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PT I - Med Chem > Drug Discovery > Flashcards

Drug Discovery Flashcards

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1
Q

Digoxin (Lanoxin)

carbohydrate

A

SOURCE:
foxglove (plant)

CHEMICAL CLASS:
steroid glycoside

THERAPEUTIC CLASS:

  • positive inotropic agent
  • treatment of congestive heart failure

MOA:
inhibition of Na+/K+ ATPase pump

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2
Q

Quinidine

stereoisomer of quinine

A

SOURCE:
cinchona (plant)

CHEMICAL CLASS:
quinine alkaloid

THERAPEUTIC CLASS: 
class I anti-arrhythmic agent

MOA:
Na+ channel blocker

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3
Q

Quinine

A

SOURCE:
cinchona (plant)

CHEMICAL CLASS:
quinine alkaloid

THERAPEUTIC CLASS:
antimalarial agent

MOA:
depresses oxygen uptake and carbohydrate metabolism; DNA intercalation

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4
Q

Morphine

A 
SOURCE: 
opium poppy (plant)

CHEMICAL CLASS:
opioid alkaloid

THERAPEUTIC CLASS:
opiate analgesic

MOA:
μ (mu) receptor agonist

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5
Q

Camptothecin

A

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
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6
Q

Lovastatin

A

SOURCE:
Aspergillus terreus & Monascus ruber
(fungus, microorganisms)

CHEMICAL CLASS:
statins

THERAPEUTIC CLASS:
hypolipidemic agent

MOA:
inhibit cholesterol biosynthesis by inhibiting HMG-CoA reductase

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7
Q

Vidarabine

A

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

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8
Q

Levothyroxine (Synthroid)

A

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

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9
Q

Hirudin

Lepirudin: Recombinant hirudin derivatives

A

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

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10
Q

Exedin-4

Exenatide (Byetta): synthetic version of Exedin-4

A

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

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11
Q

Penicillin

A

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)]

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12
Q

Adrucil (5-flurouracil)

A

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

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13
Q

Chlordiazepoxide (Librium)

A

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)

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14
Q

Diazepam (Valium)

A

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

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15
Q

Aspirin (acetylsalicylic acid)

A

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

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16
Q

Prontosil

A 
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)

17
Q

Sulfanilamide

A

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
18
Q

Oseltamivir (Tamiflu)

A

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)
19
Q

Terfenadine

A

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

20
Q

Fexofenadine (Allegra)

A

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

21
Q

Sildenafil citrate (Viagra)

A

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

22
Q

Phenothiazine

class of anti-psychotics

A

SOURCE:
observation of side effects

THERAPEUTIC CLASS:
anti-psychotic

MOA:
antagonist; blocks a number of postsynaptic receptors

23
Q

Zanamivir (Relenza)

A

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)

PT I - Med Chem (4 decks)

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