Novel derivatives of ISO-1 as potent inhibitors of MIF biological function

被引：27

作者：

Balachandran, Sarala ^{[1
]}

Rodge, Atish ^{[1
]}

Gadekar, Pradip K. ^{[1
]}

Yadav, Vitthal N. ^{[1
]}

Kamath, Divya ^{[2
]}

Chetrapal-Kunwar, Anshu ^{[2
]}

Bhatt, Pooja ^{[2
]}

Srinivasan, Shaila ^{[2
]}

Sharma, Somesh ^{[1
,2
]}

Vishwakarma, Ram A. ^{[1
]}

Dagia, Nilesh M. ^{[2
]}

机构：

[1] Piramal Life Sci, Dept Med Chem, Bombay 400063, Maharashtra, India

[2] Piramal Life Sci, Dept Pharmacol, Bombay 400063, Maharashtra, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 16期

关键词：

Oxadiazole; Phthalimide; Amide; MIF; ISO-1; Anti-inflammatory; TAUTOMERASE;

D O I：

10.1016/j.bmcl.2009.06.052

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

A series of novel 1,2,4-oxadiazole, phthalimide, amide and other derivatives of ISO-1 were synthesized and probed for inhibition of macrophage migration inhibitory factor (MIF) activity. Several compounds inhibited MIF enzymatic activity at levels better than ISO-1. Of note, compounds 7, 22, 23, 24, 25 and 27 inhibited the spontaneous secretion/release/recognition of MIF from freshly isolated human peripheral blood mononuclear cells and, more importantly, inhibited the MIF-induced production of interleukin-6 (IL-6) and/or interleukin-1b (IL-1b) significantly better than ISO-1. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：4773 / 4776

页数：4

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