Medicinal chemists around the world have been inspired by nature and have successfully extracted chemicals from plants. Research on enzymatic modifications of naturally occurring compounds has played a critical role in the search for biologically active molecules to treat diseases.
This book set explores compounds of interest to researchers and clinicians. It presents a comprehensive analysis about the medicinal chemistry (drug design, structure-activity relationships, permeability data, cytotoxicity, appropriate statistical procedures, molecular modelling studies) of different compounds. Each chapter brings contributions from known scientists explaining experimental results which can be translated into clinical practice.
Volume 3 presents (1) a brief overview of botanical and pharmacological properties of alkaloids, (2) a summary of the synthesis of natural morphinans and related alkaloids, (3) caffeine-based compounds for the treatment of neurodegenerative disorders, (4) piperine derivatives, (5) noscapine-based anti-cancer agents, (6) biogenic amines and amino acid derivatives as carbonic anhydrase modulators and (7) antimalarial compounds on quinoline scaffolds.
The objective of this book is to fulfil gaps in current knowledge with updated information from recent years. It serves as a guide for academic and professional researchers and clinicians.
This book set explores compounds of interest to researchers and clinicians. It presents a comprehensive analysis about the medicinal chemistry (drug design, structure-activity relationships, permeability data, cytotoxicity, appropriate statistical procedures, molecular modelling studies) of different compounds. Each chapter brings contributions from known scientists explaining experimental results which can be translated into clinical practice.
Volume 3 presents (1) a brief overview of botanical and pharmacological properties of alkaloids, (2) a summary of the synthesis of natural morphinans and related alkaloids, (3) caffeine-based compounds for the treatment of neurodegenerative disorders, (4) piperine derivatives, (5) noscapine-based anti-cancer agents, (6) biogenic amines and amino acid derivatives as carbonic anhydrase modulators and (7) antimalarial compounds on quinoline scaffolds.
The objective of this book is to fulfil gaps in current knowledge with updated information from recent years. It serves as a guide for academic and professional researchers and clinicians.
Table of Contents
Chapter 1 Introduction- Indole Alkaloids
- Tropane Alkaloids
- Pyridine and Piperidine Alkaloids
- Imidazole Alkaloids
- Purine Alkaloids
- Steroidal Alkaloids
- Isoquinoline Alkaloids
- Quinoline Alkaloids
- Phenylalkylamine and Phenylalkylamide Alkaloids
- Concluding Remarks
- Consent for Publication
- Conflict of Interest
- Acknowledgement
- Abbreviations
- References
- Introduction
- Total Synthesis of Morphine
- Different Substitutions on Morphinian Skeleton
- Ring a Substitutions
- Ring C Substitutions
- Ring D Substitutions
- Concluding Remarks
- Consent for Publication
- Conflict of Interest
- Acknowledgement
- References
- Introduction
- Caffeine Activity and Synthesis
- Dual Targeting Mao-B Inhibitors and A2 Receptors Antagonists
(E,E)-8-(4-Phenylbutadien-1-Yl) Derivatives
- Annulated Derivatives
- Phenoxymethyl Derivatives
- Caffeine Derivatives as Mao-B Inhibitors or A2A Receptors Antagonists
- Mao-B Inhibitors
- Benzyloxy, Aryloxy and Alkyloxy Derivatives
- A2A Receptor Antagonists
1,3-Diethyl-7-Methyl-8-Phenoxymethyl Derivatives
- Concluding Remarks
- Conflict of Interest
- Acknowledgement
- Consent of Publication
- References
- Introduction
- Piperine Derivatives: Biological Activities and Structure-Activity Relationships
- Antibacterial Activity Related to Nora Efflux Pump Inhibition
- Anti-Mycobacterial Activity
- Anti-Fungal Activity
- Anti-Viral Activity
- Anti-Protozoal Activity
- Anti-Filarial Activity
- Insecticidal, Acaricidal, and Larvicidal Activity
- Effect on Inflammation-Related Disorders
- Activity on Trpv1 Receptor
- Anti-Vitiligo Activity
- Effect on Cns Disorders (Mao-B, Gaba, Cognition, Neuroinflammation)
- Agonist Activity Against Pparγ
- Anti-Cancer Activity
- Effect on Cyp
- Concluding Remarks
- Consent for Publication
- Conflict of Interest
- Acknowledgement
- References
- Introduction
- Obtaining and Synthetic Aspects of the Noscapine Scaffold
- Mechanism of Action: Interaction of Noscapine and Its Analogs With Tubulin and Microtubules
- Noscapine: Promising Scaffold in the Development of Anti-Cancer Agents
- First Generation: Modifications in the Isoquinoline Ring
- Amino and Hydroxyl Analogs
- Halogenated Analogs
- Aryl and Alkyl Analogs
- Second Generation: Modifications in Benzofuranone Ring
- Alkyl Sulphone Analogs
- Carbonyl Analogs
- Amino and Hydroxy Analogs
- Third Generation: N-Isoquinoline Functionalization
- Aryl and Carbonyl Analogs
- Imidazo[2,1-B]Thiazole-Coupled and Triazole Analogs
- N-Propargyl Noscapine
- Isoquinoline Nucleus Absence
- Conclusion
- Consent of Publication
- Conflict of Interest
- Acknowledgments
- References
- Introduction
- Activation Studies
- Natural and Synthetic Amino Acids and Amines: Profiling on Human Cas
- Modified Amino Acids and Amines: Profiling on Human Cas
- Therapeutic Applications of Hca Activators
- Natural and Synthetic Amino Acids and Amines: Profiling on Pathogenic Cas
- Inhibition Studies
- Amino Acids as Tail
- Amino Acids as Spacers and Building Blocks for Cais
- Concluding Remarks
- Consent for Publication
- Conflict of Interest
- Acknowledgement
- References
- Introduction
- Epidemiological Aspects and Economic Burden
- Natural Products and Anti-Malarial Activity: the Advent of Quinine and Its Derivatives
- Drug Resistance
- Chemical and Synthetic Aspects of the Quinoline Heterocycle
- Recent Advances in Drug Design of Anti-Malarial Compounds: Sar Analysis
- Aminoquinoline Derivatives
- Quinoline Derivatives
- Aminoquinoline Hybrids
- Aminoquinoline Derivatives
- Metal-Complexes and Their Antimalarial Activities
- Mefloquine Derivatives
- Conclusion and Future Outlook
- Consent for Publication
- Conflict of Interest
- Acknowledgement
- References
- Subject Index
Author
- Simone Carradori
