2. Academic Validation
  3. 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

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

Affiliation

  • 1 Research Center, Green Cross Corporation, 303 Bojeong-dong, Giheung-gu, Yongin 446-770, Republic of Korea. jinhwa_2_lee@hotmail.com
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.

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