1-(1, 3-Benzodioxol-5-ylmethyl)-3-[4-(1H-imidazol-1-yl) phenoxy]-piperidine analogs as potent and selective inhibitors of nitric oxide formation

…, JL Tseng, M Whitlow, W Xu, S Yuan, G Phillips

Index: Wei, Robert G.; Adler, Marc; Davey, David; Ho, Elena; Mohan, Raju; Polokoff, Mark; Tseng, Jih-Lie; Whitlow, Marc; Xu, Wei; Yuan, Shendong; Phillips, Gary Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 9 p. 2499 - 2504

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Citation Number: 6

Abstract

A new series of 1-(1, 3-benzodioxol-5-ylmethyl)-3-[4-(1H-Imidazol-1-yl) phenoxy]-piperidine analogs were designed and identified as potent and selective inhibitors of NO formation based both on the crystal structure of a murine iNOS Δ114 monomer domain/inhibitor complex and inhibition of the NO formation in human A172 cell assays. Compound 12S showed high potency and high iNOS selectivity versus nNOS and eNOS.