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Discovery of N-(3-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-1H-indol-6-yl) thiophene-2-carboximidamide as a selective inhibitor of human neuronal nitric oxide synthase (nNOS) for the treatment of pain.
Annedi SC, Maddaford SP, Mladenova G, Ramnauth J, Rakhit S, Andrews JS, Lee DK, Zhang D, Porreca F, Bunton D, Christie L. Annedi SC, et al. Among authors: maddaford sp. J Med Chem. 2011 Oct 27;54(20):7408-16. doi: 10.1021/jm201063u. Epub 2011 Oct 5. J Med Chem. 2011. PMID: 21923116
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: maddaford sp. 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: maddaford sp. J Med Chem. 2012 Jan 26;55(2):943-55. doi: 10.1021/jm201564u. Epub 2012 Jan 10. J Med Chem. 2012. PMID: 22175766
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: maddaford sp. J Med Chem. 2012 Mar 22;55(6):2882-93. doi: 10.1021/jm3000449. Epub 2012 Mar 1. J Med Chem. 2012. PMID: 22335555
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: maddaford sp. 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
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