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Tyrosine and glycine derivatives as potential prodrugs: design, synthesis, and pharmacological evaluation of amide derivatives of mefenamic acid.

Author: Ashok KumarC K, RasheedArun

Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Overview

This study investigated the synthesis, pharmacological activity, and kinetic studies of mefenamic acid (MA) prodrugs of tyrosine and glycine. The glycine prodrug demonstrated maximum analgesic activity (86%), while both tyrosine and glycine prodrugs showed better anti-inflammatory activity (74% and 81%, respectively) compared to MA alone. Furthermore, both prodrugs exhibited fewer gastric ulcers compared to MA. These findings suggest that the prodrugs are superior to MA in terms of efficacy and gastrointestinal safety.
Paper Details　
Original Abstract of the Article :
This study deals with the synthesis, pharmacological activity, and kinetic studies of mefenamic acid (MA) prodrugs of tyrosine and glycine. The synthesis involved a series of protection and deprotection reactions. The hydrolysis of these prodrugs in the intestine was confirmed by hydrolysis kinetics...See full text at original site
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引用元：
https://doi.org/10.3109/14756360903468163

データ提供：米国国立医学図書館（NLM）

Prodrugs: A Novel Approach to Drug Delivery

Drug delivery is a crucial aspect of therapeutic intervention, and finding ways to enhance drug efficacy and minimize side effects is an ongoing challenge. Prodrugs, inactive compounds that are converted into active drugs in the body, offer a promising approach to improving drug delivery. This research focuses on the development and evaluation of novel prodrug derivatives of mefenamic acid, a nonsteroidal anti-inflammatory drug (NSAID), using tyrosine and glycine as carriers.

Prodrug Design and Evaluation

The researchers synthesized prodrug derivatives of mefenamic acid using tyrosine and glycine. They conducted kinetic studies to assess the hydrolysis of these prodrugs in simulated gastric fluid, simulated intestinal fluid, and plasma. The prodrugs were then evaluated for their analgesic, anti-inflammatory, and ulcerogenic activities. The findings revealed that both tyrosine and glycine prodrugs exhibited enhanced analgesic and anti-inflammatory activity compared to mefenamic acid. Furthermore, they demonstrated a reduced risk of gastric ulcers.

Navigating the Desert of Drug Delivery

This research explores the potential of prodrug derivatives to improve the efficacy and safety of mefenamic acid. It's like navigating a vast desert, searching for a more efficient and safer way to deliver life-saving medications.

Health Implications and Applications

This research suggests that prodrug derivatives of mefenamic acid may offer a more effective and well-tolerated treatment option for pain and inflammation. It's like finding a hidden oasis in the desert, providing a more effective and safe way to deliver pain relief.

Dr. Camel's Conclusion

This research showcases the potential of prodrug derivatives to enhance drug delivery, offering a promising approach to improving therapeutic efficacy and reducing side effects. It's like discovering a hidden oasis in the desert of drug delivery, providing a more efficient and safer path to therapeutic success.
Date :
  1. Date Completed 2011-03-25
  2. Date Revised 2013-11-21
Further Info :

Pubmed ID

20578977

DOI: Digital Object Identifier

10.3109/14756360903468163

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Languages

English

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