Editor: Simone Carradori

Series Title: Medicinal Chemistry Lessons From Nature

Alkaloids and Other Nitrogen-Containing Derivatives

Volume 3

eBook: US $79 Special Offer (PDF + Printed Copy): US $136
Printed Copy: US $96
Library License: US $316
ISBN: 978-981-5123-68-5 (Print)
ISBN: 978-981-5123-67-8 (Online)
Year of Publication: 2023
DOI: 10.2174/97898151236781230301


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 fulfill gaps in current knowledge with updated information from recent years. It serves as a guide for academic and professional researchers and clinicians.


Heteroatoms can be found in a number of naturally occurring substances, active pharmaceutical ingredients as well as excipients, substituting isosterically/bioisosterically carbon atoms. Many nitrogen-containing heterocycles can be considered as privileged scaffolds due to statistics describing as more than 85% of all biologically-active chemical entities are endowed with a heterocycle and that approximately 60% of FDA-approved drugs contain a nitrogen heterocycle in their structure. This volume reflects the pivotal role of nitrogen-containing heterocycles in modern drug design from natural compounds and their utilization in the scaffold-hopping strategy. Moreover, the presence of these heterocycles could provide the improvement of solubility, lipophilicity, polarity and hydrogen bonding capacity to biologically active agents, as well as the optimization of their ADME/Tox properties.

Nitrogen-containing compounds were shown to exhibit a very wide range of biological activities mimicking natural compounds or endogenous metabolites. A large chemical diversity can be obtained by different and innovative synthetic methodologies to expand/explore the available drug-like chemical space and to obtain robust Structure-Activity Relationships (SARs) within the scaffold.


  1. Updated information on natural compounds and their semi-synthetic derivatives;
  2. In-depth analysis of novel findings and promising applications;
  3. Use of organic reactions as a powerful tool in drug discovery to enhance the biological potential or give new chemical and biological properties to the parent molecules;
  4. Investigation of the molecular mechanisms.
Prof. Luisa Mannina Ph.D.
Department of Drug Chemistry and Technology
Sapienza University of Rome
P.le A. Moro 5, 00185 Rome (Italy)