Synthesis and anti-inflammatory activity of novel isobutyl benzophenone derivatives

VernacularTitle:新型含异丁基苯甲酮类化合物的合成及抗炎活性的初步研究
Author: Lu YANG ¹ ; Hang SHI ¹ ; Yun-lan LI ¹ ; Xi CHEN ¹ ; Si-qing NIU ¹ ; Xiao-zhi QIAO ¹ ; Jia-qi MAI ¹ ; Qing-shan LI ²
Author Information

1. College of Pharmacy, Shanxi Medical University, Taiyuan 030001, China
2. Shanxi University of Chinese Medical, Taiyuan 030619, China
Publication Type:ORIGINAL ARTICLES
Keywords: isobutylbenzophenone; synthesis; NO; anti-inflammatory effect
From: Acta Pharmaceutica Sinica 2018;53(2):256-262
CountryChina
Language:Chinese
Abstract: Twenty target compounds were synthesized by the reduction reaction of HUANG Minglong and Friedel-Crafts acylation reaction in this study. The inhibitory effects of the new compounds were tested on NO production in LPS-induced mouse macrophage RAW264.7 cells, a cellular inflammation model. The structure-activity relationships were discussed. The structures of target compounds were confirmed by ESI-MS, ¹H NMR and ¹³C NMR. In vitro activity experiments showed that 18 compounds had certain anti-inflammatory effects at the concentration of 40 μmol·L^-1, of which 9a, 8b, 7c and 9c showed strong anti-inflammatory activities, and IC₅₀ of 7c and 9c were comparable to the positive control drug ibuprofen.