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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: chang cp. 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 1-(2,4-dichlorophenyl)-N-(piperidin-1-yl)-4-((pyrrolidine-1-sulfonamido)methyl)-5-(5-((4-(trifluoromethyl)phenyl)ethynyl)thiophene-2-yl)-1H-pyrazole-3-carboxamide as a novel peripherally restricted cannabinoid-1 receptor antagonist with significant weight-loss efficacy in diet-induced obese mice.
Chang CP, Wu CH, Song JS, Chou MC, Wong YC, Lin Y, Yeh TK, Sadani AA, Ou MH, Chen KH, Chen PH, Kuo PC, Tseng CT, Chang KH, Tseng SL, Chao YS, Hung MS, Shia KS. Chang CP, et al. Among authors: chang kh. J Med Chem. 2013 Dec 27;56(24):9920-33. doi: 10.1021/jm401158e. Epub 2013 Dec 4. J Med Chem. 2013. PMID: 24224693
Function-oriented development of CXCR4 antagonists as selective human immunodeficiency virus (HIV)-1 entry inhibitors.
Wu CH, Wang CJ, Chang CP, Cheng YC, Song JS, Jan JJ, Chou MC, Ke YY, Ma J, Wong YC, Hsieh TC, Tien YC, Gullen EA, Lo CF, Cheng CY, Liu YW, Sadani AA, Tsai CH, Hsieh HP, Tsou LK, Shia KS. Wu CH, et al. Among authors: chang cp. J Med Chem. 2015 Feb 12;58(3):1452-65. doi: 10.1021/jm501772w. Epub 2015 Jan 28. J Med Chem. 2015. PMID: 25584630 Free PMC article.
Discovery and Synthesis of a Pyrimidine-Based Aurora Kinase Inhibitor to Reduce Levels of MYC Oncoproteins.
Chi YH, Yeh TK, Ke YY, Lin WH, Tsai CH, Wang WP, Chen YT, Su YC, Wang PC, Chen YF, Wu ZW, Yeh JY, Hung MC, Wu MH, Wang JY, Chen CP, Song JS, Shih C, Chen CT, Chang CP. Chi YH, et al. Among authors: chang cp. J Med Chem. 2021 Jun 10;64(11):7312-7330. doi: 10.1021/acs.jmedchem.0c01806. Epub 2021 May 19. J Med Chem. 2021. PMID: 34009981 Free PMC article.
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: chang cp. J Med Chem. 2009 Jul 23;52(14):4496-510. doi: 10.1021/jm900471u. J Med Chem. 2009. PMID: 19530697
Bromomethylthioindole Inspired Carbazole Hybrids as Promising Class of Anti-MRSA Agents.
Cheng CY, Chang CP, Lauderdale TY, Yu GY, Lee JC, Jhang YW, Wu CH, Ke YY, Sadani AA, Yeh CF, Huang IW, Kuo YP, Tsai DJ, Yeh TK, Tseng CT, Song JS, Liu YW, Tsou LK, Shia KS. Cheng CY, et al. Among authors: chang cp. ACS Med Chem Lett. 2016 Oct 21;7(12):1191-1196. doi: 10.1021/acsmedchemlett.6b00289. eCollection 2016 Dec 8. ACS Med Chem Lett. 2016. PMID: 27994762 Free PMC article.
717 results