Evaluation of new L-thiocitrulline derivatives as inhibitors of nitric oxide synthase.
New derivatives of L-thiocitrulline were prepared and assayed as inhibitors of the three isoforms of nitric oxide synthase. These compounds demonstrated weak inhibitory activity against the NOS isoforms and these results directly support a recently described model of the L-arginine binding site of NOS.
Ware
R W
RW
Department of Chemistry, Wake Forest University, Winston-Salem, NC 27109, USA.
King
S B
SB
D000818:Animals; D001665:Binding Sites; D002417:Cattle; D002956:Citrulline / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D007527:Isoenzymes / Q000037:antagonists & inhibitors; D007700:Kinetics; D051379:Mice; D019001:Nitric Oxide Synthase / Q000037:antagonists & inhibitors*; D052247:Nitric Oxide Synthase Type II; D051381:Rats; D013329:Structure-Activity Relationship; D013890:Thiourea / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology*
D004791:Enzyme Inhibitors; D007527:Isoenzymes; C086715:thiocitrulline; D002956:Citrulline; D019001:Nitric Oxide Synthase; D052247:Nitric Oxide Synthase Type II; C496317:Nos2 protein, mouse; C496318:Nos2 protein, rat; D013890:Thiourea