氧杂蒽酮与芴酮-1,4-二氢吡啶-5-膦酸酯的构效关系研究
Structure-activity relationship studies of xanthone and fluorenone-1,4-dihydropyridine-5-phosphonates.
作者信息
Budriesi R, Rampa A, Bisi A, Fabbri G, Chiarini A, Valenti P
机构信息
Department of Pharmaceutical Sciences, University of Bologna, Italy.
出版信息
Arzneimittelforschung. 1996 Apr;46(4):374-7.
PMID:8740081
Abstract
A series of xanthone and fluorenone-1,4-dihydropyridine derivatives bearing a 5-phosphonate group were prepared. The compounds were evaluated for inotropic, chronotropic and calcium antagonistic properties. The insertion of a phosphonate group is detrimental for inotropic and calcium antagonistic activity but improves the potency and selectivity for chronotropism.
摘要
制备了一系列带有5-膦酸酯基团的呫吨酮和芴酮-1,4-二氢吡啶衍生物。对这些化合物的变力性、变时性和钙拮抗特性进行了评估。膦酸酯基团的引入对变力性和钙拮抗活性不利，但提高了变时性的效力和选择性。
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