Potent heteroarylpiperidine and carboxyphenylpiperidine 1-alkyl-cyclopentane carboxamide CCR2 antagonists

…, PP Vicario, J Di Salvo, JM Ayala, M Struthers…

文献索引：Pasternak, Alexander; Goble, Stephen D.; Vicario, Pasquale P.; Di Salvo, Jerry; Ayala, Julia M.; Struthers, Mary; DeMartino, Julie A.; Mills, Sander G.; Yang, Lihu Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 3 p. 994 - 998

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被引用次数: 15

摘要

This report describes replacement of the 4-(4-fluorophenyl) piperidine moiety in our CCR2 antagonists with 4-heteroaryl piperidine and 4-(carboxyphenyl)-piperidine subunits. Some of the resulting analogs retained potency in our CCR2 binding assay and had improved selectivity versus the IKr channel; poor selectivity against IKr had been a liability of earlier analogs in this series.