Discovery and structure–activity relationships of 4-aminoquinazoline derivatives, a novel class of opioid receptor like-1 (ORL1) antagonists

…, T Niwa, S Nakagawa, Y Nakamura, A Matsuura

文献索引：Okano, Masahiko; Mito, Jun; Maruyama, Yasufumi; Masuda, Hirofumi; Niwa, Tomoko; Nakagawa, Shin-ichiro; Nakamura, Yoshitaka; Matsuura, Akira Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 1 p. 119 - 132

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被引用次数: 34

摘要

Synthesis and structure–activity relationship studies of a series of 4-aminoquinazoline derivatives led to the identification of (1R, 2S)-17, N-[(1R, 2S)-2-({2-[(4-chlorophenyl) carbonyl] amino-6-methylquinazolin-4-yl} amino) cyclohexyl] guanidine dihydrochloride, as a highly potent ORL1 antagonist with up to 3000-fold selectivity over the μ, δ, and κ opioid receptors. Molecular modeling clarified the structural factors contributing to the high affinity ...