38 Questions
Which type of salts are formed from strong acids with strong bases?
Highly dissociable salts
In terms of water solubility, what happens when a salt is formed by a weak acid and a weak base?
It does not dissociate appreciably
What are characteristics of low-molecular weight salts in terms of water solubility?
They are water soluble
How many ionizable functional groups does Tyrosine contain?
3
Which type of group in Tyrosine is ionizable based on the pH of the environment?
Alkylamine and carb acid groups
What is the pKa range for the ionizable phenolic hydroxyl group in Tyrosine?
9-10
Which type of cyclic compound is a lactone?
Cyclic ester
What compound is formed by the reaction between HBr and potassium hydroxide (KOH)?
(KBr) Potassium Bromide
Which type of isomers are formed due to restricted bond rotation of C=C and similar systems like imines?
Geometric isomers
What is the more active isomer of triprolidine, indicating a critical distance between the pyridine and pyrrolidine rings for binding to the receptor?
E-isomer
In the context of diastereomers of 1,2-dimethylcyclohexane, what allows for the possibility of conformational isomers?
Significant conformational freedom
What is the purpose of structure activity relationship (SAR) in drug development?
To analyze a large set of drug analogs and determine patterns leading to stronger interactions
Which type of isomers exhibit significantly different biological activity when the first 2 cyclohexane rings are fused into different configurations?
Steroids
What is the main purpose of developing an activity pattern from a large set of drugs?
To predict the activity of a new drug
What does functional activity at receptors involve?
Recognition or binding between drug and macromolecular receptors
What is the process of modifying functional groups of a lead compound to improve its recognition, affinity, and pharmacokinetic properties?
Lead optimization
How can interactions between drugs and biological systems be modeled?
Using computational chemistry
Where was salicylic acid originally isolated from, leading to its eventual use in treating inflammatory ailments?
Willow trees' bark
Which statement best describes structure activity relationship (SAR)?
A pattern developed by chemists to help explain drug action based on known knowledge
What does the text suggest about the accuracy of models based on current knowledge?
They are subject to limitations and may become inaccurate with new data points
Why is the interaction between drugs and biological systems described as simply recognition or binding?
To highlight the straightforward nature of drug interactions
'All models have limitations' implies that:
'All models' may not accurately represent reality
What is the major pathway for the metabolism of thioesters?
S-dealkylation to hemithioacetals
How is codeine metabolized?
O-demethylation to morphine
What is the result of P450-catalyzed oxidative dehydrohalogenation?
Formation of gem-halohydrin
How does Sevoflurane primarily undergo metabolism?
O-dealkylation to hexafluoroisopropanol
What is the role of azoreductase in liver microsomes?
Reduction of azo compounds to primary amines
What does the oxidative O-dealkylation of ethers resemble in terms of mechanism?
N-alkylation
Which compound is demethylated to yield the anticancer drug 6-mercaptopurine?
$6$-methylthiopurine
What do reactive metabolites like acyl halides and carbonyl halides generated in metabolism reactions do?
React with H2O to form carboxylic acids
Which enzyme is responsible for catalyzing the N-acetylation of arylamines?
N-acetyltransferase (NAT1 and NAT2)
What is the protective mechanism against hepatotoxicity or carcinogenicity that involves detoxifying harmful substances through glutathione conjugation?
Mercapturic acid pathway
Which enzyme catalyzes the conjugation of electrophiles with GSH for excretion in bile and urine, playing a role in detoxification?
Glutathione S-transferase (GST)
In drug metabolism, which process involves the transfer of methyl groups to substrates for their inactivation?
Methylation
Which organ is described as the primary site for drug metabolism and elimination?
Liver
What can age-related changes in elderly individuals lead to concerning drug metabolism?
Impaired drug metabolism
How does pregnancy influence hepatic drug metabolism?
By affecting the activity of specific enzymes like CYP3A4, 2A6, 2D6, and 2C9
What can genetic polymorphisms in drug-metabolizing enzymes lead to?
Differences in drug metabolism rates, affecting drug efficacy and toxicity
Test your knowledge on diastereomeric isomers and the impact of restricted bond rotation on stereoisomerism. Explore concepts such as geometric isomers and the relationship between molecular structure and biological activity.
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