Article ID Journal Published Year Pages File Type
1378573 Bioorganic & Medicinal Chemistry Letters 2005 5 Pages PDF
Abstract

A series of thiazole-4-carboxylic acid thiazol-2-ylamide (TCAT, 4) derivatives were designed and synthesized according to simple bioisosteric replacement from previously reported pyridine-2-carboxylic acid thiazol-2-ylamide (PCAT) MetAP inhibitors. The preliminary SAR studies demonstrated that these TCAT series of compounds showed different activity and selectivity compared with those of the corresponding PCAT compounds. These findings provide useful information for the design and discovery of more potent inhibitors of type I MetAPs.

Graphical abstractA new series of potent type I MetAP inhibitors were obtained by simple bioisosteric replacement of previously reported pyridine-2-carboxylic acid thiazol-2-ylamide (PCAT) MetAP inhibitors.Figure optionsDownload full-size imageDownload as PowerPoint slide

Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
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