title: Evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase.
abstract: Syntheses and evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase (NOS) are discussed. An extensive SAR was established for pyrrolidin-2-imines class of compounds. The amidines came out as the most potent inhibitors in addition to displaying selectivity.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratory, PO Box 2000, Rahway, NJ 07065, USA. kothandaraman_shankaran@merck.com
authors.forename: K
authors.initials: K
authors.lastname: Shankaran
authors.forename: Karla L
authors.initials: KL
authors.lastname: Donnelly
authors.forename: Shrenik K
authors.initials: SK
authors.lastname: Shah
authors.forename: Ravindra N
authors.initials: RN
authors.lastname: Guthikonda
authors.forename: Malcolm
authors.initials: M
authors.lastname: MacCoss
authors.forename: John L
authors.initials: JL
authors.lastname: Humes
authors.forename: Stephen G
authors.initials: SG
authors.lastname: Pacholok
authors.forename: Stephan K
authors.initials: SK
authors.lastname: Grant
authors.forename: T M
authors.initials: TM
authors.lastname: Kelly
authors.forename: K K
authors.initials: KK
authors.lastname: Wong
mesh_terms: D004353:Drug Evaluation, Preclinical / Q000379:methods; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D007097:Imines / Q000737:chemistry* / Q000494:pharmacology; D019001:Nitric Oxide Synthase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011759:Pyrrolidines / Q000737:chemistry* / Q000494:pharmacology; D013844:Thiazoles / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D004791:Enzyme Inhibitors; D007097:Imines; D011759:Pyrrolidines; D013844:Thiazoles; D019001:Nitric Oxide Synthase