氮杂前列腺素类似物。11-氮杂前列腺素衍生物的合成及生物学性质。

Azaprostaglandin analogues. Synthesis and biological properties of 11-azaprostaglandin derivatives.

作者信息

Barco A, Benetti S, Pollini G P, Baraldi P G, Guarneri M, Gandolfi C, Ceserani R, Longiave D

出版信息

J Med Chem. 1981 May;24(5):625-8. doi: 10.1021/jm00137a027.

Abstract

New nitrogen analogues of prostaglandins (11, 11a, 12, and 12a) have been synthesized starting from a 4,5-disubstituted 2-pyrrolidinone nucleus (5 and 5a) containing one side chain and a suitable functionality for elaborating the second one. These analogues had no better activity than natural prostaglandins in vitro [guinea pig ileum and trachea, rat stomach fundus strip, uterus and portal vein, ADP-induced guinea pig platelet-rich plasma (PRP) aggregation]. They similarly lacked any interesting activity in vivo [anesthetized rat blood pressure, stress, and acetylsalycilic acid (ASA) induced gastric lesions in rat].

摘要

已经从含有一个侧链和用于构建第二个侧链的合适官能团的4,5-二取代2-吡咯烷酮核（5和5a）开始合成了前列腺素的新型氮类似物（11、11a、12和12a）。这些类似物在体外[豚鼠回肠和气管、大鼠胃底条、子宫和门静脉、ADP诱导的豚鼠富血小板血浆（PRP）聚集]中没有比天然前列腺素更好的活性。它们在体内[麻醉大鼠血压、应激以及乙酰水杨酸（ASA）诱导的大鼠胃损伤]中同样缺乏任何有趣的活性。