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Bioorg Med Chem Lett. 2004 Nov 15;14(22):5513-9.

Synthesis and evaluation of pyridazinylpiperazines as vanilloid receptor 1 antagonists.

Author information

1
Discovery Research, Purdue Pharma L.P., 6 Cedar, Brook Drive, Cranbury, NJ 08512, USA. laykea.tafesse@pharma.com

Abstract

A structurally biased chemical library of pyridazinylpiperazine analogs was prepared in an effort to improve the pharmaceutical and pharmacological profile of the lead compound N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine-1(2H)-carboxamide (BCTC). The library was evaluated for VR1 antagonist activity in capsaicin-induced (CAP) and pH5.5-induced (pH) FLIPR assays in a human VR1-expressing HEK293 cell line. The most potent VR1 antagonists were found to have IC(50) values in the range of 9-200nM with improved pharmaceutical and pharmacological profiles versus the lead BCTC. These compounds represent possible second-generation BCTC analogs.

PMID:
15482915
DOI:
10.1016/j.bmcl.2004.09.010
[Indexed for MEDLINE]

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