ANTIFUNGALS … Antifungal drugs exploit the biochemical diffe…
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]
Read DetailsADRENERICS… Consider the structures shown here for the que…
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]
Read DetailsRULE OF 3s and 5s… Consider the antihistamine drugs Lorata…
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
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