The synthesis and structure–activity relationship of 4-benzimidazolyl-piperidinylcarbonyl-piperidine analogs as histamine H 3 antagonists

…, L Favreau, C Nardo, WA Korfmacher, RE West…

Index: Ting, Pauline C.; Lee, Joe F.; Albanese, Margaret M.; Wu, Jie; Aslanian, Robert; Favreau, Leonard; Nardo, Cymbelene; Korfmacher, Walter A.; West, Robert E.; Williams, Shirley M.; Anthes, John C.; Rivelli, Maria A.; Corboz, Michel R.; Hey, John A. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 17 p. 5004 - 5008

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Citation Number: 5

Abstract

A structure–activity relationship study of the lead piperazinylcarbonylpiperidine compound 3 resulted in the identification of 4-benzimidazolyl-piperidinylcarbonyl-piperidine 6h as a histamine-3 (H3) receptor antagonist. Additional optimization of 6h led to the identification of compounds 11i–k with Ki⩽ 0.5 nM and good in vivo activity.