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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
Authors Info & Affiliations
, 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
Authors Info & Affiliations
The Open Medicinal Chemistry Journal
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18 Nov 2009 •
RESEARCH ARTICLE
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DOI: 10.2174/1874104500903010008
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.