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
Identifiers and Pagination:Year: 2009
First Page: 8
Last Page: 13
Publisher ID: TOMCJ-3-8
Article History:Received Date: 10/7/2009
Revision Received Date: 19/8/2009
Acceptance Date: 20/8/2009
Electronic publication date: 18/11/2009
Collection year: 2009
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.
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.