4-(2-pyridyl)piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists |
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| Authors: | Sun Qun Tafesse Laykea Islam Khondaker Zhou Xiaoming Victory Sam F Zhang Chongwu Hachicha Mohamed Schmid Lori A Patel Aniket Rotshteyn Yakov Valenzano Kenneth J Kyle Donald J |
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| Affiliation: | Purdue Pharma L.P., 6 Cedar Brook Drive, Cranbury, NJ 08512, USA. qun.sun@pharma.com |
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| Abstract: | ![]()
A series of 4-(2-pyridyl)piperazine-1-carboxamide analogues based on the lead compound 1 was synthesized and evaluated for VR1 antagonist activity in capsaicin-induced (CAP) and pH (5.5)-induced (pH) FLIPR assays in a rat VR1-expressing HEK293 cell line. Potent VR1 antagonists were identified through SAR studies. From these studies, 18 was found to be very potent in the in vitro assay [IC(50)=4.8 nM (pH) and 35 nM (CAP)] and orally available in rat (F%=15.1). |
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