Drug Discovery Flashcards
(23 cards)
Digoxin (Lanoxin)
carbohydrate
SOURCE:
foxglove (plant)
CHEMICAL CLASS:
steroid glycoside
THERAPEUTIC CLASS:
- positive inotropic agent
- treatment of congestive heart failure
MOA:
inhibition of Na+/K+ ATPase pump
Quinidine
stereoisomer of quinine
SOURCE:
cinchona (plant)
CHEMICAL CLASS:
quinine alkaloid
THERAPEUTIC CLASS: class I anti-arrhythmic agent
MOA:
Na+ channel blocker
Quinine
SOURCE:
cinchona (plant)
CHEMICAL CLASS:
quinine alkaloid
THERAPEUTIC CLASS:
antimalarial agent
MOA:
depresses oxygen uptake and carbohydrate metabolism; DNA intercalation
Morphine
SOURCE: opium poppy (plant)
CHEMICAL CLASS:
opioid alkaloid
THERAPEUTIC CLASS:
opiate analgesic
MOA:
μ (mu) receptor agonist
Camptothecin
SOURCE:
camptotheca/happy tree bark and stem (plant)
CHEMICAL CLASS:
quinoline alkaloid
THERAPEUTIC CLASS:
anti-cancer (lung, ovarian, & cervical)
MOA:
- DNA topoisomerase inhibitor
- prevents replication of DNA (by preventing DNA unwinding) and halts cell growth
Lovastatin
SOURCE:
Aspergillus terreus & Monascus ruber
(fungus, microorganisms)
CHEMICAL CLASS:
statins
THERAPEUTIC CLASS:
hypolipidemic agent
MOA:
inhibit cholesterol biosynthesis by inhibiting HMG-CoA reductase
Vidarabine
SOURCE:
Caribbean sponge Tethya crypta containing arabinoside sugar (marine organisms)
CHEMICAL CLASS:
adenine nucleoside
THERAPEUTIC CLASS:
anti-viral
MOA:
antimetabolite; acts as a substrate and inhibitor of DNA polymerase
Levothyroxine (Synthroid)
SOURCE:
biochemical (based on mammalian biochemical pathways)
CHEMICAL CLASS: amino acid (tyrosine) derivative
THERAPEUTIC CLASS:
thyroid hormone replacement (hypothyroidism, goiter)
MOA:
agonist of thyroid receptors, mimics action of thyroid hormone
Hirudin
Lepirudin: Recombinant hirudin derivatives
SOURCE:
saliva of medicinal leeches (animal)
CHEMICAL CLASS:
65-amino acid polypeptide
THERAPEUTIC CLASS:
anti-coagulant
MOA:
thrombin inhibitor used to treat risk of blood clotting
Exedin-4
Exenatide (Byetta): synthetic version of Exedin-4
SOURCE:
saliva of Gila monster (animal)
CHEMICAL CLASS:
39-amino acid polypeptide
THERAPEUTIC CLASS:
anti-diabetic agent
MOA:
-Exedin-4 stimulates insulin release resulting in a decrease in plasma glucose conc.
-Edenatide has structural similarity with glucagon-like-protein 1 (GLP-1); increases insulin secretion
Penicillin
SOURCE:
fungus “Penicillium notatum” (microorganism) (accidental discovery - no lead molecule)
CHEMICAL CLASS:
beta-lactam
THERAPEUTIC CLASS:
antibacterial agent
MOA:
inhibits bacterial cell wall synthesis by inhibiting penicillin-binding proteins [PBP: important in bacterial cell wall formation and remodeling by transpeptidation (cross-linking)]
Adrucil (5-flurouracil)
SOURCE:
biochemical (based on mammalian biochemical pathways)
CHEMICAL CLASS:
fluorinated pyrimidine
THERAPEUTIC CLASS:
anti-cancer (colorectal and pancreatic)
MOA:
inhibits thymidylate synthase from converting dUMP to dTMP
Chlordiazepoxide (Librium)
SOURCE:
synthesized from a series of quinazoline N-oxides (accidental discovery - no lead molecule)
CHEMICAL CLASS:
benzodiazepine (first cmpd in benzodiazepine class)
THERAPEUTIC CLASS:
anti-anxiety agent
MOA:
GABA(a) receptor agonist; potentiates neuronal inhibitory actions of GABA (inhibitory NT in brain)
Diazepam (Valium)
SOURCE:
structural modification of chlordiazepoxide (3 to 10-fold more potent than chlordiazepoxide)
CHEMICAL CLASS:
benzodiazepine
THERAPEUTIC CLASS:
anti-anxiety agent
MOA:
GABA(a) receptor agonist; potentiates neuronal inhibitory actions of GABA
Aspirin (acetylsalicylic acid)
SOURCE:
salicylic acid derivative (based on a natural product)
CHEMICAL CLASS:
aromatic carboxylic acid
THERAPEUTIC CLASS: relieves pain -minor aches & mild to moderate pain -arthritis & related arthritic conditions -reduces the risk of transient ischemic attacks -myocardial infarction prophylaxis -platelet aggregation inhibitor *dose differs for each therapeutic use
MOA:
inhibits cyclooxygenase [COX: converts arachidonic acid to PGG(2)] by acetylating Ser-530 of COX-1 and Ser-516 of COX-2
Prontosil
SOURCE: random screening (red dye: protonsil rubrum, azo dye)
CHEMICAL CLASS:
sulfanilamides
THERAPEUTIC CLASS:
active in vivo against streptococcal infections
*not active in vitro (mice)
MOA:
metabolically converted to sulfanilamide (reduction)
Sulfanilamide
SOURCE:
drug metabolism studies (reductive liver metabolism of prontosil)
CHEMICAL CLASS:
sulfanilamide
THERAPEUTIC CLASS:
antibacterial
MOA:
- inhibit dihydropteroate synthase, an enzyme needed for biosynthesis of folic acid (bacteria synthesize their own)
- competes with PABA at active site
Oseltamivir (Tamiflu)
SOURCE:
rational drug design (computer aided drug design)
CHEMICAL CLASS:
cyclohexene-1-carboxylic acid/ethyl ester
THERAPEUTIC CLASS:
- anti-viral agent
- prophylaxis and treatment of seasonal and non-seasonal influenza
- prodrug; absorbed orally
MOA: neuraminidase inhibitor (NA: found in influenza virus that cleaves glycosidic bonds between terminal sailic acid residues and adjacent sugars)
Terfenadine
SOURCE:
drug metabolism studies
CHEMICAL CLASS:
diphenylmethanes
THERAPEUTIC CLASS:
- anti-histamine
- associated with cardiac arrhythmias
MOA:
H1-blocker; competes with histamine for binding at H1-receptor sites in GI tract, uterus, large blood vessels, and bronchial muscle
Fexofenadine (Allegra)
SOURCE:
drug metabolism studies
CHEMICAL CLASS:
- carboxylic acid metabolite of terfenadine
- diphenylmethanes
THERAPEUTIC CLASS:
anti-histamine
(no anti-arrhythmic side effects)
MOA:
H1-blocker; competes with free histamine for binding at H1-receptors in the GI tract, large blood vessels, and bronchial smooth muscle
Sildenafil citrate (Viagra)
SOURCE:
observation of side effects
CHEMICAL CLASS:
pyazolo-pyrimidine
THERAPEUTIC CLASS:
erectile dysfunction and pulmonary arterial hypertension
MOA:
inhibition of phosphodiesterase 5 (PDE 5: breaks cGMP to GMP, increase extracellular cGMP thereby enhancing VSM relaxation and vasodilation) resulting in smooth muscle relaxation
Phenothiazine
class of anti-psychotics
SOURCE:
observation of side effects
THERAPEUTIC CLASS:
anti-psychotic
MOA:
antagonist; blocks a number of postsynaptic receptors
Zanamivir (Relenza)
SOURCE:
rational drug design (computer aided drug design)
CHEMICAL CLASS:
cyclohexene-1-carboxylic acid/ethyl ester
THERAPEUTIC CLASS:
- anti-viral agent
- prophylaxis and treatment of seasonal and non-seasonal influenza
MOA:
neuraminidase inhibitor
(NA: found in influenza virus that cleaves glycosidic bonds between terminal sailic acid residues and adjacent sugars)
