17949 - General Medicinal Chemistry

Academic Year 2008/2009

  • Docente: Rita Gatti
  • Credits: 4
  • SSD: CHIM/08
  • Language: Italian
  • Teaching Mode: Traditional lectures
  • Campus: Bologna
  • Corso: First cycle degree programme (L) in Herbal Medicine (cod. 0036)

Learning outcomes

Aim of the course is to give the student a basic knowledge in medicinal chemistry focusing in particular on mechanisms of action at molecular level and properties involved in stability and metabolism of natural products.

Course contents

Drugs classification: chemical structure and pharmacological action. Natural, synthetic and semisynthetic drugs. New drugs discovery. Serendipity, clinic observation, random screening, combinatorial chemistry, lead discovery. Clinical trials. Principles of drug pharmacokinetics: drug absorption, drug distribution. Drug metabolism: phase I and phase II reactions. Drugs interactions. Functional groups' metabolism. Conjugation phase: glucuronic conjugation, acylic conjugation, sulphate conjugation, glutation conjugation, methylation. Prodrugs. Drug excretion: renal, biliary and pulmonary excretion. Drug target interactions: description of different chemical bonds involved. Influence of steric factors on drugs' activities: optical, geometric and conformational isomery. Isosterism and bioisosterism. Biological macromolecules as drug target. Proteins, enzymes, ionic pumps, carriers, ionic channels, membrane and intracellular receptors. Enzymatic inhibition: competitive and non-competitive inhibition. Antimetabolites. Suicide inhibitors. Transition-state analogues. Examples. Receptors and drugs. Drugs acting on cholinergic system. Enzymes and drugs. Drugs acting on acetylcholinesterase. Ionic pumps and drugs. Digitalis and Na/K pump. Phytoestrogens.

Readings/Bibliography

L.P. GRAHAM, Chimica Farmaceutica Ed. italiana, Edises, 2004.

W.O. FOYE, T.L. LEMKE, D.A. WILLIAMS, Principi di Chimica Farmaceutica, Piccin Ed. 1998.

C. MELCHIORRE, A. MINARINI, M. RECANATINI, V. TUMIATTI, M.L. BOLOGNESI- I recettori colinergici - CLUEB, Bologna, 1997.

C. MELCHIORRE - I recettori dei neurotrasmettitori. Un'introduzione per la chimica farmaceutica - CLUEB, Bologna, 1996.

Appunti dalle lezioni.

Teaching methods

28 hours of  theoric lectures (period: March - May)

Assessment methods

In order to pass this exam it will be required orally the knowledge of at least three main subjects reported in the program.

Teaching tools

All the teaching program will be explained by PC power point presentation.

Office hours

See the website of Rita Gatti