Design, synthesis, physicochemical, and pharmacological evaluation of gallic acid esters as non-ulcerogenic and gastroprotective anti-inflammatory agents

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• 作者：Mamta Sachdeva Dhingra ; Sameer Dhingra ; Renu Chadha…
• 关键词：Gallic acid esters ; Physicochemical ; Enzymatic hydrolysis on human plasma ; ADME profiling ; Anti ; inflammatory activity ; Carrageenan ; induced paw edema ; Gastroprotective ; Ulcerogenic activity
• 刊名：Medicinal Chemistry Research
• 出版年：2014
• 出版时间：November 2014
• 年：2014
• 卷：23
• 期：11
• 页码：4771-4788
• 全文大小：976 KB
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• 作者单位：Mamta Sachdeva Dhingra (1)
  Sameer Dhingra (2)
  Renu Chadha (1)
  Tejvir Singh (3)
  Maninder Karan (1)
  
  1. Department of Pharmacognosy and Natural Products, University Institute of Pharmaceutical Sciences, UGC Center of Advanced Study (UGC-CAS) in Pharmaceutical Sciences, Panjab University, Chandigarh, 160 014, India
  2. School of Pharmacy, Faculty of Medical Sciences, The University of the West Indies, St. Augustine, Eric Williams Medical Sciences Complex, Uriah Butler Highway, Champ Fleurs, Trinidad and Tobago
  3. Department of Chemistry, UGC Center of Advanced Study (UGC-CAS) in Chemistry, Panjab University, Chandigarh, 160 014, India
  
• ISSN：1554-8120

文摘

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.