Benzodiazepine-Based Drug Discovery
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Benzodiazepine-Based Drug Discovery covers benzodiazepines and benzothiazepines, which constitute two pivotal classes of heterocyclic compounds widely used as core structures of medicinal drugs for the treatment of depression, epilepsy, seizures and muscle spasms. 1,4-Benzodiazepine, 1,5-benzodiazepine, and 1,5-benzothiazepine are the most studied groups of benzodiazepines and benzothiazepines because of their outstanding potential biological activities. This book offers a broad range of recent developments and detailed coverage of the synthesis and biological activities of the drugs based on benzodiazepine and benzothiazepine matrixes, and is an ideal reference guide to researchers working in organic and medicinal chemistry. The importance of these privileged pharmacophores is not limited to the treatment of psychotic disorders because minor changes in the structures can generate various biological activities. They represent a wide range of therapeutic functions such as anticonvulsant, antianxiety, anti-depressant, antiviral, anti-HIV, anti-inflammatory, anticoagulant, anti-obesity, endothelin antagonist, cholecystokinin antagonist, and vasopressin receptor antagonist activities.
Key Features
- Presents detailed coverage of chemical structures and practical synthetic methods of benzodiazepines and benzothiazepines in drug discovery
- Compiles detailed in vivo and in vitro biological activity data of 1,4-benzodiazepine- and 1,5-benzodiazepine-based drugs that will help researchers design and develop innovative drugs
- Discusses promising avenues and potential challenges in the development of new benzodiazepines and benzothiazepines in medicinal drug synthesis
Readership
Researchers in organic chemistry both in academic and industrial settings, postgraduates in chemistry and medicinal chemistry
Table of Contents
- Cover Image
- Title Page
- Copyright
- Table of Contents
- Contributors
- Preface
- Acknowledgments
- Chapter 1 An introduction to benzodiazepines and benzothiazepines
- Chapter Outline
- 1.1 Benzodiazepines
- 1.2 Benzothiazepines
- References
- Chapter 2 Structural features of 1,4-benzodiazepines
- Chapter Outline
- 2.1 Introduction
- 2.2 Structural variations of 1,4-benzodiazepines
- 2.3 Conformational studies of 1,4-benzodiazepines
- 2.4 Polarity and charge distribution of 1,4-benzodiazepines
- 2.5 1,4-Benzothiazepines
- 2.6 Conclusion
- References
- Chapter 3 Synthesis of 1,4-benzodiazepines and 1,4-benzothiazepines
- Chapter Outline
- 3.1 Introduction
- 3.2 Synthesis of 1,4-benzodiazepines
- 3.3 Synthesis of fused 1,4-benzodiazepines
- 3.4 Synthesis of 1,4-benzothiazepines
- 3.5 Conclusion and future directions
- References
- Chapter 4 Biological behavior of 1,4-benzodiazepines and 1,4-benzothiazepines
- Chapter Outline
- 4.1 Introduction
- 4.2 Metabolism of 1,4-benzodiazepines and 1,4-benzothiazepines
- 4.3 GABA metabolism and GABA receptors
- 4.4 Mechanism of action of 1,4-benzodiazepines on GABAA receptors
- 4.5 Molecular effects of chronic 1,4-benzodiazepines exposure
- 4.6 Effect of 1,4-benzodiazepines on cholecystokinin receptors
- 4.7 Effect of 1,4-benzodiazepines on opioid receptors
- 4.8 Effect of 1,4-benzothiazepines on cellular receptors
- 4.9 Conclusion
- References
- Chapter 5 Pharmaceutical applications of 1,4-benzodiazepines
- Chapter Outline
- 5.1 Introduction
- 5.2 Short-acting 1,4-benzodiazepines
- 5.3 Intermediate-acting 1,4-benzodiazepines
- 5.4 Long-acting 1,4-benzodiazepines
- References
- Chapter 6 Structural features of 1,5-benzodiazepines and 1,5-benzothiazepines
- Chapter Outline
- 6.1 Introduction
- 6.2 Chemical properties of 1,5-benzodiazepines
- 6.3 Chemical properties of 1,5-benzodiazepinones
- 6.4 Conformational studies of 1,5-benzodiazepines and 1,5-benzodiazepinones
- 6.5 Chemical properties of 1,5-benzothiazepines
- 6.6 Conclusion
- References
- Chapter 7 Synthesis of 1,5-benzodiazepines and 1,5-benzothiazepines
- Chapter Outline
- 7.1 Introduction
- 7.2 Synthesis of 1,5-benzodiazepines
- 7.3 Synthesis of 1,5-benzothiazepines
- 7.4 Future directions
- References
- Chapter 8 Biological behavior of 1,5-benzodiazepines and 1,5-benzothiazepines
- Chapter Outline
- 8.1 Introduction
- 8.2 Interaction of 1,5-benzodiazepines and 1,5-benzothiazepines with cell receptors
- 8.3 Interaction of 1,5-benzodiazepines and 1,5-benzothiazepines with enzymes
- 8.4 Interaction of 1,5-benzodiazepines and 1,5-benzothiazepines with ion channels
- 8.5 Interaction of 1,5-benzodiazepines and 1,5-benzothiazepines with platelets
- 8.6 Conclusion
- References
- Chapter 9 Pharmaceutical applications of 1,5-benzodiazepines
- Chapter Outline
- 9.1 Introduction
- 9.2 Clobazam
- References
- Chapter 10 Pharmaceutical applications of 1,5-benzothiazepines
- Chapter Outline
- 10.1 Introduction
- 10.2 Diltiazem
- 10.3 Clentiazem
- 10.4 Thiazesim
- 10.5 Quetiapine
- 10.6 Clotiapine
- References
- Index
Product details
- No. of pages: 338
- Language: English
- Copyright: © Elsevier 2022
- Published: August 16, 2022
- Imprint: Elsevier
- Paperback ISBN: 9780128245163
- eBook ISBN: 9780323860109
About the Authors
Farzad Zamani
Farzad Zamani obtained his PhD from University of Wollongong (Australia) in 2019 under the supervision of Professor Stephen Pyne and Dr. Christopher Hyland. His research included development of transition metal-catalyzed cyclization reactions and heterocycle synthesis. Currently, he is a JSPS postdoctoral fellow in the group of Professor Takayoshi Suzuki at Osaka University working on investigation of small molecule inhibitors of RNA/epigenetic protein complexes in drug discovery.Farzad Zamani obtained his PhD from University of Wollongong (Australia) in 2019 under the supervision of Professor Stephen Pyne and Dr. Christopher Hyland. His research included development of transition metal-catalyzed cyclization reactions and heterocycle synthesis. Currently, he is a JSPS postdoctoral fellow in the group of Professor Takayoshi Suzuki at Osaka University working on investigation of small molecule inhibitors of RNA/epigenetic protein complexes in drug discovery.
Affiliations and Expertise
JSPS Postdoctoral Fellow, Osaka University, Japan
Esmail Doustkhah
Esmail Doustkhah received his PhD in 2017 in the field of catalysis and organic chemistry. In his PhD, he received several awards and scholarships. Currently, he is a JSPS fellow at NIMS in the group of Professors Y. Yamauchi and Y. Ide. His research areas include silicate nanosheet, mesoporous materials, and titania nanostructures for (photo)(bio)catalysis.
Affiliations and Expertise
JSPS Postdoctoral Fellow, Osaka University, Japan
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