title: Substituted pyrimidines as cannabinoid CB1 receptor ligands.
abstract: Cannabinoid CB1 receptors have been the avenue of extensive studies since the first clinical results of rimonabant (SR141716) for the treatment of obesity and obesity-related metabolic disorders were reported in 2001. To further evaluate the properties of CB receptors, we have designed and efficiently prepared a series of substituted pyrimidines based on chemical structure of Merck's taranabant, a cannabinoid CB1 receptor inverse agonist. Noticeably, N4-((2S,3S)-3-(3-bromophenyl)-4-(4-chlorophenyl)butan-2-yl)-N6-butylpyrimidine-4,6-diamine (13b) demonstrated good binding affinity and decent selectivity for CB1 receptor (IC(50)=16.3nM, CB2/CB1=181.6).
authors: Central Research Laboratories, Green Cross Corporation, Yongin, Gyeonggi-Do 446-770, Republic of Korea.
authors: Min Ju
authors: MJ
authors: Kim
authors: Jong Yup
authors: JY
authors: Kim
authors: Hee Jeong
authors: HJ
authors: Seo
authors: Junwon
authors: J
authors: Lee
authors: Sung-Han
authors: SH
authors: Lee
authors: Mi-Soon
authors: MS
authors: Kim
authors: Jahyo
authors: J
authors: Kang
authors: Jeongmin
authors: J
authors: Kim
authors: Jinhwa
authors: J
authors: Lee
mesh_terms: D000818:Animals; D019440:Anti-Obesity Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D008024:Ligands; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D043884:Receptor, Cannabinoid, CB1 / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D019440:Anti-Obesity Agents; D008024:Ligands; D011743:Pyrimidines; D043884:Receptor, Cannabinoid, CB1