Essentials Of Foye 39;s Principles Of Medicinal Chemistry Pdf

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Oneof the standout features of this edition is its adept balance between theoretical concepts and practical applications. The authors skillfully guide the reader through the fundamental principles of medicinal chemistry while also providing real-world examples and case studies that demonstrate the relevance of these concepts in drug discovery and development. This blend of theory and application makes the book accessible to both students and professionals in the field.

The book also shines in its coverage of contemporary issues and emerging trends in medicinal chemistry. The authors address recent developments such as personalized medicine, bioinformatics, and green chemistry, reflecting the dynamic nature of the field. This forward-looking approach ensures that the book remains relevant and up-to-date in an ever-evolving field.

Furthermore, the writing style is clear, concise, and engaging, making complex concepts more digestible for readers at various levels of expertise. The inclusion of high-quality figures, tables, and chemical structures further enhances the clarity of the content.

In terms of criticisms, some readers may find the sheer breadth of information overwhelming, especially if they are new to the subject. However, the comprehensive nature of the book ensures that it can serve as a valuable reference for readers at different stages of their academic or professional careers.

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As defined by IUPAC (International Union of Pure and Applied Chemistry) " Medicinal Chemistry is a chemistry-based discipline, also involving aspects of biological, medical and pharmaceutical sciences. It is concerned with the invention, discovery, design, identification and preparation of biologically active compounds, the study of their metabolism, the interpretation of their mode of action at the molecular level and the construction of structure-activity relationships (S.A.R.), the relationships between chemical structure and pharmacological activity for a series of compounds."

In view of this, the first part of the course (general part) aims to provide students with some theoretical concepts of medicinal chemistry, necessary to uderstand the action of drugs. Hints will also be given to the main approaches in the study of the relationships between chemical structure and biological activity.

To this end, the folloowing subjects will be discussed:

- physico-chemical properties of drugs (acid-base behavior, solubility, lipophilicity, electronic effect of substituents, molecular dimensions, reactivity, stereochemistry, drug-receptor interactions)

- some aspects of the methods used in the discovery and the development of new drugs (lead compound identification through random screening, rationale approaches, serendipity and optimization strategy, such as isosteric modification and prodrugs development)

- mechanisms and molecular targets (receptors, enzyme) responsible for the pharmacodynamic behaviour of a drug

- principles regulating the pharmacokinetic of a drug (absorption, distribution, metabolism, elimination and toxicity)

The second part of the course (systematic) aims to provide some application of the principles and methods discussed in the general part and will describe the achievements of pharmaceutical research, dealing with drugs acting on the central and peripheral nervous system and drugs able to counteract inflammatory processes. Starting from the discovery of the lead compound, each class of drugs will be examined by means of structure activity relationschips, physico-chemical properties, pharmacodynamic and pharmacokinetic.

Overall, the course aims to confer characterizing knowledge, essential to cover professional roles in the pharmaceutical and healthcare sectors

The course will address the following topics: 1.Overview: drug definitions; tipe of drugs, small drugs and biological drugs; drugs uses and actions. Historical overview and general aspects about drug discovery and medicinal chemistry development. 2. Main molecular targets and drugs action: ligand-gated ion channels, voltage-gated ion channels, G protein-coupled receptors, nuclear receptors (transcription factors); agonists, antagonits, inverse agonists, affinity, potency, efficacy and dose-response curves. Enzyme inhibitors. 3. Forces involved in drug-receptor interactions: London dispersion force and Van der Waals interactions, hydrophobic interaction, hydrogen bond, charge transfer complex, dipoles and ionic interactions, covalent bonds. Stereoisomers and stereospecific interactions. Conformational isomers, rigid analogs and study of the bioactive conformation. Pharmacophore identification. 4. Physico-chemical properties of drugs: substituent effects (electronic, lipophilic and steric) and measurement methods; Q.S.A.R. hints and equations of Ferguson and Hansch; acid-base properties and Henderson-Hasselbach equation; lipophilicity/hydrophilicity: partition coefficient and distribution coefficient; solvent properties of water, solubility, solubility prediction and rate of dissolution (Noyes-Whitney equation); stereochemistry and specific rotation; molecular hindrance. 5. Physico-chemical properties, pharmaceutical formulation and administration routes. Physico-chemical properties and pharmacokinetic beahavior: gastro-intestinal tract, mechanism of drug absorption and absorption rate (Fick equation and Michaelis-Menten eaquation); capillary permeability in different districts of the body and blood brain barrier; prediction of drug absorption: Lipinski rule, PSA (polar surface area) and "flexibility"; main pharmacokinetic parameters and their determination (AUC, bioavailability, Cmax, Tmax, Css, apparent volume of distribution, clearance, % binding to plasma proteins, T1/2 and duration of drug action). 6. Phase I and phase II methabolic reactions (oxidations, reductions, hydrolysis, conjugations); drugs toxicity. 7. Discovery and structural modification of new drug-candidate: lead compound and lead optimization through functional groups modification. Isosteres and biososteres 8. Prodrugs. 9. Classification of drugs. 10. Drugs affecting cholinergic neurotransmission (muscarinic agonists, antimuscarinic agents, acethylcholinesterase inhibitors, nicotinic antagonists). 11. Local anesthetics. 12. Central analgesics (opioids). 13. Antipyretics and non steroidal anti-inflammatory drugs (paracetamol, COX1/COX2 inhibitors, antigout agents). 14. Corticosteroids. 15. Histamine antagonists and related antiallergic drugs. 16. Drugs affecting dopaminergic neurotransmission (antipsychotics and antiparkinsons). 17. Drugs affecting serotoninergic and adrenergic neurotransmission (antidepressant). 18. Drugs affecting GABAergic neurotransmission (sedatives-hypnotics, anxiolytics, antiseizures, central myorelaxants).

(Please Note: Medicinal Chemistry, by definition, is concerned with the study of the relationships between chemical structure and the biological activity of pharmacologically active compounds (see IUPAC definition). Therefore, to address the content of the course and understand its technical language, it is very important to have acquired the knowledge gained from the study of the General Physiology and related subjects, such as Anatomy and Biochemistry, as well as the knowledge derived from the study of Organic and Inorganic Chemistry.)

D1 (knowledge and understanding): the student will have to show knowledge and understanding of the contents and concepts provided by the course, by answering specific questions, during the written and oral examinations.

D2 (applying knowledge and understanding): the student will have to be able to apply the knowledge and the logic acquired to formulate plausible hypotheses on the pharmacodynamic and pharmacokinetic behavior of specific substances.

D3 (making judgements): the student will have to indicate the most appropriate molecule for therapeutic treatment of a disease, based on knowledge of the relationships between its physico-chemical characteristics, and the pharmacokinetic and pharmacodynamic behavior.

D4 (communication skills): the student will have to show communication skills by formulating clear and comprehensible answers to the questions proposed, using, where necessary, the typical diagrams and the terminology of the mathematical, physical, chemical, biological, pharmacological and medical languages.

D5 (learning skills): the student will have to show learning skills necessary to undertake the study of subjects related to the course itself, and/or advanced ones.

Foye - Lemke - Zito - Roche - Williams: "Essentials of Foye's Principles of Medicinal Chemistry" (In comparison with the integral version, indicated above, It summarizes the most important chemical features of therapeutically relevant chemical classes of drugs. See chapters: 2,3, 5,7, 8, 9, 12, 18, 21, 22)

R. B. Silverman, M. W. Holladay: "The organic chemistry of drug design and drug action". Elsevier

G.L. Patrick: "An Introduction to Medicinal Chemistry", Oxford university press.

C.G. Wermuth: "The Practice of Medicinal Chemistry", Academic Press.

Laurence Brunton, Bruce A. Chabner, Bjrn C. Knollmann:"Goodman & Gilman: The Pharmacological Basis of Therapeutics", Lawrence Brunton.

Bertram G. Katzung e P. Preziosi: "Basic and Clinical Pharmacology", LANGE Basic Science.

University textbooks: General Biology, General and Organic Chemistry, Biological Chemistry, General Physiology, Pharmacology and General Pathology.

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