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- …

…, J Ramnauth, P Renton, T Rybak, S Silverman…

Index: Annedi, Subhash C.; Maddaford, Shawn P.; Ramnauth, Jailall; Renton, Paul; Rybak, Taras; Silverman, Sarah; Rakhit, Suman; Mladenova, Gabriela; Dove, Peter; Andrews, John S.; Zhang, Dongqin; Porreca, Frank European Journal of Medicinal Chemistry, 2012 , vol. 55, p. 94 - 107,14 Title/Abstract Full Text Show Details Annedi, Subhash C.; Maddaford, Shawn P.; Ramnauth, Jailall; Renton, Paul; Rybak, Taras; Silverman, Sarah; Rakhit, Suman; Mladenova, Gabriela; Dove, Peter; Andrews, John S.; Zhang, Dongqin; Porreca, Frank European Journal of Medicinal Chemistry, 2012 , vol. 55, p. 94 - 107

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Citation Number: 11

Abstract

We recently reported a series of 1, 6-disubstituted indoline-based thiophene amidine compounds (5) as selective neuronal nitric oxide synthase (nNOS) inhibitors to mitigate the cardiovascular liabilities associated with hERG K+ channel inhibition (IC50= 4.7 μM) with previously reported tetrahydroquinoline-based selective nNOS inhibitors (4). The extended structure–activity relationship studies within the indoline core led to the identification of 43 ...