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

Match the substances on the right to the things they are obtained from, listed on the left.

Which of the following reflects the order in which various stages of the drug discovery and development take place?

Natural products are often used as lead compounds in the design and synthesis of novel drugs. Which of the following general characteristics of a natural product is most likely to be a disadvantage in synthesising analogues?

According to ‘Lipinski’s Rule of 5’, a compound intended for oral administration should have a molecular weight less than: [blank1]

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]

logP questions

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

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]

Pharmacist’s Guide to Herbals…