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PDA Test 4 > Lecturw 6 > Flashcards

Lecturw 6 Flashcards

0
Q

SAR for anti microbial acidity

A

Differ from normal SAR
Replacing benzene decease
Adding substitute decrease

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1
Q

Sulfa drugs

A

Mimic and inhibit the biosynthesis of DHF

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2
Q

Anti diabetic activity

A

Increase insulin production

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3
Q

Diuretic activity

A

Increase water excretion

Inhibited ion channels

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4
Q

Paclitaxel activity

A

Replace HBD with HBA will decrease effect

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5
Q

Drug in-likeness

A

Non drugs show up active giving false positives
Bind number of receptors
Self aggression

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6
Q

Larger therapeutic index

A

Greater margin of safety

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7
Q

More life-threatening disease ➡️

A

The lower the acceptable TI

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8
Q

Branched-chain groups

A

less lipophilic, lower potency, bad

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9
Q

Cyclization

A

Does not affect potency but increases lipophilicity and decreases metabolism

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10
Q

Changes from bioisosteric replacements

A

Allows you to tinker with whichever parameters are necessary to increase solubility or reduce toxicity
This includes size, shape, electron distribution, lipid solubility, water solubility, etc

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11
Q

Structural

A

size, shape, H bonding

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12
Q

Receptor interactions

A

Lipid and H2O solubility

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13
Q

Pharmacokinetics

A

Lipophilicity, hydrophilicity, pKa and H bonding

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14
Q

Metabolism

A

Chemical reactivity

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15
Q

Phenylalanine peptidomimetrics

A

Increased lipophilicity and conformational rigidity

Better absorption and poor recognition by proteases

16
Q

Boric acid as a CO2 H bioisostere

A

Non-toxic readily synthesized

Example: bortezomib

17
Q

Boronia acid as a proteasome inhibitor

A

Tighter binding and enhanced bioactivity

18
Q

Circumventing metabolism

A

Prodrug designed to be slowly converted to active drug to prolong plasma levels

19
Q

Esther prodrug

A

Used to protect acid function as a master

PDA Test 4 (8 decks)

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