Design and Synthesis of Imidazopyrimidine Derivatives as Potent iNOS Dimerization Inhibitors
Guo-Hua Chu*, a, Bertrand Le Bourdonneca, Minghua Gua, Christopher W Ajelloa, Lara K Leistera, Ian Sellittoa, Joel A Casselb, Paul A Tuthilla, Heather O’ Harea, Robert N DeHavenb, Roland E Dollea
a Department of Chemistry, Adolor Corporation, 700 Pennsylvania Drive, Exton, PA 19341, USA
b Department of Pharmacology, Adolor Corporation, 700 Pennsylvania Drive, Exton, PA 19341, USA
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.
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* Address correspondence to this author at the Department of Chemistry, Adolor Corporation, 700 Pennsylvania Drive, Exton, PA 19341, USA; Tel: 484-595-1024; Fax: 484-595-1513; E-mail: firstname.lastname@example.org