2. Academic Validation
  3. 4-(2-pyridyl)piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists

4-(2-pyridyl)piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists

  • Bioorg Med Chem Lett. 2003 Oct 20;13(20):3611-6. doi: 10.1016/s0960-894x(03)00759-5.
Qun Sun 1,  Laykea Tafesse,  Khondaker Islam,  Xiaoming Zhou,  Sam F Victory,  Chongwu Zhang,  Mohamed Hachicha,  Lori A Schmid,  Aniket Patel,  Yakov Rotshteyn,  Kenneth J Valenzano,  Donald J Kyle
Affiliations

Affiliation

  • 1 Purdue Pharma L.P., 6 Cedar Brook Drive, Cranbury, NJ 08512, USA. qun.sun@pharma.com
PMID: 14505681 DOI: 10.1016/s0960-894x(03)00759-5
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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