Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2005 Feb 1;15(3):719-23.
doi: 10.1016/j.bmcl.2004.11.021.

4-(2-Pyridyl)piperazine-1-benzimidazoles as potent TRPV1 antagonists

Bin Shao  1 , Jincheng Huang, Qun Sun, Kenneth J Valenzano, Lori Schmid, Scott Nolan
Affiliations

4-(2-Pyridyl)piperazine-1-benzimidazoles as potent TRPV1 antagonists

Bin Shao et al. Bioorg Med Chem Lett. .

Abstract

A series of 4-(2-pyridyl)piperazine-1-benzimidazole analogues based on compound 1 was synthesized and evaluated for TRPV1 antagonist activity in capsaicin-induced (CAP) and pH5.5-induced (pH) FLIPR assays in a human TRPV1-expressing HEK293 cell line. Potent TRPV1 antagonists were identified through SAR studies. From these studies, several antagonists were found, with IC(50) values ranging from 32 nM to approximately 5000 nM. Among these, 11 [IC(50)=90 nM (CAP) and 104 nM (pH)] was further evaluated and found to be orally available in rats (F%=19.7).

PubMed Disclaimer

LinkOut - more resources