N-(3-Acyloxy-2-Benzylpropyl)-N′-Dihydroxytetrahydrobenzazepine and Tetrahydroisoquinoline Thiourea Analogues as Vanilloid Receptor Ligands

Add time:09/27/2019    Source:sciencedirect.com

The vanilloid receptor represents a promising target for drug development. Building on our previous strategies which have generated potent agonists for VR1, we now describe a series of novel N-(3-acyloxy-2-benzylpropyl)-N′-dihydroxytetrahydrobenzazepine and tetrahydroisoquinoline thiourea analogues, several of which are potent VR1 antagonists. We report here the rationale for the design, the synthesis, and the in vitro characterization of activity in assays for [3H]resiniferatoxin binding and 45Ca influx using heterologously expressed rat VR1.

We also recommend Trading Suppliers and Manufacturers of N-(3,4-DIMETHYLPHENYL)THIOUREA (cas 16738-18-4). Pls Click Website Link as below: cas 16738-18-4 suppliers

Prev:N-[4-(Methylsulfonylamino)benzyl]thiourea analogues as vanilloid receptor antagonists: analysis of structure–activity relationships for the ‘C-Region’
Next:3-D-QSAR Analysis of N-(3-Acyloxy-2-benzylpropyl)-N′-dihydroxytetrahydrobenzazepine and Tetrahydroisoquinoline and N-(3-Acyloxy-2-benzylpropyl)-N′-(4-hydroxy-3-methoxybenzyl) Thioureas Analogues as Potent Vanilloid Receptor Ligands)