Discovery of 2-(4-((1H-1,2,4-triazol-1-yl)methyl)-5-(4-bromophenyl)-1-(2-chlorophenyl)-1H-pyrazol-3-yl)-5-tert-butyl-1,3,4-thiadiazole (GCC2680) as a potent, selective and orally efficacious cannabinoid-1 receptor antagonist

  • Bioorg Med Chem. 2010 Sep 1;18(17):6377-88. doi: 10.1016/j.bmc.2010.07.013.
Jinhwa Lee  1 ,  Hee Jeong Seo ,  Suk Ho Lee ,  Jeongmin Kim ,  Myung Eun Jung ,  Sung-Han Lee ,  Kwang-Seop Song ,  Junwon Lee ,  Suk Youn Kang ,  Min Ju Kim ,  Mi-Soon Kim ,  Eun-Jung Son ,  Minwoo Lee ,  Ho-Kyun Han
Affiliations
  • 1. Research Center, Green Cross Corporation, 303 Bojeong-dong, Giheung-gu, Yongin 446-770, Republic of Korea. [email protected]
PMID: 20673729 DOI: 10.1016/j.bmc.2010.07.013
Abstract

Structure-activity relationship studies in a series of diarylpyrazolyl thiadiazoles identified cannabinoid-1 receptor antagonists with excellent potency and selectivity. Based on its exceptional in vivo efficacy in animal models and its favorable pharmacokinetic and toxicological profiles, 2-(4-((1H-1,2,4-triazol-1-yl)methyl)-5-(4-bromophenyl)-1-(2-chlorophenyl)-1H-pyrazol-3-yl)-5-tert-butyl-1,3,4-thiadiazole (GCC2680) was selected as a preclinical candidate for the treatment of obesity.