Evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase.
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Shankaran K, Donnelly KL, Shah SK, Guthikonda RN, MacCoss M, Humes JL, Pacholok SG, Grant SK, Kelly TM, Wong KK
Evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase.
Bioorg Med Chem Lett. 2004 Sep 6;14(17):4539-44.
- PubMed ID
- 15357988 [ View in PubMed]
- 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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- Binding Properties
Drug Target Property Measurement pH Temperature (°C) 2-Aminothiazoline Nitric oxide synthase, endothelial IC 50 (nM) 1100 N/A N/A Details