期刊
MEDICINAL CHEMISTRY RESEARCH
卷 23, 期 11, 页码 4771-4788出版社
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-014-1041-x
关键词
Gallic acid esters; Physicochemical; Enzymatic hydrolysis on human plasma; ADME profiling; Anti-inflammatory activity; Carrageenan-induced paw edema; Gastroprotective; Ulcerogenic activity
资金
- University Grants Commission
In our effort to identify the effective gastric sparing and protective anti-inflammatory agents, a series of gallic acid esters were synthesized, characterized, and studied to assess their physicochemical properties. Subsequently, the esters were evaluated for their anti-inflammatory activity and effect on gastric mucosa by most active compounds. All the compounds exhibited promising anti-inflammatory activity in carrageenan-induced rat paw edema model. In particular, 7a, 7c, 7f, and 7h emerged as the most active compounds in the series. The findings of gastric ulcer and antioxidant studies suggested these compounds as non-ulcerogenic and gastroprotective. Further, the predicted ADME properties of all the tested compounds were found to be in the ranges as predicted by QikProp for 95 % of known oral drugs and also satisfy the Lipinski's rule of five.
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