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PHA 051 - MEDICINAL ORG. CHEMISTRY > SAS 2 - PHYSICOCHEMICAL PROPERTIES OF ORGANIC MEDICINAL AGENTS > Flashcards

SAS 2 - PHYSICOCHEMICAL PROPERTIES OF ORGANIC MEDICINAL AGENTS Flashcards

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1
Q

What is physicochemical

A

is the influence of the physical and chemical attributes of a compound or the active drug on its effect

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2
Q

Give 5 properties that influence the physicochemical?

A

solubility
dissociation constant
molar refractivity
ionization
drug shape
complexation
bioisosterism

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3
Q

what are the 3 expressions/ units in solubility?

A

mass of solute per volume of solvent
mass of solute per mass of solvent
moles of solute per volume

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4
Q

give some methods that can modify drug structure in drug design?

A

Use of co-solvents
addition of polar groups (carboxylic acid, ketone, amines)
complexation
surfactants
reduce intrarmolecular forces

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5
Q

provide examples of co-solvents?

A

polyethylene glycol
propylene glycol
ethanol
sorbitol

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6
Q

what is the another word of complexation?

A

chelation

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7
Q

how complexation/chelation occur?

A

though proton donor-accepting process

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8
Q

what is it formally called the proton/acceptor of proton in complexation/chelation?

A

Lewis acid-base reaction

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9
Q

Define intermolecular forces

A

the area between two or more molecules of the same compounds

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10
Q

Define intramolecular forces

A

the area between two atoms of the same compound

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11
Q

Why do intermolecular increases boiling point?

A

due to polymeric aggregate

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12
Q

why do intramolecular decreases boiling point?

A

due to chelation which prevents the formation of intermolecular forces

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13
Q

what increases solubility?

A

increased in hydrogen bonding

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14
Q

complete the sentence: if the anion of acid was stabilized by _________ _______ ___ _______________ ______ it would increase the strength of acid.

A

hydrogen bonding of intramolecular forces

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15
Q

In Spectroscopic properties…hydrogen bonding shifts the position of bands in _________ and _____ spectra of organic compounds

A

infrared and NMR spectra of organic compounds

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16
Q

this is define as the solubility in lipid medium when an aqueous solution is present.

imPARTs

A

Partition coefficient

17
Q

partition coefficient is also define as?

A

Lipophilicity

18
Q

this is define as the measurement of the acid/base strength

A

dissociation constant

19
Q

dissociation constant is also known as?

A

acidity constant/ ionization constant

20
Q

what are the weak acid?

A

Phenobarbital, Pentobarbital, Acetaminophen, Aspirin

21
Q

what are the weak base?

A

Cocaine, Ephedrine, Morphine

22
Q

this allows to measure the strength of a compound at any ph

A

pKa

23
Q

It represents the size and polarizability of a fragment or molecule

A

Molar refractivity

24
Q

The accumulation of an ionized drug in a compartment of the body is known as ___ __________

A

ion trapping

25
Q

the ratio of ionized/unionized drug is determined by ___________-____________ _______________

A

Henderson-Hasselbalch relationship

26
Q

complexation happens through what process?

*lewis

A

Lewis acid-base reaction

27
Q

complexation is limited to 3 atoms, what are these?

A

N,O, S

28
Q

+ antidote for organic arsenical, lewisite
+ treatment for antimony, drug, mercury poisoning

A

Dimercaprol

29
Q

antidote for copper poisoning

A

Penicillamine

30
Q

analog of antibacterial and antifungal agents

A

8-hydroxyquinoline

31
Q

having the SAME number and arrangement of electrons

A

Isosterism

32
Q

having SIMILAR molecular shapes and volumes

A

Bioisosteres

33
Q

Bioisosterism have 2 classifications, what are these?

A

Classical and Non-classical

33
Q

Bioisosterism have 2 classifications, what are these?

A

Classical and Non-classical

34
Q

what are the classical bioiososteres?

A

Fl vs hydrogen replacement
amino-hydroxyl interchanges
thiol-hydroxyl interchanges
fluorine, hydroxyl, amino, and methyl group interchanges

35
Q

applies the Grimm’s law

A

fluorine, hydroxyl, amino, and methyl group interchanges

PHA 051 - MEDICINAL ORG. CHEMISTRY (13 decks)

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