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


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© Chu et al.; Licensee Bentham Open.

open-access license: This is an open access article licensed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/3.0/)which permits unrestricted, non-commercial use, distribution and reproduction in any medium, provided the work is properly cited.

* 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: chuguo@hotmail.com


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.