Synthesis and evaluation of thiazole carboxamides as vanilloid receptor 1 (TRPV1) antagonists

Autor:	Qingyian Liu, Randall W. Hungate, Rami Tamir, Shimin Xu, Elizabeth M. Doherty, James J. S. Treanor, Christopher H. Fotsch, Mark H. Norman, Lana Klionsky, Yunxin Bo, Nianhe Han, Ning Xi, Narender R. Gavva
Rok vydání:	2005
Předmět:	medicine.drug_class Stereochemistry Clinical Biochemistry TRPV1 TRPV Cation Channels Pharmaceutical Science chemistry.chemical_element Carboxamide CHO Cells Calcium Biochemistry Chemical synthesis Structure-Activity Relationship chemistry.chemical_compound Cricetulus Cricetinae Drug Discovery medicine Animals Humans Thiazole Molecular Biology Oxamic Acid Molecular Structure Organic Chemistry Antagonist Amides In vitro Thiazoles chemistry Capsaicin Molecular Medicine lipids (amino acids peptides and proteins)
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 15:5211-5217
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2005.08.100
Popis:	A thiazole derivative, 2-(2,6-dichlorobenzyl)-N-(4-isopropylphenyl) thiazole-4-carboxamide (1), was identified as a TRPV1 antagonist. We synthesized various thiazole analogs and evaluated them for their ability to block capsaicin- or acid-induced calcium influx in TRPV1-expressing CHO cells. The IC50 values of the most potent antagonists were ca. 0.050 μM in these assays.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aaa35474f27b282cc330e041798d14e9 https://doi.org/10.1016/j.bmcl.2005.08.100 Zobrazit plný text záznamu Full Text from ScienceDirect