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1,2,3,4-tetrahydroquinoline-based selective human neuronal nitric oxide synthase (nNOS) inhibitors: lead optimization studies resulting in the identification of N-(1-(2-(methylamino)ethyl)-1,2,3,4-tetrahydroquinolin-6-yl)thiophene-2-carboximidamide as a preclinical development candidate.
Ramnauth J, Renton P, Dove P, Annedi SC, Speed J, Silverman S, Mladenova G, Maddaford SP, Zinghini S, Rakhit S, Andrews J, Lee DK, Zhang D, Porreca F. Ramnauth J, et al. Among authors: renton p. J Med Chem. 2012 Mar 22;55(6):2882-93. doi: 10.1021/jm3000449. Epub 2012 Mar 1. J Med Chem. 2012. PMID: 22335555
Design, synthesis, and biological evaluation of 3,4-dihydroquinolin-2(1H)-one and 1,2,3,4-tetrahydroquinoline-based selective human neuronal nitric oxide synthase (nNOS) inhibitors.
Ramnauth J, Speed J, Maddaford SP, Dove P, Annedi SC, Renton P, Rakhit S, Andrews J, Silverman S, Mladenova G, Zinghini S, Nair S, Catalano C, Lee DK, De Felice M, Porreca F. Ramnauth J, et al. Among authors: renton p. J Med Chem. 2011 Aug 11;54(15):5562-75. doi: 10.1021/jm200648s. Epub 2011 Jul 8. J Med Chem. 2011. PMID: 21699209 Free PMC article.
Discovery of cis-N-(1-(4-(methylamino)cyclohexyl)indolin-6-yl)thiophene-2-carboximidamide: a 1,6-disubstituted indoline derivative as a highly selective inhibitor of human neuronal nitric oxide synthase (nNOS) without any cardiovascular liabilities.
Annedi SC, Ramnauth J, Maddaford SP, Renton P, Rakhit S, Mladenova G, Dove P, Silverman S, Andrews JS, Felice MD, Porreca F. Annedi SC, et al. Among authors: renton p. J Med Chem. 2012 Jan 26;55(2):943-55. doi: 10.1021/jm201564u. Epub 2012 Jan 10. J Med Chem. 2012. PMID: 22175766
Discovery of a potent, orally bioavailable and highly selective human neuronal nitric oxide synthase (nNOS) inhibitor, N-(1-(piperidin-4-yl)indolin-5-yl)thiophene-2-carboximidamide as a pre-clinical development candidate for the treatment of migraine.
Annedi SC, Maddaford SP, Ramnauth J, Renton P, Rybak T, Silverman S, Rakhit S, Mladenova G, Dove P, Andrews JS, Zhang D, Porreca F. Annedi SC, et al. Among authors: renton p. Eur J Med Chem. 2012 Sep;55:94-107. doi: 10.1016/j.ejmech.2012.07.006. Epub 2012 Jul 14. Eur J Med Chem. 2012. PMID: 22840695
296 results