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Bioisosterism in Drug Discovery and Development - An Overview
B S Jayashree1, P Sai Nikhil1, Soumyajeet Paul1
1Department of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka-576104, India.
Medicinal Chemistry (Shariqah (United Arab Emirates))
|January 28, 2022
Summary
Bioisosterism is a key strategy in drug discovery for creating safer and more effective medicines. This medicinal chemistry approach optimizes drug properties and enhances therapeutic outcomes.
Area of Science:
- Medicinal Chemistry
- Drug Discovery and Development
Background:
- Bioisosterism is a vital tool for modifying lead compounds.
- It aims to improve drug safety, efficacy, and economic viability.
Purpose of the Study:
- To highlight the significance of bioisosterism in drug discovery.
- To showcase its application in developing diverse drug classes and enzyme inhibitors.
Main Methods:
- Review of literature on bioisosterism in drug design.
- Analysis of its role in optimizing pharmacokinetic profiles and target selectivity.
Main Results:
- Bioisosterism is crucial for enhancing desired activity and reducing undesirable properties.
- Successfully applied across numerous drug classes including antibacterials, antivirals, and anticancer agents.
- Demonstrated efficacy in inhibiting key enzymes like thymidylate synthase and DNA polymerase.
Conclusions:
- Bioisosterism is an indispensable strategy in medicinal chemistry for rational drug design.
- Its application is versatile, with no apparent limitations across drug classes.
- Continues to be a cornerstone for developing improved therapeutics.
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