ANTIBIOTICS … Consider the three drug structures shown here for the following questions: *** a) Which drug(s) is/are likely categorized as beta-lactam antibiotics? [blank1] *** b) Which drug(s) is/are likely categorized as tetracycline antibiotics? [blank2] *** c) Which drug(s) is/are likely to mimic the normal substrate for the bacterial enzyme transpeptidase? [blank3] *** d) What is the normal substrate for the enzyme transpeptidase? [blank4] *** e) The portion of Drug I above that mimics the normal substrate contains what functional group? [blank5] *** f) Briefly describe a gram(+) bacterial cell wall [blank6] *** g) Briefly describe a gram(-) bacterial cell wall [blank7]

Anticancer drugs vinblastine and vincristine are derived from which plant?

Brazzein, a protein-like sweetener, is heat and pH stable mainly due to …

ANTIFUNGALS … Antifungal drugs exploit the biochemical differences between healthy cells and infected cell. *** a) The “azole” class of antifungal drugs, function by inhibiting the production of what sterol that is unique to fungi? [blank1] *** b) What is the sterol found in normal mammalian cell membranes? [blank2] *** c) Consider the portion of the biosynthesis pathway for a key component of the fungal membrane … What type of enzyme is responsible for this reaction? [blank7] *** d) Name an antifungal “azole” drug discussed in class. [blank3] *** e) What metal element are these drugs attracted to in the active sites of fungal enzymes (hint: and also P450s)? [blank4] *** f)  Consider the portion of the biosynthesis pathway for a key component of the fungal membrane … What type of enzyme is responsible for this reaction?  [blank5] *** g) Would the reaction shown above be classified as a Phase I or Phase II type reaction? [blank6]

Which of the following is not classed as an in vitro test?

Which of the following statements best describes the efficacy of a drug?

ADRENERICS… Consider the structures shown here for the questions below: *** a)  Define the term AGONIST: [blank1] *** b) Define the term ANTAGONIST: [blank2]  *** c) Drug (ii) is called albuterol and is used to treat the respiratory disease known as asthma. Albuterol is an agonist that binds in a similar manner compared to an endogenous neurotransmitter, compound (i.). Name compound (i.) [blank3] *** d)  Drug (iii) is called propranolol and it is an antagonist compared to compound (i.). Briefly describe the pharmacophore common to all three structures (i. ii. and iii.) [blank4] *** e) Briefly, how do the varying structures shown above lead to their agonist or antagonist activity? [blank5] *** f)  Rank the drugs in order from most water soluble to least water soluble: [blank6] Structure (i.) is a “Catecholamine”, where the catechol portion is circled in the figure below. It undergoes metabolism to an inactive compound. *** g) Provide a generic name for an enzyme that could complete this metabolic reaction. [blank7]

Which of the following statements best describes the affinity of a drug?

RULE OF 3s and 5s… Consider the antihistamine drugs Loratadine (Claritin®) and Desloratadine (Clarinex®). Recall Lipinski’s Rule of 5 and answer the following questions… *** a) Does DESLORATADINE meet the requirements for hydrogen bond donor capability?   How many HBD groups are present? [blank1]       *** b) Does DESLORATADINE meet the requirement for hydrogen bond acceptor capability? How many HBA groups are present? [blank2]         *** c) Is the in vivo metabolic conversion of loratadine to desloratadine a Phase I or II rxn? [blank3] *** d) Using the “RULE OF 3s”, complete the table below to predict whether the logP values for the drug DESLORATADINE would be less than, greater than, or equal to 0.     Carbon# =  [blank4] Water# = [blank5] Log P   [blank6]  0  

Given the following log P values, what is the predicted log P value for the disubstituted structure?