Substituted 2-aminopyridines as inhibitors of nitric oxide synthases

A series of substituted 2-aminopyridines was prepared and evaluated as inhibitors of human nitric oxide synthases (NOS). 4,6-Disubstitution enhanced both potency and specificity for the inducible NOS with the most potent compound having an IC 50 of 28 nM.

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 10; no. 17; pp. 1975 - 1978
Main Authors:	Hagmann, William K, Caldwell, Charles G, Chen, Ping, Durette, Philippe L, Esser, Craig K, Lanza, Thomas J, Kopka, Ihor E, Guthikonda, Ravi, Shah, Shrenik K, MacCoss, Malcolm, Chabin, Renee M, Fletcher, Daniel, Grant, Stephan K, Green, Barbara G, Humes, John L, Kelly, Theresa M, Luell, Sylvie, Meurer, Roger, Moore, Vernon, Pacholok, Stephen G, Pavia, Tony, Williams, Hollis R, Wong, Kenny K
Format:	Journal Article
Language:	English
Published:	Oxford Elsevier Ltd 04-09-2000 Elsevier
Subjects:	Aminopyridines - chemical synthesis Aminopyridines - pharmacology Biological and medical sciences Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Humans Medical sciences Miscellaneous Nitric Oxide Synthase - antagonists & inhibitors Pharmacology. Drug treatments Structure-Activity Relationship Human Rat Enzyme Nitrogen heterocycle Isozyme Rodentia Enzyme inhibitor Selectivity In vitro Nitric-oxide synthase Pyridine derivatives In vivo Vertebrata Mammalia Structure activity relation Mouse Animal Oxidoreductases Chemical synthesis
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Summary:	A series of substituted 2-aminopyridines was prepared and evaluated as inhibitors of human nitric oxide synthases (NOS). 4,6-Disubstitution enhanced both potency and specificity for the inducible NOS with the most potent compound having an IC 50 of 28 nM.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(00)00389-9