Synthesis and .alpha.-adrenergic activities of 2- and 4-substituted imidazoline and imidazole analogs
作者:Yoshiya Amemiya、Seoung S. Hong、Burrah V. Venkataraman、Popat N. Patil、Gamal Shams、Karl Romstedt、Dennis R. Feller、Fu Lian Hsu、Duane D. Miller
DOI:10.1021/jm00082a017
日期:1992.2
Seven analogues of medetomidine and naphazoline were synthesized and evaluated for their alpha 1 (aorta) and alpha 2 (platelet) activities. The analogues were composed of 2- and 4-substituted imidazoles and imidazolines attached through a methylene bridge to either the 1- or 2-naphthalene ring system. In general the 1-naphthalene analogues were the most potent inhibitors of epinephrine-induced platelet
合成了美托咪定和萘甲唑啉的七个类似物,并评估了它们的alpha 1(主动脉)和alpha 2(血小板)活性。该类似物由2-和4-取代的咪唑和咪唑啉通过亚甲基桥连接至1-或2-萘环系统组成。通常,1-萘类似物是肾上腺素诱导的血小板聚集的最有效抑制剂。在1-α肾上腺素系统(主动脉)中1-萘类似物(2、5-7)是部分激动剂,而2-萘类似物(3、8、9)是拮抗剂,这一事实引起了人们极大的兴趣。因此,适当地取代的美托咪定和萘并萘的萘类似物提供了α1-激动剂,α1-拮抗剂和α2-拮抗剂活性的光谱。