- Synthesis of new triazolyl-oxazoline chiral ligands and study of their coordination to Pd(II) metal centers
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We report an improved protocol for the synthesis of TryOx, a family of N,N chiral ligands in which a 1,2,3-triazol-4-yl moiety bears a chiral 2-oxazoline as the substituent in 4 position. TryOxs were successfully employed for the preparation of cationic P
- Scrivanti, Alberto,Sole, Roberto,Bortoluzzi, Marco,Beghetto, Valentina,Bardella, Noemi,Dolmella, Alessandro
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Read Online
- Triazolecarboxamidate Donors as Supporting Ligands for Nickel Olefin Polymerization Catalysts
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To increase the structural diversity of dinucleating platforms that are used in the construction of olefin polymerization catalysts, we are exploring new ligand designs that feature non-Alkoxide/phenoxide bridging groups. In the current study, we demonstr
- Xiao, Dawei,Do, Loi H.
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Read Online
- Copper(I)-chitin biopolymer based: An efficient and recyclable catalyst for click azide–alkyne cycloaddition reactions in water
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The naturally occurring α-chitin biopolymer was employed for the immobilisation of copper(I) ion, resulting into a new bioconjugate complex, namely, Cu(I)-α-chitin (CuI-CHT) with catalytic efficiency in copper-catalysed azide–alkyne cycloaddition reaction
- Bahsis, Lahoucine,Ablouh, El-Houssaine,Hachim, Mouhi Eddine,Anane, Hafid,Taourirte, Moha,Julve, Miguel,Stiriba, Salah-Eddine
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- Design and synthesis of substituted (1-(benzyl)-1: H -1,2,3-triazol-4-yl)(piperazin-1-yl)methanone conjugates: Study on their apoptosis inducing ability and tubulin polymerization inhibition
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A library of substituted (1-(benzyl)-1H-1,2,3-triazol-4-yl)(piperazin-1-yl)methanone derivatives were designed, synthesized and screened for their in vitro cytotoxic activity against BT-474, HeLa, MCF-7, NCI-H460 and HaCaT cells by employing 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Among all the synthesized analogues, compound 10ec displayed the highest cytotoxicity with the IC50 value of 0.99 ± 0.01 μM towards BT-474 cancer cell line. The target compound (10ec) was also evaluated for its tubulin polymerization inhibition study. Detailed biological studies such as acridine orange/ethidium bromide (AO/EB), DAPI and annexin V-FITC/propidium iodide staining assay suggested that compound 10ec induced the apoptosis of BT-474 cells. The clonogenic assay revealed that the inhibition of colony formation in BT-474 cells by 10ec in concentration-dependent manner. Moreover, the flow cytometric analysis revealed that 10ec induced apoptosis via cell cycle arrest at the sub-G1 and G2/M phase. In silico studies of sulfonyl piperazine-integrated triazole conjugates unveil that they possess drug-like properties. According to the molecular modelling studies, compound 10ec binds to the colchicine binding site of the tubulin.
- Alvala, Mallika,Babu, Bathini Nagendra,Devi, Ganthala Parimala,Godugu, Chandraiah,Manasa, Kesari Lakshmi,Nagesh, Narayana,Sigalapalli, Dilep Kumar,Thatikonda, Sowjanya,Vuppaladadium, Sowmya
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p. 1295 - 1302
(2020/12/01)
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- Synthesis and Characterization of Copper(I)‐Cysteine Complex Supported on Magnetic Layered Double Hydroxide as an Efficient and Recyclable Catalyst System for Click Chemistry Using Choline Azide as Reagent and Reaction Medium
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Abstract: In this study, Fe3O4@LDH@cysteine–Cu(I) nanoparticles as a novel and recyclable catalytic system was designed and successfully synthesized. These nanoparticles show high catalytic activity for preparation of the triazole fa
- Pazoki, Farzane,Salamatmanesh, Arefe,Bagheri, Sepideh,Heydari, Akbar
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p. 1186 - 1195
(2019/11/16)
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- ω-Quinazolinonylalkyl aryl ureas as reversible inhibitors of monoacylglycerol lipase
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The serine hydrolase monoacylglycerol lipase (MAGL) is involved in a plethora of pathological conditions, in particular pain and inflammation, various types of cancer, metabolic, neurological and cardiovascular disorders, and is therefore a promising target for drug development. Although a large number of irreversible-acting MAGL inhibitors have been discovered over the past years, there are only few compounds known so far which inhibit the enzyme in a reversible manner. Therefore, much effort is put into the development of novel chemical entities showing reversible inhibitory behavior, which is thought to cause less undesired side effects. To explore a wide range of chemical structures as MAGL binders, we have applied a virtual screening approach by docking small molecules into the crystal structure of human MAGL (hMAGL) and envisaged a library of 45 selected compounds which were then synthesized. Biochemical investigations included the determination of the inhibitory potency on hMAGL and two related hydrolases, i.e. human fatty acid amide hydrolase (hFAAH) and murine cholesterol esterase (mCEase). The most promising candidates from theses analyses, i.e. three ω-quinazolinonylalkyl aryl ureas bearing alkyl spacers of three to five methylene groups, exhibited IC50 values of 20–41 μM and reversible, detergent-insensitive behavior towards hMAGL. Among these compounds, the inhibitor 1-(3,5-bis(trifluoromethyl)phenyl)-3-(4-(4-oxo-3,4-dihydroquinazolin-2-yl)butyl)urea (96) was selected for further kinetic characterization, yielding a dissociation constant Ki = 15.4 μM and a mixed-type inhibition with a pronounced competitive component (α = 8.94). This mode of inhibition was further supported by a docking experiment, which suggested that the inhibitor occupies the substrate binding pocket of hMAGL.
- Dato, Florian M.,Neud?rfl, J?rg-Martin,Gütschow, Michael,Goldfuss, Bernd,Pietsch, Markus
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supporting information
(2019/11/13)
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- Synthesis and biological evaluation of 1-benzyl-N-(2-(phenylamino)pyridin-3-yl)-1H-1,2,3-triazole-4-carboxamides as antimitotic agents
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A library of 1-benzyl-N-(2-(phenylamino)pyridin-3-yl)-1H-1,2,3-triazole-4-carboxamides (7a–al) have been designed, synthesized and screened for their anti-proliferative activity against some selected human cancer cell lines namely DU-145, A-549, MCF-7 and HeLa. Most of them have shown promising cytotoxicity against lung cancer cell line (A549), amongst them 7f was found to be the most potent anti-proliferative congener. Furthermore, 7f exhibited comparable tubulin polymerization inhibition (IC50 value 2.04 μM) to the standard E7010 (IC50 value 2.15 μM). Moreover, flow cytometric analysis revealed that this compound induced apoptosis via cell cycle arrest at G2/M phase in A549 cells. Induction of apoptosis was further observed by examining the mitochondrial membrane potential and was also confirmed by Hoechst staining as well as Annexin V-FITC assays. Furthermore, molecular docking studies indicated that compound 7f binds to the colchicine binding site of the β-tubulin. Thus, 7f exhibits anti-proliferative properties by inhibiting the tubulin polymerization through the binding at the colchicine active site and by induction of apoptosis.
- Prasad, Budaganaboyina,Lakshma Nayak,Srikanth,Baig, Mirza Feroz,Subba Reddy,Babu, Korrapati Suresh,Kamal, Ahmed
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p. 535 - 548
(2018/11/26)
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- Synthesis and evaluation of novel purple acid phosphatase inhibitors
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Transgenic studies in animals have demonstrated a direct association between the level of expression of purple acid phosphatase (PAP; also known as tartrate-resistant acid phosphatase) and the progression of osteoporosis. Consequently, PAP has emerged as
- Hussein, Waleed M.,Feder, Daniel,Schenk, Gerhard,Guddat, Luke W.,McGeary, Ross P.
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- Highly regioselective and sustainable solar click reaction: A new post-synthetic modified triazole organic polymer as a recyclable photocatalyst for regioselective azide-alkyne cycloaddition reaction
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The synthesis of pharmaceutically active 1,2,3-triazoles has been continuously scrutinized in the search for unique and effective catalysts to make the process efficient, green, and sustainable. Here, we are presenting a new visible light active Ni(ii) cyclam-integrated triazole-linked organic polymer (Ni-TLOP) photocatalyst for the synthesis of 1,2,3-triazole compounds with excellent efficiency and regioselectivity. The reaction was studied for a series of substrates and the absolute regioselectivity of a representative triazole product has also been confirmed by X-ray crystallography. The proficiency and chemical orthogonality of the Ni-TLOP are remarkable and it shows enhanced efficiency and regioselectivity. The use of a recyclable photocatalyst and non-hazardous reagents makes the catalytic system sustainable and environmentally friendly. This photocatalyzed click reaction technique has been successfully applied to the expedient synthesis of one of the most sold anti-epileptic drugs rufinamide.
- Yadav, Dolly,Singh, Nem,Kim, Tae Wu,Kim, Jae Young,Park, No-Joong,Baeg, Jin-Ook
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p. 2677 - 2685
(2019/06/13)
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- 4β-amidotriazole linked podophyllotoxin congeners: DNA topoisomerase-IIα inhibition and potential anticancer agents for prostate cancer
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Topoisomerases (topo-I and topo-II) have occupied a significant role in DNA replication, transcription, and are a promising set of antitumor targets. In the present approach, a series of new 4β-amidotriazole linked podophyllotoxin derivatives (10a-i and 1
- Reddy, V. Ganga,Bonam, Srinivasa Reddy,Reddy, T. Srinivasa,Akunuri, Ravikumar,Naidu,Nayak, V. Lakshma,Bhargava, Suresh K.,Kumar, H.M. Sampath,Srihari,Kamal, Ahmed
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p. 595 - 611
(2018/01/01)
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- Copper(I)–Caffeine Complex Immobilized on Silica-Coated Magnetite Nanoparticles: A Recyclable and Eco-friendly Catalyst for Click Chemistry from Organic Halides and Epoxides
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Abstract: Copper(I)–caffeine complex immobilized on silica-coated magnetite nanoparticles was successfully synthesized and fully characterized by analyzing FT-IR, X-ray diffraction, scanning electron microscopy, energy-dispersive X-ray, inductively couple
- Salamatmanesh, Arefe,Kazemi Miraki, Maryam,Yazdani, Elahe,Heydari, Akbar
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p. 3257 - 3268
(2018/09/06)
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- Preparation method of 1-subtituted-1H-1,2,3-triazole-4-carboxylic acid
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The invention provides a preparation method of 1-subtituted-1H-1,2,3-triazole-4-carboxylic acid. The preparation method includes the following steps: 1-substituted-4,5-dibromo-1H-1,2,3-triazole is added to an isopropylmagnesium chloride, such that 1-substituted-4-bromo-1H-1,2,3-triazole is obtained through a reaction; an isopropylmagnesium chloride-lithium chloride complex is added directly, such that a mixture of 1-substituted-1H-1,2,3-triazole-4-carboxylic acid and 1-substituted-4-bromo-1H-1,2,3-triazole-5-carboxylic acid is obtained; a base and iodomethane are added to the mixture, such that methyl 1-substituted-4-bromo-1H-1,2,3-triazole-5-carboxylare is obtained through a reaction; the aqueous layer is adjusted with hydrochloric acid until a pH value is 1-5; extraction is carried out with an organic solvent, and drying and concentration crystallization are carried out, such that 1-substituted-1H-1,2,3-triazole-4-carboxylic acid is obtained. The method is suitable for industrial production, and has a great application value.
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- Catalytic cyclization of 2,3-dibromopropionates with benzyl azides to afford 1-benzyl-1,2,3-triazole-4-carboxylate: The use of A nontoxic bismuth catalyst
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We synthesized 1,2,3-triazoles via the cyclization of 2,3-dibromopropionates with benzyl azides. Bismuth chloride is an efficient catalyst, and the reaction is accelerated by weak bases such as sodium acetate. A variety of functional groups are compatible
- Sun, Hong-Bin,Li, Dong,Xie, Weiping,Deng, Xinlin
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p. 423 - 430
(2016/04/19)
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- Tuning the Hydrophilicity and Hydrophobicity of the Respective Cation and Anion: Reversible Phase Transfer of Ionic Liquids
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The separation and recycling of catalyst and cocatalyst from the products and solvents are of critical importance. In this work, a class of functionalized ionic liquids (ILs) were designed and synthesized, and by tuning the hydrophilicity and hydrophobici
- Yao, Wenhui,Wang, Huiyong,Cui, Guokai,Li, Zhiyong,Zhu, Anlian,Zhang, Suojiang,Wang, Jianji
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supporting information
p. 7934 - 7938
(2016/09/13)
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- Urea assisted copper(I)-catalyzed azide-alkyne cycloaddition reactions in water
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Urea assisting easy and greener synthesis of 1,4-disubstituted 1,2,3-triazoles has been achieved using copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) reaction in water. The click reaction affords notable features, such as high efficiency and regio
- Ali, Abdul Aziz,Chetia, Mitali,Sarma, Diganta
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p. 1711 - 1714
(2016/04/04)
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- Recyclable Cu(i)/melanin dots for cycloaddition, bioconjugation and cell labelling
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Development of biocompatible and high-performance heterogeneous catalysts for bioconjugation and cell labeling is highly challenging. Melanin has previously been used as a target for melanoma imaging and therapy. Herein, this important biomarker was trans
- Sun, Yao,Hong, Suhyun,Ma, Xiaowei,Cheng, Kai,Wang, Jing,Zhang, Zhe,Yang, Meng,Jiang, Yuxin,Hong, Xuechuan,Cheng, Zhen
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p. 5888 - 5892
(2016/08/31)
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- TRIAZOLE MODIFIED COUMARIN AND BIPHENYL AMIDE-BASED HSP90 INHIBITORS
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Provided herein are compounds of the formulas:. which are 90-kDa heat shock protein inhibitors. Pharmaceutical compositions of the compounds are also provided. In some aspects, these compounds may be used for the treatment of diseases, including cancer, e
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Page/Page column 58
(2016/01/01)
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- Recyclable catalytic dendrimer nanoreactor for part-per-million Cu I catalysis of "click" chemistry in water
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Upon catalyst and substrate encapsulation, an amphiphilic dendrimer containing 27 triethylene glycol termini and 9 intradendritic triazole rings serves as a catalytic nanoreactor by considerably accelerating the Cu I-catalyzed alkyne-azide cycl
- Deraedt, Christophe,Pinaud, No?l,Astruc, Didier
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supporting information
p. 12092 - 12098
(2014/10/16)
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- Phase transfer agent assisted biphasic CuAAC reaction
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A phase transfer agent assisted biphasic Cu(i) catalyzed azide-alkyne 1,3-dipolar cycloaddition (CuAAC) reaction system was developed. A biphasic reaction medium consisting of water and an organic solvent ensures the dissolution of reagents and substrates
- Kim, Jae Hyun,Kim, Sanghee
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p. 26516 - 26523
(2014/07/08)
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- Triazole containing novobiocin and biphenyl amides as Hsp90 C-terminal inhibitors
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Hsp90 C-terminal inhibitors are advantageous for the development of new cancer chemotherapeutics due to their ability to segregate client protein degradation from induction of the prosurvival heat shock response, which is a major detriment associated with
- Zhao, Jinbo,Zhao, Huiping,Hall, Jessica A.,Brown, Douglas,Brandes, Eileen,Bazzill, Joseph,Grogan, Patrick T.,Subramanian, Chitra,Vielhauer, George,Cohen, Mark S.,Blagg, Brian S. J.
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supporting information
p. 1317 - 1323
(2014/10/15)
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- A bis(triazolecarboxamido) ligand for enantio- and regioselective molybdenum-catalyzed asymmetric allylic alkylation reactions
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A modular, enantiomerically pure bis(1H-1,2,3-triazole-4-carboxamide) has been assembled from N,N'-[(1R,2R)-cyclohexane-1,2-diyl]dipropiolamide through a copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction and evaluated as a ligand in the molybde
- Ozkal, Erhan,Pericas, Miquel A.
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supporting information
p. 711 - 717
(2014/04/03)
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- Facet-dependent catalytic activity of Cu2O nanocrystals in the one-pot synthesis of 1,2,3-triazoles by multicomponent click reactions
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We report the highly facet-dependent catalytic activity of Cu2O nanocubes, octahedra, and rhombic dodecahedra for the multicomponent direct synthesis of 1,2,3-triazoles from the reaction of alkynes, organic halides, and NaN3. The catalytic activities of clean surfactant-removed Cu 2O nanocrystals with the same total surface area were compared. Rhombic dodecahedral Cu2O nanocrystals bounded by {110} facets were much more catalytically active than Cu2O octahedra exposing {111} facets, whereas Cu2O nanocubes displayed the slowest catalytic activity. The superior catalytic activity of Cu2O rhombic dodecahedra is attributed to the fully exposed surface Cu atoms on the {110} facet. A large series of 1,4-disubstituted 1,2,3-triazoles have been synthesized in excellent yields with high regioselectivity under green conditions by using these rhombic dodecahedral Cu2O catalysts, including the synthesis of rufinamide, an antiepileptic drug, demonstrating the potential of these nanocrystals as promising heterogeneous catalysts for other important coupling reactions.
- Chanda, Kaushik,Rej, Sourav,Huang, Michael H.
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p. 16036 - 16043
(2014/04/03)
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- 1,2,3-Triazoles as versatile directing group for selective sp2 and sp3 C-H activation: Cyclization vs substitution
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Selective cyclization and substitution was achieved with designated 1,2,3-triazole acid auxiliary groups under Pd catalyzed C-H activation conditions. Both sp2 and sp3 C-H bonds were effectively activated, giving the desired products
- Ye, Xiaohan,He, Zhengrong,Ahmed, Tonia,Weise, Keith,Akhmedov, Novruz G.,Petersen, Jeffrey L.,Shi, Xiaodong
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p. 3712 - 3716
(2013/11/19)
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- An abnormal N-heterocyclic carbene-copper(I) complex in click chemistry
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Herein we report the synthesis of a copper(I) chloro complex using an abnormal N-heterocyclic carbene (aNHC) salt, 1,3-bis(2,6-diisopropylphenyl)-2,4- diphenylimidazolium. The Cu(aNHC) complex efficiently catalyzed Huisgen 1,3-dipolar cycloaddition reacti
- Sau, Samaresh Chandra,Roy, Sudipta Raha,Sen, Tamal K.,Mullangi, Dinesh,Mandal, Swadhin K.
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p. 2982 - 2991
(2014/03/21)
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- Cycloaddition reactions of propiolamidinium salts
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Thermal and microwave-assisted [3+2] cycloadditions between differently substituted propiolamidinium tetraphenylborates 3a-d and N-methyl-C- phenylnitrone, benzyl azide, and N-(3-azidopropyl)phthalimide were studied. The activation parameters of the [3+2]
- Weingaertner, Werner,Maas, Gerhard
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p. 6372 - 6382
(2013/01/15)
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- Unusual Cu(I)-catalyzed 1,3-dipolar cycloaddition of acetylenic amides: Formation of bistriazoles
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C-carbamoyl-1,2,3-triazoles have recently attracted much interest due to their potent biological activity. While synthesizing C-carbamoyl-1,2,3-triazoles by the copper(I)-catalyzed 1,3-dipolar cycloaddition of organic azides 1 and acetylenic amides 2, we
- Kwon, Mihyun,Jang, Yujin,Yoon, Sunyoung,Yang, Dongsik,Jeon, Heung Bae
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experimental part
p. 1606 - 1609
(2012/04/17)
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- Copper(I) oxide and benzoic acid 'on water': A highly practical and efficient catalytic system for copper(I)-catalyzed azide-alkyne cycloaddition
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A simple combination of Cu2O and PhCO2H 'on H 2O' has been developed as a highly practical and efficient catalytic system for copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC). It not only provides a further evidence
- Shao, Changwei,Zhu, Rui,Luo, Sheng,Zhang, Qun,Wang, Xinyan,Hu, Yuefei
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supporting information; experimental part
p. 3782 - 3785
(2011/08/06)
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- INDOLE AMIDE DERIVATIVES AND RELATED COMPOUNDS FOR USE IN THE TREATMENT OF NEURODEGENERATIVE DISEASES
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This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.
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- Boronic acid catalysis for mild and selective [3+2] dipolar cycloadditions to unsaturated carboxylic acids
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Herein, the concept of boronic acid catalysis (BAC) for the activation of unsaturated carboxylic acids is applied in several classic dipolar [3 + 2] cycloadditions involving azides, nitrile oxides, and nitrones as partners. These cycloadditions can be used to produce pharmaceutically interesting, small heterocyclic products, such as triazoles, isoxazoles, and isoxazolidines. These cycloadducts are formed directly and include a free carboxylic acid functionality that can be employed for fur-ther transformations, thereby avoiding prior masking or functionalization. In all cases, BAC provides faster reactions, under milder conditions, with much improved product yields and regioselectivities. In some instances, such as triazole formation from the reaction of azides with 2-alkynoic acids, catalysis with ort/io- nitrophenylboronic acid circumvents the undesirable product decarboxylation observed when using thermal activation. By using NMR spectroscopic studies, the boronic acid catalyst was shown to provide activation by a LUMO-lowering effect in the unsaturated carboxylic acid, likely via a monoacylated hemiboronic ester intermediate.
- Zheng, Hongchao,McDonald, Robert,Hall, Dennis G.
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supporting information; experimental part
p. 5454 - 5460
(2010/09/15)
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- A convenient and efficient synthesis of C-carbamoyl-1,2,3-triazoles from alkyl bromide by a one-pot sequential addition: Conversion of ester to amide using Zr(Ot-Bu)4
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A convenient and efficient one-pot sequence has been developed for the synthesis of C-carbamoyl-1,2,3-triazoles from alkyl bromide using (i) sodium azide, (ii) methyl propiolate and copper iodide, and (iii) amines, zirconium tert-butoxide, and 1-hydroxybe
- Yang, Dongsik,Kwon, Mihyun,Jang, Yujin,Jeon, Heung Bae
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experimental part
p. 3691 - 3695
(2010/08/20)
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- On the reactivity of activated alkynes in copper and solvent-free Huisgens reaction
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Terminal alkynes substituted by a carbonyl-type electron-withdrawing group have been found to undergo Huisgens cycloaddition with azides at room temperature in a solvent-free manner; without a need of either heating or catalysis. Metallic salts, other tha
- Elamari, Hichem,Jlalia, Ibtissem,Louet, Charlotte,Herscovici, Jean,Meganem, Faouzi,Girard, Christian
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scheme or table
p. 1179 - 1183
(2010/11/02)
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- Novel imidazole derivatives
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The invention is concerned with novel imidazole derivatives of formula (I), wherein m, E, R1, R2, R3, R4, R5, R6 and R7 are as defined in the description and in the claims, as we
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Page/Page column 17
(2009/01/23)
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- Improved copper(I)-NHC catalytic efficiency on huisgen reaction by addition of aromatic nitrogen donors
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A study was conducted to demonstrate copper(I)-NHC catalytic efficiency improvement on Huisgen reaction by adding aromatic nitrogen donors. Several unsaturated nitrogen heterocycles such as l-histidine, a ubiquitous amino acid residue associated to all ty
- Teyssot, Marie-Laure,Chevry, Aurelien,Traikia, Mounir,El-Ghozzi, Malika,Avignant, Daniel,Gautier, Arnaud
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supporting information; experimental part
p. 6322 - 6326
(2010/03/03)
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- Phosphoramidite accelerated copper(i)-catalyzed [3 + 2] cycloadditions of azides and alkynes
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Monodentate phosphoramidite ligands are used to accelerate the copper(i)-catalyzed 1,3-dipolar cycloaddition of azides and alkynes (CuAAC) rapidly yielding a wide variety of functionalized 1,4-disubstituted-1,2,3- triazoles; Cu(i) and Cu(ii) salts both function as the copper source in aqueous solution to provide excellent yields.
- Campbell-Verduyn, Lachlan S.,Mirfeizi, Leila,Dierckx, Rudi A.,Elsinga, Philip H.,Feringa, Ben L.
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supporting information; experimental part
p. 2139 - 2141
(2009/09/05)
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- Synthesis and antibiotic activity of a small molecules library of 1,2,3-triazole derivatives
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A small library of simple 1,4-disubstituted 1,2,3-triazoles was prepared using a known one-pot procedure starting from organic halides and terminal alkynes. The compounds were then tested for their antibacterial activity against normal and resistant speci
- Aufort, Marie,Herscovici, Jean,Bouhours, Pascale,Moreau, Nicole,Girard, Christian
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p. 1195 - 1198
(2008/12/21)
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- Click chelators for platinum-based anticancer drugs
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Triazoles from "click chemistry" are convenient ligands for the formation of platinum complexes bearing combined triazole-amine or triazole-carboxylate moieties. Striking differences in the chelation modes are observed between the two series. One of the triazole-amine platinum complexes exhibits selective cytotoxicity against breast cancer cells lines. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
- Maisonial, Aurelie,Serafin, Patrycja,Traikia, Mounir,Debiton, Eric,Thery, Vincent,Aitken, David J.,Lemoine, Pascale,Viossat, Bernard,Gautier, Arnaud
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p. 298 - 305
(2008/09/17)
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- Cu(I)-catalyzed intramolecular cyclization of alkynoic acids in aqueous media: A "click side reaction"
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(Chemical Equation Presented) Alkynoic acids, in particular, 4-pentynoic acid derivatives, undergo intramolecular cyclizations to enol lactones under reaction conditions typically applied for the Cu(I)-catalyzed cycloaddition of terminal alkynes and azide
- Mindt, Thomas L.,Schibli, Roger
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p. 10247 - 10250
(2008/03/28)
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- Substituted N-aryl heterocycles, process for their preparation and their use as medicaments
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The invention relates to substituted N-aryl heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I in which the radicals have the stated meanings, the N-oxides and the physiologically tolerated salts thereof and process for the preparation thereof are described. The compounds are suitable for example as anorectic agents.
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- SUBSTITUTED N-ARYLHETEROCYCLES, METHOD FOR PRODUCTION AND USE THEREOF AS MEDICAMENTS
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The invention relates to N-arylheterocycles and the physiologically-acceptable salts and physiologically-functional derivatives thereof. Compounds of formula (I), where the groups have the given meanings, the N-oxides and the physiologically-acceptable salts and methods for production thereof are disclosed. The compounds are suitable as anorectics for example.
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Page/Page column 344
(2010/02/08)
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- 1-,2-,and 3-N,N-dialkylcarbamyl-1-H-1,2,3-triazoles
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A compound having the structural formula STR1 wherein X is hydrogen or bromine; Y is bromine, phenyl, C1 -C4 alkyl or C4 -C6 cycloalkyl; R1 and R2 independently are C1 -C6 alkyl or R1 and R2 together form a ring with the nitrogen to which they are attached having 3-8 carbon atoms, optionally substituted with one or two methyl groups.
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- UNSATURATED CARBONYL-CONTAINING COMPOUNDS. XXVIII. CYCLOADDITION OF ORGANIC AZIDES TO α-ACETYLENIC KETONES AND ACIDS
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The reaction of α-acetylenic ketones and acids with organic azides leads to the formation of 1-alkyl(aryl)-4-acyl(carboxy)-1,2,3-triazoles or to a mixture of the 1,4- and 1,5-disubstituted isomers.The effect of the structure of the initial compound and of the solvent on the direction of cycloaddition was investigated.
- Vereshchagin, L. I.,Tikhonova, L. G.,Maksikova, A. V.,Serebryakova, E. S.,Proidakov, A. G.,Filippova, T. M.
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p. 641 - 648
(2007/10/02)
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