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unit 3 Flashcards

1
Q

The biological activity of a targeted drug molecule is solely dependent on its physicochemical characteristics, essentially the ___ and ____

A
  • NATURE AND TYPE OF FUNCTIONAL MOIETIES
  • SPATIAL ARRANGEMENT
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2
Q

Modulating the structure of a drug implies ___,___,___ of certain groups in the drug.

A

INTRODUCTION
ELIMINATION
SUBSTITUTION

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3
Q

It plays an important role in modifying the biological activities of many compounds.

A

PHYSICOCHEMICAL PROPERTIES

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4
Q

Substances that are present at the same proportional saturation in a given medium have the same degree of biological action

A

FERGUSON PRINCIPLE

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5
Q

According to ___, it is unnecessary neither to define the nature of the biophase or the receptor nor to to measure the concentration of the drug at this site.

A

FERGUSON

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6
Q

If equilibrium conditions exist between the drug in molecular biophase and in extracellular fluids, the tendency to escape from each phase is the same, even though the concentrations in the two phases are different.

A

THERMODYNAMIC ACTIVITY

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7
Q

It is approximately equivalent to the degree of saturation of each phase

A

THERMODYNAMIC ACTIVITY

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8
Q

It is a bond in which a hydrogen atom serves to hold two other atoms together.

A

HYDROGEN BOND

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9
Q

The H-bond is usually formed only between:

A

HYDROGEN AND ELECTRONEGATIVE ATOMS

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10
Q

Most common atoms capable of forming H-bonds

A

FLUORINE
OXYGEN
NITROGEN

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11
Q

Atoms capable of forming H-bonds to a lesser extent:

A

CHLORINE
SULFUR

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12
Q

The compounds that are capable of forming hydrogen bonding are only:

A

SOLUBLE IN WATER

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13
Q

The hydrogen bonds occur within one molecule

A

INTRAMOLECULAR HYDROGEN BONDING

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14
Q

The hydrogen bonds occur between two or more molecules

A

INTERMOLECULAR HYDROGEN BONDING

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15
Q

They are frequently much weaker than the other.

A

INTERMOLECULAR; INTRAMOLECULAR

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16
Q

It would greatly increase its potential for aqueous solubility.

A

MULTIPLE HYDROGEN BONDING GROUPS IN ANY DRUG MOLECULE

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17
Q

It is essential for all the drug molecules to transport to the site of action on a receptor.

A

MINIMAL AQUEOUS SOLUBILITY

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18
Q

H-bond strength of acetic acid dimer in vapour state

A

7.64 kcal/mol

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19
Q

H-bond strength of acetic acid dimer in benzene

A

4.85 kcal/mol

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20
Q

In water, the h-bond strength is:

A

4.5 kcal/mol

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21
Q

In ice, the bond strength is:

A

6 kcal/mol

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22
Q

The physical states of substances, such as water, DNA, protein and various drug molecules are maintained by:

A

HYDROGEN BONDING

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23
Q

The most frequently observed H-bonds in biological systems are between the:

A

HYDROXYL (OH)
AMINO (NH)

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24
Q

No analgesic property
Melting point: 127 degrees C
Insoluble in Water
Slightly soluble in Ether
Forms intermolecular H-bond

A

1-Phenyl-3-methy-5-pyrazolone

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25
Good analgesic agent Melting point: 112 degrees C Soluble in Water Moderately soluble in Ether Does not form intermolecular h-bond
1-Phenyl-2,3-dimethy-5-pyrazolone (antipyrine)
26
Increase in ionization INTENSIFIES A DRUG’s WATER SOLUBILITY and DECREASES ITS LIPOSOLUBILITY
27
Drugs cross cellular membranes in UNDISSOCIATED forms as:
INTACT MOLECULES
28
Drugs cross cellular membranes in DISSOCIATED form as:
IONS
29
Are predominantly of the UNIONIZED form at the LOWER pH of the gastric fluid, and absorbed from the stomach as well as intestine.
WEAKLY ACIDIC DRUGS
30
Some very weak acidic drugs whose pKa are greater than 7 and are unionized at all pH values
PHENYTOIN MANY BARBITURATES
31
They are poorly absorbed in the stomach since they are present largely in the ionized form at low pH
MOST WEAK BASES
32
Those with pKa values between 5 and 11, shows pH dependent absorption.
STRONG BASE
33
This stronger base has a pKa > 11 and are ionized throughout the gastrointestinal tract and tend to be POORLY ABSORBED.
GUANITHIDINE
34
The liposolubility is affected by pH of the environment medium and by the degree of dissociation pKa.
35
The degree of dissociation, pKa, is calculated from the following equation.
HENDERSON-HASSELBALCH EQUATION
36
STRONG ACID - LOW PKA VALUE WEAK ACID - HIGH PKA VALUE
37
STRONG BASE - HIGH PKA VALUE WEAK BASE - LOW PKA VALUE
38
It may be defined as a quantitative expression of the tendency of a compound that has to give or receive electrons.
REDOX POTENTIAL
39
Redox Potential equation
Eh = E10 - 0.06 / n
40
Eh = E10 = n =
- REDOX POTENTIAL OF THE SYSTEM BEING STUDIED - STANDARD POTENTIAL AT GIVEN PH - NUMBER OF ELECTRONS TRANSFERRED
41
It means greater tendency for reduction to occur.
HIGHER EO
42
It means greater tendency for oxidation to occur
LOWER EO
43
The property of the surface of a liquid that allows it to resist an external force, due to the cohesive nature of its molecules.
SURFACE TENSION
44
It is defined as a material that can reduce the surface tension of water. at lower concentrations.
SURFACTANT
45
It may enhance or retard the drug absorption, which depends upon the chemical nature of surfactant, its concentration, its effect on biological membrane, and micelle formation.
SURFACE AGENT
46
At lower concentrations, the surfactants _____
ENHANCE THE ABSORPTION RATE
47
Molecular aggregates which entrap the drug molecule in their hydrophobic core, and result in the retardation of the rate of absorption.
MICELLE
48
Classification of Surface-active agents
ANIONIC SURFACTANTS CATIONIC SURFACTANTS NONIONIC SURFACTANTS AMPHOTERIC SURFACTANTS
49
Examples of Anionic Surfactants
- ORDINARY SOAPS - SALTS OF BILE ACIDS - SALTS OF THE SULPHATE OR PHOSPHATE ESTERS OF ALCOHOLS - SALTS OF SULPHONIC ACID
50
Examples of Cationic Surfactants
- HIGH MOLECULAR WEIGHT ALIPHATIC AMINES - QUATERNARY AMMONIUM DERIVATIVES
51
Examples of Nonionic Surfactants
- POLYETHYLENE ETHERS - GLYCOL ESTERS OF FATTY ACIDS
52
Application of Surface Tension
BACTERICIDAL ACTIVITY ANTHELMINTIC ACTIVITY OF HYDROXY RESORCINOL
53
It results from a donor-acceptor mechanism or Lewis acid-base reaction.
COMPLEXES OR COORDINATION
54
The compounds that are obtained by donating electrons to metal ions with the formation of ring structures.
CHELATES
55
The compounds that are capable of forming a ring structure with metal atoms.
LIGANDS
56
A ligand that has a single basic group capable of bonding to the metal ion and is an UNIDENTATE LIGAND
AMMONIA
57
A ligand having more than one accessible basic binding site
MULTIDENTATE
58
It is a BIDENTATE ligand form, and chelates with Cu (II)
ETHYLENEDIAMINE
59
An antidote that chelates iron in iron poisoning
DEFEROXAMINE
60
Used in treatment of lead poisoning
DIMERCAPROL
61
Used to treat Anemia
VITAMIN B12
62
A naturally-occuring cobalt complex
VITAMIN B12
63
Used in the treatment of Copper and Wilson’s disease
L-PENICILLAMINE
64
Different ways atom can flex or bend
CONFORMATIONAL ISOMERS
65
Different arrangements in the space for atoms or groups in single bonds.
CONFORMATIONS
66
Two ways conformational isomers are presented:
SAWHORSE FORMULA NEWMAN’S PROJECTION FORMULA
67
It shows how the spatial orientation of all C-H bonds is arranged at an angle.
SAWHORSE FORMULA
68
The two carbon atoms are represented by a circle and a carbon-carbon bond is viewed along its axis.
NEWMAN’S PROJECTION FORMULA
69
Line representation towards the center of the circle represents the bonds attached to the FRONT CARBON
NEWMAN’s PROJECTION FORMULA
70
Lines going to the edge of the circle are used to view the bonds attached to the REAR CARBON
NEWMAN’s PROJECTION FORMULA
71
It has a higher energy than the anticonformation (staggered) due to stearic chuchu
GAUCHE CONFORMATION
72
HIGH ENERGY MOLECULE - LEAST STABLE LOW ENERGY MOLECULE - MORE STABLE
73
It has lower energy (the most stable)
ANTICONFORMATION / STAGGERED
74
Energy and Stability is inversely proportional
75
Most stable to least stable
1. STAGGERED CONFORMATION 2. GAUCHE 3. ECLIPSED CONFORMATION 4. ECLIPSED (A)
76
Are configurational isomers which have the ability to rotate plane-polarized light clockwise or counterclockwise.
OPTICAL ISOMERS
77
Categories of Optical Isomers
ENANTIOMERS DIASTEREOMERS
78
Are mirror images, non superimposable
ENANTIOMERS
79
Are a pair of molecules that exist in two forms that are mirror images of one another but cannot be superimposed one upon the other.
ENANTIOMERS
80
non-mirror images, non-superimposable
DIASTEREOMERS
81
Defined as compounds which have the same molecular formula and sequence of bonded elements but which are non-superimposable, non-mirror images
DIASTEREOMERS
82
It is of vital importance to the medicinal chemists because the biological characteristics of isosteres appear to be similar; more frequently than physical or chemical characteristics.
ISOSTERISM
83
It is used to reduce toxicity, change bioavailability, or modify the activity of the lead compound, and may alter the metabolism of the lead.
BIOISOSTERISM
84
Two types of Bioisosteres
CLASSICAL NONCLASSICAL
85
They have similarities in shape and electronic configuration of atoms, groups, and molecules, which they replace.
CLASSICAL BIOISOSTERES
86
They do not obey the steric and electronic definition of classical isosteres. Also, they do not have the same number of atoms as replacements.
NONCLASSICAL BIOISOSTERES

PMOC (3 decks)

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