2-取代-N-羧甲基-1,5-苯并硫氮杂䓬-4-酮和-1,4-苯并噻嗪-3-酮的合成及其作为血管紧张素转换酶抑制剂的评价。
Synthesis of 2-substituted-N-carboxymethyl-1,5-benzothiazepin-4-ones and -1,4-benzothiazin-3-ones and their evaluation as angiotensin converting enzyme inhibitors.
作者信息
Trapani G, Latrofa A, Franco M, Liso G
机构信息
Dipartimento Farmacochimico, Università di Bari.
出版信息
Farmaco. 1995 Feb;50(2):107-12.
PMID:7766274
Abstract
The title compounds 7a-d and 8a-e were synthesized and their in vitro inhibitory activity of angiotensin-converting enzyme (ACE) was examined. In general, these compounds possess poor ACE inhibitory activity. Among the benzothiazinone compounds, which are generally more active than the cyclohomologous compounds 7, 8b is the most effective (IC50 of 170 microM).
摘要
合成了标题化合物7a - d和8a - e，并检测了它们对血管紧张素转换酶（ACE）的体外抑制活性。一般来说，这些化合物的ACE抑制活性较差。在通常比环同系物7更具活性的苯并噻嗪酮化合物中，8b是最有效的（IC50为170微摩尔）。
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