Structure-activity relationships of potent, selective inhibitors of neuronal nitric oxide synthase based on the 6-phenyl-2-aminopyridine structure.

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Lowe JA 3rd, Qian W, Drozda SE, Volkmann RA, Nason D, Nelson RB, Nolan C, Liston D, Ward K, Faraci S, Verdries K, Seymour P, Majchrzak M, Villalobos A, White WF

Structure-activity relationships of potent, selective inhibitors of neuronal nitric oxide synthase based on the 6-phenyl-2-aminopyridine structure.

J Med Chem. 2004 Mar 11;47(6):1575-86.

PubMed ID

14998342 [ View in PubMed

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Abstract

The synthesis and structure-activity relationships of a series of 6-phenyl-2-aminopyridines that potently and selectively inhibit the neuronal isoform of nitric oxide synthase (nNOS) are described. Compound 14bi from this series exhibits potent in vivo activity in harmaline-induced cGMP formation in rat cerebellum, a functional model of nNOS inhibition, and in the PCP-induced hypermotility model in the rat. These results suggest that 14bi may be a useful reagent for evaluating potential therapeutic applications of nNOS inhibitors in the central nervous system.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
7-Nitroindazole	Nitric oxide synthase, endothelial	IC 50 (nM)	2500	N/A	N/A	Details