Design and Synthesis of Imidazopyrimidine Derivatives as Potent iNOS Dimerization Inhibitors

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

Design and Synthesis of Imidazopyrimidine Derivatives as Potent iNOS Dimerization Inhibitors

Guo-Hua Chu^{*, a}, Bertrand Le Bourdonnec^a, Minghua Gu^a, Christopher W Ajello^a, Lara K Leister^a, Ian Sellitto^a, Joel A Cassel^b, Paul A Tuthill^a, Heather O’ Hare^a, Robert N DeHaven^b, Roland E Dolle^a

^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

Article Information

Identifiers and Pagination:

Year: 2009
Volume: 3
First Page: 8
Last Page: 13
Publisher ID: TOMCJ-3-8
DOI: 10.2174/1874104500903010008

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

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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

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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RESEARCH ARTICLE

Design and Synthesis of Imidazopyrimidine Derivatives as Potent iNOS Dimerization Inhibitors

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