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 IC50 of 28 nM.
Hagmann
W K
WK
Department of Medicinal Chemistry, Merck Research Laboratories Rahway, NJ 07065, USA. william_hagmann@merck.com
Caldwell
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Chen
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Williams
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D000631:Aminopyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D019001:Nitric Oxide Synthase / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D000631:Aminopyridines; D004791:Enzyme Inhibitors; D019001:Nitric Oxide Synthase