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新型诱导血小板聚集的手性抑制剂:1-(4-[(1-羟基羰基)-乙氧基]-苄基)-1H-1,2,3-三唑的(R)-和(S)-甲酯及乙酯的对映体特异性作为确定其生物靶点的工具

New chiral inhibitors of induced platelet aggregation: the enantiomeric specificity of (R)- and (S)-methyl and ethyl esters of 1-(4-[(1-hydroxycarbonyl)-ethoxy]-benzyl)-1H-1,2,3-triazole as a tool for determining their biological target.

作者信息

Biagi G, Giorgi I, Livi O, Scartoni V, Catalani R, Gervasi G

机构信息

Laboratori BALDACCI spa, Pisa.

出版信息

Farmaco. 1996 Dec;51(12):761-6.

PMID:9050207
Abstract

The synthesis of title enantiomers was accomplished and their biological behaviour as inhibitors of rabbit platelet aggregation process induced by ADP and arachidonic acid was determined. Structure-activity comparison with that of SM-12502 [(2R,5S)-(+) 3,5-dimethyl-2-(3-pyridyl)-thiazolidin-4-one hydrochloride] and Dazoxiben [4-[2-(1H-imidazol-1-yl)-ethoxy]-benzoic acid] allowed us to formulate the possible capability for the synthesized compounds to interact with the biological targets of the model molecules.

摘要

完成了标题对映体的合成,并测定了它们作为ADP和花生四烯酸诱导的兔血小板聚集过程抑制剂的生物学行为。通过与SM-12502 [(2R,5S)-(+)3,5-二甲基-2-(3-吡啶基)-噻唑烷-4-酮盐酸盐]和达唑氧苯[4-[2-(1H-咪唑-1-基)-乙氧基]-苯甲酸]进行构效关系比较,使我们能够推测合成化合物与模型分子的生物靶点相互作用的可能能力。

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