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Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
1,5-Benzothiazepine, a versatile pharmacophore: a review
Jitender B Bariwal1, Kuldip D Upadhyay, Atul T Manvar
1Department of Chemistry, Saurashtra University, Rajkot 360 005, Gujarat, India.
European Journal of Medicinal Chemistry
|July 22, 2008
Summary
This review highlights 1,5-benzodiazepines, versatile scaffolds with significant cardiac and psychotherapeutic activities. Research explores structural modifications for various therapeutic targets, showcasing their pharmacological potential.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Organic Chemistry
Background:
- 1,5-Benzothiazepine and 1,5-benzodiazepine are key seven-membered heterocyclic systems.
- Diltiazem and clentiazem demonstrate the cardiac potential of 1,5-benzothiazepines.
- 1,5-Benzodiazepines are recognized as crucial biologically active scaffolds.
Purpose of the Study:
- To review the pharmacological profile of 1,5-benzodiazepines.
- To detail structural modifications for diverse therapeutic targets.
- To provide a brief description of the targeted biological systems.
Main Methods:
- Literature review of scientific articles.
- Analysis of structural modifications in 1,5-benzodiazepine derivatives.
- Summary of pharmacological activities and target interactions.
Main Results:
- 1,5-Benzodiazepines exhibit significant psychotherapeutic and cardiac activities.
- Structural modifications have been successfully employed to target various biological systems.
- Agents like thiazesim and quetiapine fumarate underscore their psychotropic potential.
Conclusions:
- 1,5-Benzodiazepines represent a privileged scaffold in drug discovery.
- Further exploration of structural modifications can yield novel therapeutic agents.
- This class of compounds holds promise for treating cardiac and central nervous system disorders.
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