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11,12-断前列腺素。5. 8-乙酰基-或8-(1-羟乙基)-12-羟基-13-芳氧基十三烷酸及磺酰胺电子等排体作为血小板聚集抑制剂

11,12-Secoprostaglandins. 5. 8-Acetyl- or 8-(1-hydroxyethyl)-12-hydroxy-13-aryloxytridecanoic acids and sulfonamide isosteres as inhibitors of platelet aggregation.

作者信息

Bicking J B, Jones J H, Holtz W J, Robb C H, Kuehl F A, Minsker D H, Cragoe E J

出版信息

J Med Chem. 1978 Oct;21(10):1011-8. doi: 10.1021/jm00208a003.

Abstract

The synthesis of a series of 8-acetyl- (or 1-hydroxyethyl-) 12-hydroxy-13-aryloxytridecanoic acids and their sulfonamide isosteres is described. These compounds are formally derived from members of earlier reported series of modified secoprostaglandins by replacing the omega-butyl chain termini by substituted aryloxy groups. A number of these compounds are potent inhibitors of collagen-induced blood platelet aggregation in guinea pigs on oral administration.

摘要

描述了一系列8-乙酰基-(或1-羟乙基-)12-羟基-13-芳氧基十三烷酸及其磺酰胺等排体的合成。这些化合物正式衍生自早期报道的一系列修饰的类前列腺素类似物,通过用取代的芳氧基取代ω-丁基链末端。其中许多化合物在豚鼠口服给药时是胶原诱导的血小板聚集的有效抑制剂。

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