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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-((2 S,3 S)-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 = 16.3 nM, CB2/CB1 = 181.6).
Published Version
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