Inhibition of protein glycation by urea and thiourea derivatives of glycine/proline conjugated benzisoxazole analogue - Synthesis and structure-activity studies

被引：56

作者：

Shantharam, C. S. ^{[1
]}

Vardhan, D. M. Suyoga ^{[1
]}

Suhas, R. ^{[1
]}

Sridhara, M. B. ^{[1
]}

Gowda, D. Channe ^{[1
]}

机构：

[1] Univ Mysore, Dept Studies Chem, Mysore 570006, Karnataka, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 60卷

关键词：

Amino acids; Conjugation; Urea/thiourea; Antiglycation; BIOLOGICAL EVALUATION; LYSINE; BENZOTHIAZOLE; BENZOXAZOLE; GLUCOSE; DESIGN;

D O I：

10.1016/j.ejmech.2012.12.029

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Synthesis of a new series of urea/thiourea derivatives of Gly/Pro conjugated benzisoxazole has been reported. Structure of the compounds was characterized by physical and spectroscopical data and has been screened for their in vitro antiglycation activity. Several compounds showed promising activity with IC50 <5 mu M compared to standard rutin (IC50 = 41.9 mu M). Further, it was found that compounds containing methoxy and bromine substituents have exerted highly potent activity. Thus, the title compounds represent novel class of potent antiglycating agents. (C) 2012 Elsevier Masson SAS. All rights reserved.

引用

页码：325 / 332

页数：8

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