具有亚型选择性抗毒蕈碱活性的新型咪唑衍生物(1)。
Novel imidazole derivatives with subtype-selective antimuscarinic activity (1).
作者信息
Miyachi H, Kiyota H, Segawa M
机构信息
Central Research Laboratories, Kyorin Pharmaceutical Co., Ltd., Tochigi, Japan.
出版信息
Bioorg Med Chem Lett. 1998 Jul 21;8(14):1807-12. doi: 10.1016/s0960-894x(98)00312-6.
PMID:9873438
Abstract
A series of N-substituted 4-amino-2,2-diphenylbutyramide derivatives was prepared as part of a search for subtype-selective antimuscarinic agents. The representative compound KRP-197, bearing a 2-methylimidazole ring as a surrogate of aliphatic amine, was found to be a highly potent and both M1- and M3-selective antimuscarinic agent.
摘要
作为寻找亚型选择性抗毒蕈碱剂的一部分，制备了一系列N-取代的4-氨基-2,2-二苯基丁酰胺衍生物。代表性化合物KRP-197带有2-甲基咪唑环作为脂肪胺的替代物，被发现是一种高效且对M1和M3均具有选择性的抗毒蕈碱剂。
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