Synthesis, Hydrolysis Kinetics and Pharmacological Evaluation of Aceclofenac Prodrugs

ISSN: 1875-614X (Online)
ISSN: 1871-5230 (Print)


Volume 15, 3 Issues, 2016


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Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Inflammatory and Anti-Allergy Agents

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Editor-in-Chief:
Claudiu T. Supuran
Neurofarba Department
University of Florence
Florence
Italy


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Synthesis, Hydrolysis Kinetics and Pharmacological Evaluation of Aceclofenac Prodrugs



Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry, 13(3): 188-194.

Author(s): Bharat V. Dhokchawle and Anil B Bhandari.

Affiliation: Department of Pharmaceutical Chemistry, St. John Institute of Pharmacy and Research, Vevoor, Manor Road, Palghar (E), Tal-Palghar, Thane (M.S) 401404, India.

Abstract

The mutual prodrugs of aceclofenac with various naturally available antioxidants; menthol, thymol, eugenol, guiacol and vanillin have been synthesized by the DCC coupling method, purified and characterized by spectral data, as well as, partition coefficient, solubility and hydrolytic studies. The title compounds have more lipophilic character as compared to the parent moieties and good stability in acidic environment, which is prerequisite for the oral absorption of the drug. Under gastric as well as intestinal pH conditions these prodrugs showed variable susceptibility towards hydrolysis. The synthesized derivatives were evaluated for antiinflammatory, analgesic activities and ulcerogenic potential. Prodrug showed improved solubility in organic solvents, which implies lipophilic character of ester prodrugs and were also found to be chemically stable in acidic environment. The aceclofenac mutual prodrugs showed improved analgesic and anti-inflammatory activities with reduced ulcerogenicity.




Keywords:

Aceclofenac, antioxidant, anti-inflammatory, analgesic, ulcerogenicity, prodrug, dicyclohexylcarbodimide.



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Article Details

Volume: 13
Issue Number: 3
First Page: 188
Last Page: 194
Page Count: 7
DOI: 10.2174/1871523013666141114203105
Price: $58
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