Potent heteroarylpiperidine and carboxyphenylpiperidine 1-alkyl-cyclopentane carboxamide CCR2 antagonists |
| |
| Authors: | Pasternak Alexander Goble Stephen D Vicario Pasquale P Di Salvo Jerry Ayala Julia M Struthers Mary DeMartino Julie A Mills Sander G Yang Lihu |
| |
| Institution: | Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, 126 East Lincoln Avenue, Rahway, NJ 07065, USA. alexander_pasternak@merck.com |
| |
| Abstract: | 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 I(Kr) channel; poor selectivity against I(Kr) had been a liability of earlier analogs in this series. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ |
