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Evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase
Authors:Shankaran K  Donnelly Karla L  Shah Shrenik K  Guthikonda Ravindra N  MacCoss Malcolm  Humes John L  Pacholok Stephen G  Grant Stephan K  Kelly T M  Wong K K
Affiliation:Department of Medicinal Chemistry, Merck Research Laboratory, PO Box 2000, Rahway, NJ 07065, USA. kothandaraman_shankaran@merck.com
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.
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