2H/4H-Chromenes-A Versatile Biologically Attractive Scaffold.
1School of Chemical Engineering, Yeungnam University, Gyeongsan-si, South Korea.
Frontiers in Chemistry
|August 28, 2020
Summary
2H/4H-chromene (2H/4H-ch) derivatives are versatile heterocyclic compounds with diverse biological activities and mild side effects. This review details their synthesis, mechanisms, and structure-activity relationships (SAR) for drug development.
Area of Science:
- Medicinal Chemistry
- Organic Synthesis
- Pharmacology
Background:
- 2H/4H-chromene (2H/4H-ch) represents a significant class of heterocyclic compounds.
- These compounds possess a simple structure and exhibit a favorable safety profile with mild adverse effects.
- A variety of 2H/4H-ch analogs have been synthesized, demonstrating diverse biological activities through multiple mechanisms.
Purpose of the Study:
- To review diverse synthetic strategies and mechanisms for 2H/4H-chromene derivatives.
- To highlight the various biological profiles and structure-activity relationships (SAR) of bioactive 2H/4H-ch compounds.
- To provide a comprehensive resource for researchers in designing novel 2H/4H-ch analogs.
Main Methods:
- Literature review of synthetic routes for 2H/4H-chromene analogs.
- Analysis of reported biological activities and their underlying mechanisms.
- Compilation of structure-activity relationship (SAR) data for 2H/4H-chromene derivatives.
Main Results:
- Multiple synthetic pathways for 2H/4H-chromene derivatives have been identified.
- 2H/4H-chromene compounds exhibit a broad spectrum of biological activities, including anticancer, anticonvulsant, antimicrobial, anticholinesterase, antituberculosis, and antidiabetic effects.
- Direct assessment of parent 2H/4H-ch derivatives facilitates orderly SAR analysis.
Conclusions:
- 2H/4H-chromene scaffolds are promising for developing new therapeutic agents.
- Understanding synthetic strategies and SAR is crucial for optimizing the biological activity of 2H/4H-ch analogs.
- This review serves as a valuable guide for the scientific community in advancing 2H/4H-ch based drug discovery.
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