Journal of Pharmaceutical Research

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Synthesis, Characterization and Pharmacological Evaluation of Ester Prodrugs of Naproxen


Affiliations
1 Vellore Institute of Technology, Vellore – 632 007, Tamil Nadu, India
2 Ratnam Institute of Pharmacy, Pidathapolur, Nellore – 524 346, Andhra Pradesh, India
3 SRM College of Pharmacy, SRM University, Kattankulathur, Chennai-603203, TamilNadu, India
4 DCRN College of Pharmacy, Ilkollu, Andhra Pradesh, India
 

Naproxen suffers from the general side effects of NSAIDs, owing to presence of free carboxylic acid group. The study aimed to retard the adverse effects of gastrointestinal origin. Ten prodrugs of Naproxen were synthesized by amidation with N-Substituted-2-chloroacetamide. Purified synthesized prodrugs were characterized by their M.P., TLC, IR, 1H NMR, MS and elemental analysis. The purity of the synthesized prodrugs was monitored by HPLC. Synthesized prodrugs were subjected to acute oral toxicity studies, anti-inflammatory activity and reduced ulcerogenic activity. Marked reduction of ulcerogenic activity and anti-inflammatory activities were obtained in all cases as compared to Naproxen. Among synthesized prodrugs, viz. A-5, A-6 and A-8 showed significant anti-inflammatory activity and A-2 and A-5 showed reduced ulcerogenic activity compared to Naproxen. In acute oral toxicity studies, all synthesized prodrugs were found to be non toxic at dose of 2000 mg/kg.

Keywords

Naproxen, Prodrugs, Glycolamide Ester Conjugates, Characterization, Pharmacological Activity.
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  • Synthesis, Characterization and Pharmacological Evaluation of Ester Prodrugs of Naproxen

Abstract Views: 222  |  PDF Views: 94

Authors

V. Sai Saraswathi
Vellore Institute of Technology, Vellore – 632 007, Tamil Nadu, India
D. Saravanan
Ratnam Institute of Pharmacy, Pidathapolur, Nellore – 524 346, Andhra Pradesh, India
J. Padmavathy
Ratnam Institute of Pharmacy, Pidathapolur, Nellore – 524 346, Andhra Pradesh, India
I. Aparna Lakshmi
Ratnam Institute of Pharmacy, Pidathapolur, Nellore – 524 346, Andhra Pradesh, India
D. Raju
SRM College of Pharmacy, SRM University, Kattankulathur, Chennai-603203, TamilNadu, India
Ch. Praveen kumar
Ratnam Institute of Pharmacy, Pidathapolur, Nellore – 524 346, Andhra Pradesh, India
C. R. Prakash
DCRN College of Pharmacy, Ilkollu, Andhra Pradesh, India

Abstract


Naproxen suffers from the general side effects of NSAIDs, owing to presence of free carboxylic acid group. The study aimed to retard the adverse effects of gastrointestinal origin. Ten prodrugs of Naproxen were synthesized by amidation with N-Substituted-2-chloroacetamide. Purified synthesized prodrugs were characterized by their M.P., TLC, IR, 1H NMR, MS and elemental analysis. The purity of the synthesized prodrugs was monitored by HPLC. Synthesized prodrugs were subjected to acute oral toxicity studies, anti-inflammatory activity and reduced ulcerogenic activity. Marked reduction of ulcerogenic activity and anti-inflammatory activities were obtained in all cases as compared to Naproxen. Among synthesized prodrugs, viz. A-5, A-6 and A-8 showed significant anti-inflammatory activity and A-2 and A-5 showed reduced ulcerogenic activity compared to Naproxen. In acute oral toxicity studies, all synthesized prodrugs were found to be non toxic at dose of 2000 mg/kg.

Keywords


Naproxen, Prodrugs, Glycolamide Ester Conjugates, Characterization, Pharmacological Activity.