Smith J R, Wahhab A, Moore D, Ganter R C, Moore G J
Department of Pharmacology and Therapeutics, Faculty of Medicine, University of Calgary, Alberta, Canada.
Drug Des Discov. 1994 Nov;12(2):113-9.
A series of analogues related to Losartan in which the imidazole ring substituents were transposed have been prepared. Biological evaluation, both in vitro and in vivo, demonstrated that the orientation of the imidazole ring has a subtle yet significant effect upon the potency of these analogues. This information has provided an insight into the possible mode of receptor binding of Losartan and related compounds.
已制备了一系列与氯沙坦相关的类似物,其中咪唑环取代基进行了互换。体外和体内的生物学评估表明,咪唑环的取向对这些类似物的效力有微妙但显著的影响。这一信息为深入了解氯沙坦及相关化合物的受体结合可能模式提供了线索。