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Synthesis of 2,3‐Disubstituted 1,4‐Naphthoquinones as Antiplatelet Agents
Author(s) -
Lien JinCherng,
Wu ChiRei,
Hour MannJen,
Huang LiJiau,
Huang TurFu,
Kuo ShengChu
Publication year - 2008
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200800024
Subject(s) - chemistry , mechanism of action , naphthoquinone , stereochemistry , pharmacology , platelet aggregation , structure–activity relationship , biological activity , phospholipase a2 , 1,4 naphthoquinone , platelet , phospholipase , combinatorial chemistry , biochemistry , in vitro , enzyme , medicinal chemistry , organic chemistry , medicine
In continuing search for novel antiplatelet agents, the highly potent agent 2‐chloro‐3‐methoxycarbonylethylcarboxamido‐1,4‐naphthoquinone 2 was selected as lead compound. Structure‐activity relationships in this series were examined. Some of these compounds showed significant antiplatelet activities. Further studies on the action mechanism showed that 2‐acetamido‐3‐chloro‐1,4‐naphthoquinone 4 has a direct inhibitory action on cytosolic phospholipase A 2 (cPLA 2 ) activity in platelets.