Design, synthesis, and biological evaluation of novel alkenylthiophenes as potent and selective CB1 cannabinoid receptor antagonists
Journal
Organic & Biomolecular Chemistry
Journal Volume
6
Journal Issue
3
Pages
447-450
Date Issued
2008
Author(s)
Cheng-Ming Chu
Abstract
A novel class of (5-(pent-1-enyl)thiophen-2-yl)pyrazole antagonists was discovered, many of which exhibited potent CB1 activity and good CB1/2 selectivity, suggesting that along with a 1,3-transposition of the carbonyl of the pyrazole 3-carboxamide, bioisosteric replacement of the conventional pyrazole 5-aryl group with a thienyl ring substituted with an appropriate alkenyl moiety is viable.
SDGs
Publisher
Royal Society of Chemistry
Type
journal article