Open Medicinal Chemistry Journal 2009-01-01

Design and Synthesis of Imidazopyrimidine Derivatives as Potent iNOS Dimerization Inhibitors.

Guo-Hua Chu, Bertrand Le Bourdonnec, Minghua Gu, Christopher W Ajello, Lara K Leister, Ian Sellitto, Joel A Cassel, Paul A Tuthill, Heather O' Hare, Robert N Dehaven, Roland E Dolle

Index: Open Med. Chem. J. 3 , 8-13, (2009)

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Abstract

A series of imidazopyrimidine derivatives with the general formula I was synthesized and identified as potent inhibitors of iNOS dimer formation, a prerequisite for proper functioning of the enzyme. Stille and Negishi coupling reactions were used as key steps to form the carbon-carbon bond connecting the imidazopyrimidine core to the central cycloalkenyl, cycloalkyl and phenyl ring templates.