- NBS mediated protocol for the synthesis of N-bridged fused heterocycles in water
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A facile and environmental friendly protocol for the synthesis of N-bridged fused bicyclic compounds such as imidazo[1,2-a]pyridines, imidazo[1,2-a]pyrimidines, and imidazo[2,1-b]thiazole, from commercially available starting materials has been developed.
- Bhagat, Saket B.,Telvekar, Vikas N.
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supporting information
p. 3662 - 3666
(2017/08/23)
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- Design, synthesis and biological evaluation of imidazo[2,1-b]thiazole and benzo[d]imidazo[2,1-b]thiazole derivatives as Mycobacterium tuberculosis pantothenate synthetase inhibitors
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In the present study, we have designed imidazo[2,1-b]thiazole and benzo[d]imidazo[2,1-b]thiazole derivatives from earlier reported imidazo[1,2-a]pyridine based Mycobacterium tuberculosis (MTB) pantothenate synthetase (PS) inhibitors. We synthesized thirty compounds and they were evaluated for MTB PS inhibition study, in vitro anti-TB activities against replicative and non-replicative MTB, in vivo activity using Mycobacterium marinum infected Zebra fish and cytotoxicity against RAW 264.7 cell line. Among them compound 2-methyl-N′-(4-phenoxybenzoyl)benzo[d]imidazo[2,1-b]thiazole-3-carbohydrazide (5bc) emerged as potent compound active against MTB PS with IC50 of 0.53 ± 0.13 μM, MIC of 3.53 μM, 2.1 log reduction against nutrient starved MTB, with 33% cytotoxicity at 50 μM. It also showed 1.5 log reduction of M. marinum load in Zebra fish at 10 mg/kg.
- Samala, Ganesh,Devi, Parthiban Brindha,Saxena, Shalini,Meda, Nikhila,Yogeeswari, Perumal,Sriram, Dharmarajan
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p. 1298 - 1307
(2016/03/01)
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- Discovery of new chemical entities as potential leads against Mycobacterium tuberculosis
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A series of biheterocyclic (1H-indole, benzofuran, pyrazolo[1,5-a]pyrimidine, pyrazolo[1,5-a]pyrimidin-5(4H)-one, imidazo[2,1-b]thiazole and pyrazolo[5,1-b]thiazole) derivatives were synthesized and evaluated for their anti-tubercular activities. The imid
- Lu, Xiaoyun,Tang, Jian,Liu, Zhiyong,Li, Minke,Zhang, Tianyu,Zhang, Xiantao,Ding, Ke
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supporting information
p. 5916 - 5919
(2016/12/06)
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- HETEROARYLS AND THEIR USE AS PI3K INHIBITORS
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This invention provides compounds of formula (IA) or (IB): wherein R1, R2, G1 and HY are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
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Page/Page column 328
(2010/08/18)
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- FUSED IMIDAZOLE CARBOXAMIDES AS TRPV3 MODULATORS
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The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided
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Page/Page column 10
(2010/06/22)
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- FUSED IMIDAZOLE CARBOXAMIDES AS TRPV3 MODULATORS
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The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided
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Page/Page column 23
(2010/08/05)
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- Reaction of 2-Aminothiazoles with Reagents containing a C-Halogen and a C=O Electrophilic Centre
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Seven reagents of different types having in common a C-Hal and a C=O electrophilic centre have been used in a study of their reactions with 2-aminothiazoles.Three reagents, CHBrAc2 and ROCHBrCO2Et (R = Me, Ph), gave imidazothiazoles, thus providing useful routes to the 5-acetyl and 5-ethoxycarbonyl derivatives.Unexpectedly, the solvent (acetone) was involved in the reaction of the fourth reagent, CHBr(CO2Et)2, with 2-aminothiazole which led to 5,5-di(ethoxycarbonyl)-6,6-dimethyl-5,6-dihydroimidazothiazole (yield 81percent).With the last three reagents (AcCHBrNO2, BzCHBrCN and ICH2CO2C6H4NO2-p) the outcome was simpler, viz., the formation of 2-amidothiazoles.It is proposed that electrophilic attack by the endo-N of the 2-aminothiazole is the first step in all cases.This occurs at the C-Hal centre of the first four reagents and is followed by cyclisation to the exo-N.In the last three electrophiles the presence of the groups well suited to leaving as stabilised anions favours addition to the C=O group; the intermediates so formed subsequently isomerise to the more stable exo-N substituted products.
- Compton, Victoria J.,Meakins, G. Denis,Raybould, Amanda J.
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p. 2029 - 2032
(2007/10/02)
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- RESEARCH ON HETEROCYCLIC COMPOUNDS. XIV. - Imidazothiazole and imidazobenzothiazole derivatives : synthesis and antiinflammatory activity.
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A group of ethyl 6-methylimidazothiazole-5-carboxylates and 2-methylimidazobenzothiazole-3-carboxylates was prepared by reaction of ethyl 2-chloroacetoacetate with some 2-aminothiazoles and 2-aminobenzothiazoles, respectively.Such reactions may sometimes afford a side product which was isolated and characterized.The ethyl esters were then converted into the corresponding acids by hydrolysis.Three of these acids were evaluated for antiinflammatory, analgesic, and antipyretic activities, as well as for ulcerogenic potential.
- Abignente, E.,Caprariis, P. De,Sacchi, A.,Marmo, E.,Berrino, L.,Matera, M. G.
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p. 533 - 545
(2007/10/02)
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