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

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

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

Bioorg Med Chem Lett. 2012 Jan 1;22(1):53-6. doi: 10.1016/j.bmcl.2011.11.078. Epub 2011 Nov 28.

PubMed ID
22172700 [ View in PubMed
]
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 alpha,beta-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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
Mycophenolic acidInosine-5'-monophosphate dehydrogenase 2IC 50 (nM)1500N/AN/ADetails