Hit-to-lead optimization of pyrrolo[1,2-a]quinoxalines as novel cannabinoid type 1 receptor antagonists |
| |
| Authors: | György Szabó Róbert Kiss Dóra Páyer-Lengyel Krisztina Vukics Judit Szikra Andrea Baki László Molnár János Fischer György M. Keserű |
| |
| Affiliation: | 1. Gedeon Richter Plc, Budapest 10, PO Box 27, H-1475, Hungary;2. Department of Pharmaceutical Chemistry, Semmelweis University, Budapest, H?gyes Endre u. 9., H-1092, Hungary |
| |
| Abstract: | ![]()
Hit-to-lead optimization of a novel series of N-alkyl-N-[2-oxo-2-(4-aryl-4H-pyrrolo[1,2-a]quinoxaline-5-yl)-ethyl]-carboxylic acid amides, derived from a high throughput screening (HTS) hit, are described. Subsequent optimization led to identification of in vitro potent cannabinoid 1 receptor (CB1R) antagonists representing a new class of compounds in this area. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
