Research paperSynthesis of novel 2-(1-adamantanylcarboxamido)thiophene derivatives. Selective cannabinoid type 2 (CB2) receptor agonists as potential agents for the treatment of skin inflammatory disease

Add time:08/16/2019    Source:sciencedirect.com

A set of CB2R ligands, based on the thiophene scaffold, was synthesized and evaluated in in vitro assays. Compounds 8c-i, k, l, bearing the 3-carboxylate and 2-(adamantan-1-yl)carboxamido groups together with apolar alkyl/aryl substituents at 5-position or at 4- and 5-positions of the thiophene ring possess high CB2R affinity at low nanomolar concentration, good receptor selectivity, and agonistic functional activity. The full agonist 8g, showing the best balance between receptor affinity and selectivity, was tested in vitro in an experimental model of allergic contact dermatitis and proved to be able to block the release of MCP-2 in HaCaT cells at 10 μM concentration.

We also recommend Trading Suppliers and Manufacturers of 5-AMINO-4-CYANO-N,N-DIETHYL-3-METHYLTHIOPHENE-2-CARBOXAMIDE (cas 107815-98-5). Pls Click Website Link as below: cas 107815-98-5 suppliers

Prev:Chapter IV Brain endothelin and natriuretic peptide receptors
Next:Research paperStructural basis for potent inhibition of d-amino acid oxidase by thiophene carboxylic acids)