Evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase.
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.
Shankaran
K
K
Department of Medicinal Chemistry, Merck Research Laboratory, PO Box 2000, Rahway, NJ 07065, USA. kothandaraman_shankaran@merck.com
Donnelly
Karla L
KL
Shah
Shrenik K
SK
Guthikonda
Ravindra N
RN
MacCoss
Malcolm
M
Humes
John L
JL
Pacholok
Stephen G
SG
Grant
Stephan K
SK
Kelly
T M
TM
Wong
K K
KK
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
D004791:Enzyme Inhibitors; D007097:Imines; D011759:Pyrrolidines; D013844:Thiazoles; D019001:Nitric Oxide Synthase