1,4-thienodiazepine-2,5-diones has been screened for the activity against p53-Mdm2 interaction. Biological evaluations demonstrated that some compounds exhibited promising antagonistic activity.
- Huang, Yijun,Wolf, Siglinde,Bista, Michal,Meireles, Lidio,Camacho, Carlos,Holak, Tad A.,Doemling, Alexander
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experimental part
p. 116 - 129
(2011/03/20)
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- Azo dyes
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The azo dyes relate to thiophene azo dyes of the general formula: where R1 is Cyano or C1-C5 alkoxy carbonyl; R2 is hydrogen, halogene, C1-C2 alkyl, phenyl, or substituted phenyl; and R3 is C1-C5 alkoxy carbonyl, C1-C4 alkanoyl, benzoyl, phenyl, alkyl substituted phenyl, or alkoxy phenyl; or R2 and R3 are fused cycloalkane with C3-C5.
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(2010/04/25)
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- Discovery of novel thieno[2,3-d]pyrimidin-4-yl hydrazone-based inhibitors of Cyclin D1-CDK4: Synthesis, biological evaluation, and structure-activity relationships
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The synthesis and evaluation of new analogues of thieno[2,3-d]pyrimidin-4-yl hydrazones are described. 2-Pyrdinecarboxaldehyde [6-(tert-butyl)thieno[2,3-d]pyrimidine-4-yl]hydrazone derivatives have been identified as cyclin-dependent kinase 4 (CDK4) inhibitors. The potency, selectivity profile, and structure-activity relationship of this series of compounds are discussed.
- Horiuchi, Takao,Chiba, Jun,Uoto, Kouichi,Soga, Tsunehiko
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scheme or table
p. 305 - 308
(2011/02/28)
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- Reactions of some anellated 2-aminothiophenes with electron poor acetylenes
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The reactivity of 2-aminothiophenes in two different anellations: (a) [b]-anellation to a saturated carbocycle and (b) [3,4-c]-anellation to benzopyrans, towards typical acetylenic dienophiles has been investigated. Because of the absence of conjugation, the thiophenes of type (a) do not undergo [4+2]-cycloaddition with acetylenic dienophiles. Instead, the N-vinylated products 2 and 3 were obtained with dimethyl acetylene dicarboxylate (DMAD). Electron poor alkynes react with the thiophenes of type (b) in three main ways: DMAD reacts in a [4+2]-mode in dioxane to give the products 7, 8 and 14; a Michael addition type reaction also takes place at the doubly vinylene homologous carbon atoms (C-1 in the starting materials 4, 9 and 10) in dioxane, methanol or ethanol. Methyl propiolate reacts in a similar way. The doubly N-vinylated product 26 was obtained from 10 in toluene and the C-1 vinylated products 24B and 27 were obtained from 9 in dioxane and 10 in methanol. The reaction of 10 with phenyl ethyl propiolate in dimethylformamide gave no addition product, instead a dimer of the acetylenic reagent was the isolated product. The accuracy of the assigned structures 5, 12 and 13a could be achieved on the basis of a single-crystal X-ray structure analysis of compound 13a. The reaction mechanism and the nature of the isolated products are dependent on the nature of the solvent. No addition reaction was observed between 17 and DMAD. The influence of the N-substitution on the nature of the addition (Michael or Diels-Alder) could be settled through the reactions of 18 and 21 with DMAD, which gave 19 and 14 (via 22), respectively as the only isolable products.
- Sopbué Fondjo, Emmanuel,D?pp, Dietrich,Henkel, Gerald
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p. 7121 - 7131
(2007/10/03)
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- Gewald synthesis of 2-aminothiophenes on a soluble polymer-support
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A variety of polysubstituted thiophenes have been prepared via a solvent-free one-pot microwave assisted Gewald reaction using poly (ethylene glycol) as a soluble polymer support.
- Zhang, Haiqing,Yang, Guichun,Chen, Jianian,Chen, Zuxing
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p. 360 - 361
(2007/10/03)
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- ANTHELMINTIC AND INSECTICIDAL THIOPHENE DERIVATIVES
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Novel anthelmintic compositions containing thiophene derivatives as active ingredients are disclosed.
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- THIENOPYRIMIDINES
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Thienopyrimidines of the formula (I) and their physiologically acceptable salts, in which R1, R2 and X are as defined in claim 1, exhibit phosphodiesterase V inhibition and can be employed for the treatment of illnesses of the cardiovascular system and for the treatment and/or therapy of impotence.
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