1. PHC 222 Medicinal Chemistry-1- Part(I) Dr. Huda Al Salem Lecture (1)

2. Basic Medicinal Chemistry Terminology You are going to study the following: 1- Drug: definition, sources, Meaning of SAR, Nomenclature & classification 2- Receptor: definition, sources & types 3- Drug-Receptor Interaction: examples, affinity, efficacy, agonist, antagonist & pharmacophore.

4. I- Drug Drug is a pharmacologically active compound which is used to prevent and/or treat diseases Sources of drugs 1- Natural sources: drugs obtained from plants, marine & microorganisms such as: opium shellfish penicillium fungi

5. I- Drug 2- Synthetic sources: by production & screening of structural analogues of the lead compound such as: procaine(local anesthetic) cocaine

6. I- Drug Lead compound Is a pharmacologically active compound whose chemical structure is used as a starting point for chemical modifications. Structure-Activity Relationship (SAR) Is the relationship between the structure of a particular compound or a group of compounds and its (their) biological activity.

7. I- Drug Nomenclature of drugs 1- Chemical name: It represents the exact chemical structure of the drug 2- Generic name: the name which is chosen by official agencies e.g. WHO 3-Trade name: the name that is given by the manufacturer(company) Paracetamol Panadol, Adole N-(P-hydroxyphenyl) acetamide

8. I- Drug Another example.. Propranolol Inderal

9. I- Drug Classification of drugs 1- Pharmacological action: analgesic, antihypertensive 2- Target system: adrenergic, cholinergic…etc 3-Chemical structure: penicillins, alkaloids…etc 4- Mechanism of action at molecular level: Anticholinestrases,  blocker….etc

10. II-Receptor

11. Receptor is an integral biological macromolecule embedded in the biological system. Sites of receptor could be.. Cell membrane, cytoplasm or cell nucleus. Components of receptor could be.. Lipids, Proteins, Carbohydrates Or Nucleic acids

12. II-Receptor Types of receptors: 1.Structural and functional component of a cell membrane which consists of lipoprotein e.g. Ion channels. 2.Enzymes e.g. Acetylcholeinestrase & carbonic anhydrase 3.Non enzymatic protein receptors.. e. g. Adrenergic receptors 4.Receptors of nucleic acid e.g. DNA & RNA

13. II-Receptor The receptor binds to a specific molecule (ligand) and initiates the cellular response to this molecule. Role of Receptor

14. II-Receptor Ligand Is a specific molecule that forms a complex with the receptor to give a biological response