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Which of the following is an acidic functional group?
Carboxylic acid
Which of the following is a basic functional group?
Alicyclic amine
A drug that contacts at least one acidic and at least one basic functional group is classified as
Amphoteric
Why are salts commonly made for drugs
To enhance solubility in aqueous solutions
Unionized drugs are generally favored for
Penetration across membranes like the BBB
An acidic drug would typically bind to which plasma protein?
Albumin
A lipid-soluble organic salt is typically formulated for
Intramuscular (IM) depot injections
According to the general rule for water solubility based on LogP, a compound with a LogP of +0.5 is considered
Insoluble in water
Which of the following acidic functional groups typically has the lowest pKa?
Sulfate
The basicity of a functional group is generally stronger when
Its pKa is higher
What type of bond is generally considered the strongest in drug-target interactions
Covalent bond
Noncovalent bonds are primarily characterized by their dependence on
pH and the inverse proportionality to the distance between interacting groups
The energy of an ionic bond interaction is inversely proportional to the
Distance between the interacting ions
Which of the following noncovalent bonds has the lowest strength (0.5-1 kcal/mol)
Van der Waals attraction
Wat phenomenon describes the tendency of nonpolar molecules to associate in water, driven by the desire of water molecules to maximize their hydrogen bonding?
Hydrophobic interactions
According to Lipinski’s Rule of Five, for a drug to have good oral bioavailability, its molecular weight should be less than
500
Which of the following is NOT one of Lipinski’s Rule of Five criteria for oral drugs?
High melting point
What is the primary purpose of Structure-Activity Relationships (SARs) studies?
To relate the chemical structure of compounds to their biological activity
When comparing chemical structures to understand their pharmacological activity, what aspects are analyzed?
Their functional groups and how they influence activity
A chiral center is a carbon atom bonded to how many different groups
Four
Which of the following is NOT a possible consequence of drug metabolism on the activity of the drug?
Increased therapeutic window
What is the most important site for drug metabolism in the body?
Liver
Phase I reactions primarily aim to
Enhance drug excretion and prepare for Phase II reactions
Cytochrome P450 enzymes are primarily responsible for which type of Phase I reactions?
Oxidation
The nomenclature CYP1A2 indicates:
CYP is the enzyme, 1 is the family, A is the subfamily, 2 is the individual gene
An oxidation reaction is characterized by either a decrease in hydrogen content or an increase in
Oxygen, nitrogen, or halogen content
Arene oxide intermediates, formed during the oxidation of aromatic rings, are known to be
Electrophilic and chemically reactive
Aromatic hydroxylation reactions proceed most readily in which type of rings?
Activated (electron-rich) rings
Side chain oxidation of alkyl side chains often occurs on which carbons?
The terminal or penultimate carbon
Which of the following is a Phase II (conjugation) reaction?
Glucouronidation