Evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase |
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| 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 |
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| Institution: | Department of Medicinal Chemistry, Merck Research Laboratory, PO Box 2000, Rahway, NJ 07065, USA. kothandaraman_shankaran@merck.com |
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| 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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