Synthesis and evaluation of new sulfur-containing L-arginine-derived inhibitors of nitric oxide synthase

K Ichimori, DJ Stuehr, RN Atkinson…

Index: Ichimori, Kohji; Stuehr, Dennis J.; Atkinson, Robert N.; King, S. Bruce Journal of Medicinal Chemistry, 1999 , vol. 42, # 10 p. 1842 - 1848

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Citation Number: 24

Abstract

A series of compounds (7, 8, 10-17, 23) containing new functional groups derived by the combination of the substrate, intermediate, product, and known inhibitors of nitric oxide synthase (NOS) were prepared and evaluated against NOS. While none of the compounds assayed acted as a nitric oxide-producing substrate, the sulfur-containing arginine derivatives 10-12 were competitive inhibitors of iNOS with K i's of 202, 7, and 58 μM, ...