The projection of physical and chemical properties of basic compounds that are to be tested in drug design is fundamental, even before the launch of the synthesis program that leads to the development of a hit, as well as drugs that treat the pathology in question. These properties lead not only to the development of the main constituents, but also to the development of future drugs.
This book begins by specifying the description of drugs, their cycle, their life and the role of chemistry in drug design. It then studies the projection, evaluation and importance of pKa, lipophilicity, the solubility and the polar surface. Then, the core medicinal chemistry concepts (Lipinsky’s rule of five, prodrugs, pharmacophores) are detailed. Finally, the book studies that which concerns the European Pharmacopeia – the industrialist’s bible – its role and the description of the monographs of the active principles.
1. Medicines and Drugs.
2. Importance and Evaluation of the pKa.
3. Importance and Evaluation of Lipophilicity.
4. Importance and Evaluation of Solubility.
5. Importance and Evaluation of the Polar Surface Area (PSA and TPSA).
6. Lipinski’s Rule of Five.
7. Principle of a Prodrug.
9. The European Pharmacopoeia.
Roland Barret is Professor Emeritus and the author of over 70 scientific publications. He previously taught organic chemistry and then medicinal chemistry at the Facultés de Pharmacie in Lyon, France, and then at the University of Science and Technology of Hanoi, Vietnam, and the University of Reims Champagne-Ardenne, France.
Table of Contents
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