Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1361954 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
Heteroalicyclic carboxamidines were synthesised and evaluated as inhibitors of nitric oxide synthases. (2R)-2-Pyrrolidinecarboxamidine, in particular, was shown to be a highly potent in vitro (IC50 = 0.12 μM) and selective iNOS inhibitor (>100-fold vs both eNOS and nNOS), with probable binding to the key anchoring glutamate residue and co-ordination to the haem iron.
Graphical abstractThe exploration of heterocyclic carboxamidines as iNOS inhibitors led to the identification of (2R)-2-pyrrolidinecarboxamidine as a potent and selective haem-co-ordinating inhibitor.Figure optionsDownload full-size imageDownload as PowerPoint slide
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Robert J. Young, Wendy Alderton, Anthony D.R. Angell, Paul J. Beswick, David Brown, C. Lynn Chambers, Miriam C. Crowe, John Dawson, Christopher C.F. Hamlett, Simon T. Hodgson, Savvas Kleanthous, Richard G. Knowles, Linda J. Russell, Richard Stocker,