Synthesis,SAR and intramolecular hydrogen bonding pattern of 1,3,5-trisubstituted 4,5-dihydropyrazoles as potent cannabinoid CB1 receptor antagonists |
| |
| Authors: | Jos HM Lange Martina AW van der Neut Arnold P den Hartog Henri C Wals Jan Hoogendoorn Herman H van Stuivenberg Bernard J van Vliet Chris G Kruse |
| |
| Institution: | Solvay Pharmaceuticals, Research Laboratories, Chemical Design & Synthesis Unit, C. J. van Houtenlaan 36, 1381 CP Weesp, The Netherlands |
| |
| Abstract: | The synthesis, structure–activity relationship (SAR) studies and intramolecular hydrogen bonding pattern of 1,3,5-trisubstituted 4,5-dihydropyrazoles are described. The target compounds 6–18 represent a novel class of potent and selective CB1 receptor antagonists. Based on X-ray diffraction data, the orally active 17 is shown to elicit a different intramolecular H-bonding mode as compared to ibipinabant (3) and SLV330 (4). |
| |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
