ORGANIC MEDICINAL CHEMISTRY Flashcards
(50 cards)
- Practice of medicinal chemistry devoted to the discovery of drugs and development of new drugs
ORGANIC MEDICINAL CHEMISTRY
Food Drug and Cosmetic Act R.A#
RA 3720
- A relatively small region of a macromolecule w/c may be: Isolatable enzyme, Structural or functional component of cell membrane, Specific intracellular substances (w/c a drug binds to produce a physiologic response)
RECEPTOR
Selection of structure components, the steric, electronic, & solubility characteristics of a drug w/c makes it interchangeable w/ drugs of the same pharmacologic class
ISOSTERISM
Grp of cmpds or atoms having the same # and arrangement of electrons
ISOSTERES
“Biotransformation”
DRUG METABOLISM
Advantages of PRODRUGS
- Mask bitterness
- Incr. absorption of drug leading to higher plasma conc.
Cmpds that are inactive in native form but easily metabolized to the active agent
PRODRUGS
Paracetamol toxic from
NAPQI
N-acetyl-Pbenzoquinone
PHASE 1 OF METABOLISM
FUNCTIONALIZATION
Involves oxidation, reduction and hydrolysis
FUNCTIONALIZATION
Most common & important in drug metabolism
OXIDATION
Enzyme that adds O2 to the substrae
Cytochrome P450
Most dominant isoform of Cytochrome P450
Cyp3A4
Isoform of enzyme Cytochrome P450 that is for metabolism of antidepressant drugs
Cyp2D6
SUSCEPTIBILITY RULE
Esters > Thioesters > Carbonyls > Amide > Carbamate > Ureide
PHASE 2 OF METABOLISM
CONJUGATION
Attachment of small polar endogenous molecules such as glucuronic acid, sulfate and amino acids & etc. to the Phase 1 metabolites or parent drugs
CONJUGATION
Main enzyme responsible for attaching polar endogenous molecule to the Phase 1 metabolites
TRANSFERASES
Most common conjugation pathway
GLUCORONIDATION
Enzyme for GLUCORONIDATION
UDP-Glucoronosyltransferase
Enzyme that is underdeveloped in neonates that cx Gray-baby syndrome
UDP - Glucuronosyltransferase
Cofactor of UDP - Glucuronosyltransferase
Glucoronic acid
Enzyme for SULFATION
Sulfotransferase
