module 2 Flashcards
Focuses on quality aspects of medicines
and aims to ensure fitness for medicinal
products.
Pharmaceutical Chemistry
The study of drugs, and involves drug
development.
* Pharmaceutical chemistry work is usually
done in a laboratory setting.
* Involves cures and remedies for disease,
analytical techniques, pharmacology,
metabolism, quality assurance, and drug
chemistry.
Pharmaceutical Chemistry
Structure-Activity Relationship
Relationship of how structural features of the molecule contribute to or
take away from, the desired biological activity.
Structure-Activity Relationship
Alexander Crum Brown
Thomas Richard Fraser
Many compounds containing tertiary amine groups exhibited activity as
muscle
relaxants when converted to quaternary ammonium compounds.
Molecules with widely differing pharmacologic properties could be converted to
muscle relaxants with properties similar to those of tubocurarine
when
methylated.
– Morphine
– Nicotine
– Atropine
Natural neurotransmitter and activator of muscle contraction
– Discovered by Loewri and Navrati
Acetylcholine
Selectivity of drug action via the concept of a
“magic bullet” by
Ehrlich
“selective toxicity”
by Albert
– how one chemical group can
produce two different biological effects (muscle relaxation and
muscle contraction)
Discovery of acetylcholine
binding of two molecules to receptors on the α-β and
δ-α subunits causes the opening of the channel, subsequent
movement of potassium through the channel is associated with a
graded depolarization causing muscle contraction
Acetylcholine
non-depolarizing competitive antagonist at nicotinic
acetylcholine receptors, causing the relaxation of skeletal muscle.
d-Tubocurarine
Physicochemical Properties
A. Acids and Bases
B. Solubility
C. Drug Polarity
D. Partition coefficient (P)
E. Lipinski’s rule of five
Have a direct effect on absorption, excretion, and compatibility with
other drugs in solution
Acid-Base Properties
