Download 52 MCQs on Medicinal Chemistry and Drug Design | MEDC 310 and more Exams Health sciences in PDF only on Docsity!
Medicinal Chemistry and Drug Design
MEDC 310
First Hour Exam
February 21, 2007
Name:____________________________ Pledge: _______________________
(All questions are 2.25 points unless otherwise stated.)
G.E. Kellogg
- What is the most logical and molecular approach to drug discovery?
A) Synthetic and Biophysical Organic Chemistry. B) Structure Based Drug Design. C) QSAR. D) High Throughput Screening (finding a needle in a hay stack). E) Isosteric Replacement.
- QSAR is an abbreviation for:
A) Quality Structure Analysis for Receptors B) Quiet Structure Analysis by Researchers C) Quantitative Structure-Activity Relationships D) Quick Structure Analysis Reasoning E) None of the above.
- Grimm’s Hydride Displacement Law states that a CH 3 can be replaced with an NH in a molecule without a change in structure:
TRUE FALSE
- Linus Pauling described the two main folds of proteins. They are:
A) μ-spiral and β-cone B) α-box and ε-zigzag C) α-helix and β-sheet D) π-sphere and β-helix E) α-sheet and β-helix
Y.A. Zhang
- Which one of the following comments is NOT correct?
A) The basic structural component of membrane system is phospholipid molecules and their chemical structure decides the character of the membrane architecture. B) While some drugs can pass through the membrane by passive diffusion, others may be carried into the cells by carrier protein via active transport. Both processes need energy compensation. C) After absorption some drug molecules may act on the target protein while others may be metabolized even before reaching the site of action. D) After being absorbed, some drug molecules will bind to plasma proteins non-specifically and will not be available for pharmaco-logical activity until they are released.
- The compound shown below is Indomethacin and it is a typical non-steroidal anti-inflammatory drug. Its pKa would be in the range of:
N
CH 2 COOH
CH 3
H 3 CO
O
Cl
Indomethacin
A) 0 - 2 D) 10 - 12 B) 2 - 4 E) > 14 C) 7 - 9
- In which part of the GI tract will indomethacin be best absorbed (the answer of Question 6 should be used to determine the correct answer for this question)?
A) Mouth (pH 6-7) D) Colon (pH 8) B) Stomach (pH 1-3) E) Not absorbed if given orally C) Small Intestine (pH 7-7.5)
- The amount of neurotransmitter in the synapse is regulated by one of several mechanisms. Which one of the following is not directly involved in this action:
A) transporter B) signal transduction C) somatodendritic (cell body) autoreceptors D) terminal autoreceptors
- Several types of agents can activate (or enhance the actions of) a postsynaptic neuron. Which of the following would not be included among these:
A) an agonist B) a releasing agent C) an indirect agonist D) a negative allosteric modulator E) a positive allosteric modulator
14-15. Receptors can be grouped into two major superfamilies: G-protein coupled receptors and ligand-gated ion channel (LGIC) receptors. Whereas the former are composed of seven transmembrane-spanning helicies made up of various amino acid residues, the latter are quite different. For example, LGIC nicotinic acetylcholinergic receptors and 5-HT3 serotonin receptor consists of (14) _________ subunit(s), each consisting of (15) _______ transmembrane- spaning helicie(s). Complete the last sentence by selecting answers from the list below:
A) one D) four B) two E) five C) three
- The neurotransmitter dopamine (DA) binds at five different populations of receptors (i.e., D1-D5). All five of these receptor types are classified as:
A) G-protein coupled receptors B) ligand-gated ion channel receptors
- Which of the following classes of agents does not include examples of antipsychotics:
A) benzodiazepines C) phenothiazines B) butyrophenones D) thioxanthenes
- Which of the following effects is common to most 6-6-6 tricyclic antipsychotics?
A) Anticholinergic activity B) Antihistaminic activity C) Extrapyramidal stimulation D) Answers A), B) and C) are correct E) Answers A) and B), but not C) is correct.
- For optimal antipsychotic activity among the 6-6-6 tricyclic antipsychotics, agents should possess all of the following features except for:
A) an electron donating group at the ring 2-position B) a three atom chain separating the ring from the terminal amine C) a basic tertiary amine D) ability to interact with dopamine receptors
- Long-acting repository forms (i.e., prodrugs) of antipsychotics (such as those discussed in class) take advantage of a chemical reaction that occurs in vivo to result in formation of an active form of the drug. This chemical reaction is best described as:
A) alkylation D) esterification B) acylation E) aminolysis C) hydrolysis
- Parkinson’s disease and the side effects associated with antipsychotic therapy involve:
A) lack of dopamine in functionally important synapses in the brain B) excess dopamine in functionally important synapses in the brain C) lack of serotonin in functionally important synapses in the brain D) excess serotonin in functionally important synapses in the brain
- Amphetamine produces its central stimulant effects primarily by:
A) blockade of dopamine reuptake B) blockade of postsynaptic dopamine receptors C) release of presynaptic dopamine D) interaction with somatodendritic receptors on DA neurons E) interaction with terminal autoreceptors of DA neurons
R. Young
- Identify the compound that is known as “XTC” (“Ecstasy”).
A) MDMA B) Methylenedioxymethamphetamine C) Cathinone D) DOM E) A) and B)
- Only rats and mice have been used as subjects in drug discrimination studies.
TRUE FALSE
- Which statement(s) is(are) false?
A) The drug discrimination procedure provides only quantitative information about a compound. B) Only stimulants and hallucinogens have been used in drug discrimination studies. C) Results from some drug discrimination studies have been shown to parallel(correlate) with human studies. D) A) and B) only E) All of the above.
- With respect to drug discrimination studies of DOM, which statement(s) is(are) true?
A) DOM can function as a discriminative stimulus B) R(-)-DOM is less potent than S(+)-DOM C) DOM generalization occurs to amphetamine D) All of these E) A) and B) only
- (-)-Cathinone is also known as
A) “natural amphetamine” B) “STP” C) “Khat” D) A) and C) E) None of these
- The process of teaching an organism to press a lever is called
A) Discrimination B) Antagonism C) Stereoselectivity D) Shaping E) None of these
B.E. Windle
- For modern scientific methods described in class, which one of the following steps is the biggest limitation?
A) Developing a hypothesis B) Designing an experiment C) Collecting large amounts of data D) Making conclusions from experiments E). Analyzing large amounts of data
- What's the first step in modern scientific methods described in class?
A) Developing a hypothesis B) Designing an experiment C) Collecting large amounts of data D) Making conclusions from experiments E) Analyzing large amounts of data
- For which one of the following tasks is Cluster Analysis best used?
A) Collecting data B) Developing a hypothesis C) Developing a model D) Testing a hypothesis E) Making conclusions
- Which of the following is NOT a way that a genetic difference can affect the response of a patient to a drug?
A) Transport of the drug B) Metabolism of the drug C) drug mutates cellular DNA D) Interaction with the drug target
- Plasma concentrations of a drug as a function of time following intravenous administration of 200 mg can be described by the equation C=10 mg/L e-0.173t^. The volume of distribution and clearance of this drug are:
A) V = 0.5 L; CL = 0.09 L/h B) V = 20 L; CL = 3.46 L/h C) V = 10 L; CL = 0.173 L/h D) V = 10 L; CL = 1.73 L/h
- The half-life (t (^) ½ ) of a drug is:
A) The time it takes for AUC to increase by ½. B) The time it takes for AUC to decrease by ½. C) The time it takes for the elimination rate constant to decrease by ½. D) The time it takes for drug concentrations to decrease by ½.
- Which of the following statements is correct?
A) Volume of distribution is how much of a drug is administered intravenously B) Bioavailability is approximately 80% after intravenous administration of a drug C) Lipophilic drugs are usually eliminated by metabolism D) Renal clearance involves Phase I enzymes
W.H. Soine
- Which of the following statement(s) describe a “designer” drug?
A) It is often a structural modification of a controlled or regulated drug. B) It is usually not illegal. C) It may retain pharmacological activity similar to the regulated drug. D) The toxicity and doses are usually unknown. E) All of the above.
- Problem(s) associated with clandestinely prepared drugs include:
A) Unknown or unanticipated pharmacological effects. B) Difficulty formulating the drug at the appropriate dose. C) Small difference between therapeutic effect and toxicity. D) Drug may be impure. E) All of the above.
- Drug impurities associated with clandestinely prepared drugs include:
A) Feces in marihuana B) Cyanide in phencyclidine C) Mercury in methamphetamine D) Quinidine instead of quinine to “cut” heroin E) All of the above
- If the therapeutic index of a designer drug based on a common drug increases from 2 to 20 this means:
A) The designer drug is safer. B) Toxic effects from the common drug is less likely. C) There is a small difference between therapeutic effect and toxicity for the designer drug compared with the common drug. D) There is no difference between therapeutic effect and toxicity for the designer drug compared with the common drug. E) None of the above.
- When MPTP was found in samples of MPPP (a meperidine or Demerol analog) an unanticipated problem that developed in young people that used the drug was:
A) Heroin addition B) Overdoses due to an increase in activity C) Food poisoning D) Parkinson’s disease E) Stroke and cardiac arrest
- Dragon’s Blood, which was being sold on the streets of Virginia as “red heroin” is an example of:
A) A material with unknown or unanticipated pharmacological effects. B) A new compound that will soon replace heroin on the “street”. C) A highly toxic drug. D) An extremely pure form of heroin. E) All of the above.
