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The design, synthesis and in vitro immunosuppressive evaluation of novel isobenzofuran derivatives.

Abstract：

:The synthesis and biological evaluation of a series of novel isobenzofuran-based compounds are described. The compounds were evaluated for their immunosuppressive effects of T-cell proliferation and IMPDH type II inhibitor activity in vitro, as well as their structure-activity relationships were assessed. Several compounds demonstrated highly efficacious immunosuppressive properties, especially compounds 2d, 2e, 2h and 2j, which were superior to MPA, while compounds 2k, 2m, 2n, 4c and 5d exhibited an equipotent inhibitory activity compared to MPA. Generally, it was obviously demonstrated that α,β-unsaturated amides proved more potent than the diamide and urea series. The present study provides a guide for further research on development of safe and effective immunosuppressive agents.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Yang N,Wang QH,Wang WQ,Wang J,Li F,Tan SP,Cheng MS

doi

10.1016/j.bmcl.2011.11.078

subject

Has Abstract

pub_date

2012-01-01 00:00:00

pages

53-6

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)01622-2

journal_volume

22

pub_type

杂志文章

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