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Bioisosteric replacement of the pyrazole 5-aryl moiety of N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A). A novel series of alkynylthiophenes as potent and selective cannabinoid-1 receptor antagonists.
Tseng SL, Hung MS, Chang CP, Song JS, Tai CL, Chiu HH, Hsieh WP, Lin Y, Chung WL, Kuo CW, Wu CH, Chu CM, Tung YS, Chao YS, Shia KS. Tseng SL, et al. Among authors: shia ks. J Med Chem. 2008 Sep 11;51(17):5397-412. doi: 10.1021/jm800066v. Epub 2008 Aug 20. J Med Chem. 2008. PMID: 18712856
Discovery of 2-[5-(4-chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-1H-pyrazol-3-yl]-1,5,5-trimethyl-1,5-dihydro-imidazol-4-thione (BPR-890) via an active metabolite. A novel, potent and selective cannabinoid-1 receptor inverse agonist with high antiobesity efficacy in DIO mice.
Wu CH, Hung MS, Song JS, Yeh TK, Chou MC, Chu CM, Jan JJ, Hsieh MT, Tseng SL, Chang CP, Hsieh WP, Lin Y, Yeh YN, Chung WL, Kuo CW, Lin CY, Shy HS, Chao YS, Shia KS. Wu CH, et al. Among authors: shia ks. J Med Chem. 2009 Jul 23;52(14):4496-510. doi: 10.1021/jm900471u. J Med Chem. 2009. PMID: 19530697
Discovery of 1-(2,4-dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide as a potential peripheral cannabinoid-1 receptor inverse agonist.
Hung MS, Chang CP, Li TC, Yeh TK, Song JS, Lin Y, Wu CH, Kuo PC, Amancha PK, Wong YC, Hsiao WC, Chao YS, Shia KS. Hung MS, et al. Among authors: shia ks. ChemMedChem. 2010 Sep 3;5(9):1439-43. doi: 10.1002/cmdc.201000246. ChemMedChem. 2010. PMID: 20652930 No abstract available.
67 results