The TosMIC approach to 3-(oxazol-5-yl) indoles: application to the synthesis of indole-based IMPDH inhibitors.

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Dhar TG, Shen Z, Fleener CA, Rouleau KA, Barrish JC, Hollenbaugh DL, Iwanowicz EJ

The TosMIC approach to 3-(oxazol-5-yl) indoles: application to the synthesis of indole-based IMPDH inhibitors.

Bioorg Med Chem Lett. 2002 Nov 18;12(22):3305-8.

PubMed ID

12392738 [ View in PubMed

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Abstract

A modified approach to the synthesis of 3-(oxazolyl-5-yl) indoles is reported. This method was applied to the synthesis of series of novel indole based inhibitors of inosine monophosphate dehydrogenase (IMPDH). The synthesis and the structure-activity relationships (SARs), derived from in vitro studies, for this new series of inhibitors is given.

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Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Mycophenolic acid	Inosine-5'-monophosphate dehydrogenase 2	IC 50 (nM)	15	N/A	N/A	Details