Substituted 2-aminopyridines as inhibitors of nitric oxide synthases

W K Hagmann; C G Caldwell; P Chen; P L Durette; C K Esser; T J Lanza; I E Kopka; R Guthikonda; S K Shah; M MacCoss; R M Chabin; D Fletcher; S K Grant; B G Green; J L Humes; T M Kelly; S Luell; R Meurer; V Moore; S G Pacholok; T Pavia; H R Williams; K K Wong

doi:10.1016/s0960-894x(00)00389-9

Substituted 2-aminopyridines as inhibitors of nitric oxide synthases

Bioorg Med Chem Lett. 2000 Sep 4;10(17):1975-8. doi: 10.1016/s0960-894x(00)00389-9.

Authors

Affiliation

¹ Department of Medicinal Chemistry, Merck Research Laboratories Rahway, NJ 07065, USA. william_hagmann@merck.com

PMID: 10987430
DOI: 10.1016/s0960-894x(00)00389-9

Abstract

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.

MeSH terms

Aminopyridines / chemical synthesis*
Aminopyridines / pharmacology
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacology
Humans
Nitric Oxide Synthase / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Aminopyridines
Enzyme Inhibitors
Nitric Oxide Synthase