3, 5-Disubstituted indole derivatives as selective human neuronal nitric oxide synthase (nNOS) inhibitors

…, SP Maddaford, J Ramnauth, P Renton, J Speed…

Index: Annedi, Subhash C.; Maddaford, Shawn P.; Ramnauth, Jailall; Renton, Paul; Speed, Joanne; Rakhit, Suman; Andrews, John S.; Porreca, Frank Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 5 p. 1980 - 1984

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Citation Number: 11

Abstract

A series of 3, 5-disubstituted indole derivatives was designed, synthesized and evaluated as inhibitors of human nitric oxide synthase (NOS). Various guanidine isosteric groups were explored at the 5-position of the indole ring, while keeping the basic amine side chain such as N-methylpiperidine ring, fixed at the 3-position of the indole ring. Compounds having 2- thiophene amidine and 2-furanyl amidine groups (7, 8, 10 and 12) showed increased ...