Structure-activity relationship study of novel NR2B-selective antagonists with arylamides to avoid reactive metabolites formation.

Makoto Kawai,Isao Sakurada,Asato Morita,Yuko Iwamuro,Kazuo Ando,Hirofumi Omura,Sachiko Sakakibara,Tsutomu Masuda,Hiroki Koike,Teruki Honma,Kazunari Hattori,Tadayuki Takashima,Kunihiko Mizuno,Mayumi Mizutani,Mitsuhiro Kawamura

Bioorganic & Medicinal Chemistry Letters（2007）

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摘要

Replacement of the phenol moiety with pyrazole led to a novel potent NMDA-NR2B selective antagonist (5b) with an improved metabolic profile. Through this study, a close correlation between reactive metabolites formation and calculated HOMO energies of parent compounds was found.

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关键词

Reactive metabolite,Bioactivation,NR2B,NMDA,Metabolic stability

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