phc 222 medicinal chemistry-1- part(i) dr. huda al salem lecture (1)
TRANSCRIPT
PHC 222Medicinal Chemistry-1-
Part(I)Dr. Huda Al Salem
Lecture (1)
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.
I- DrugDrug is a pharmacologically active compound which is used to prevent and/or treat diseases
Sources of drugs1 -Natural sources: drugs obtained from plants, marine &
microorganisms such as :
opium shellfish
penicillium fungi
I- Drug
2 -Synthetic sources: by production & screening of structural analogues of the lead compound
such as : procaine(local
anesthetic)
cocaine
I- Drug
Structural analogue
Is a compound having a structure similar to that of another one, but differs from it in respect of a certain component.
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.
I- DrugNomenclature 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
I- Drug
Another example..
-,VRSURS\ ODP LQR- - -QDSKWK\ OR[ \ - -SURSDQRO
Propranolol
Inderal
I- DrugClassification 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, - b blocker….etc
II-Receptor
II-Receptor
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,
CarbohydratesOr Nucleic acids
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
II-Receptor
The receptor binds to a specific molecule (ligand) and initiates the cellular response to this molecule.
Role of Receptor
II-Receptor
L R+ L-R Complex
Biological Response
LigandIs a specific molecule that forms a complex with the receptor to give a biological response