Discovery of benzamide analogs as negative allosteric modulators of human neuronal nicotinic receptors: Pharmacophore modeling and structure–activity …

…, S Long, TF González-Cestari, BJ Henderson…

Index: Yi, Bitna; Long, Sihui; Gonzalez-Cestari, Tatiana F.; Henderson, Brandon J.; Pavlovicz, Ryan E.; Werbovetz, Karl; Li, Chenglong; McKay, Dennis B. Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 15 p. 4730 - 4743

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Citation Number: 4

Abstract

The present study describes our ongoing efforts toward the discovery of drugs that selectively target nAChR subtypes. We exploited knowledge on nAChR ligands and their binding site that were previously identified by our laboratory through virtual screenings and identified benzamide analogs as a novel chemical class of neuronal nicotinic receptor (nAChR) ligands. The lead molecule, compound 1 (4-(allyloxy)-N-(6-methylpyridin-2-yl) ...