Synthesis,In Vitro Anti-Inflammatory Activity and Molecular Docking of Butyrate Benzophenone Compound

摘要

Twelve new butyric acid ester-containing benzophenone compounds were synthesized by Friedel-Crafts acylation reaction,Esterification reaction and Clemmensen reduction reaction.Biological evaluation indicated that all compounds exhibit certain anti-inflammatory activities against Lipopolysaccharides(LPS)induced inflammatory in mouse macrophages(RAW264.7).In particular,a novel compound,4-[3-isobutyl-4-methoxy-5-(pyrrolidine-1-carbonyl)-phenyl]-butyric acid ethyl ester(7 g)showed the highest anti-inflammatory activity with the IC_(50)value of 18.60±7.79 μM for nitric oxide(NO)which is better than that of the positive control Ibuprofen(IC_(50)=37.6± 6.9 μM)and the positive control compound of COX-2 inhibitor(IC_(50)=47.2±0.4 μM),indicating that it could be a potential candidate for further development as a anti-inflammatory drug.