Quiz 2

What are the 2 types of optical isomers?

______ isomers are a result of the rotation around single bonds between two atoms

Which form of DES is more active- trans DES or cis DES?

______ are mirror images and a plane of symmetry may exist.

Which enantiomer is primarily used in nature to synthesize proteins (D or L)?

T/F: enantiomers have all the same physical properties except for the direction each rotates plane polarized light

_________ occur when 2 or more optically active centers are present in a molecule (2 chiral centers)

Ephedrine and Psuedoephedrine are diastereomers. Do they have different melting points and solubilities in water?

T/F: most drugs available are diastereomers.

What are all the reasons why stereoisomers display different biological responses?

What are some examples of drugs that have been heavily modeled using 3D structures?

What technique is explaining why side effects occur, variability in efficacy, and most importantly possible new indications for drugs?

What is a strucural component or functional group of a molecule whose steric, electronic, and solubility characteristics are interchangeable?

What are some examples of acyclic steric isosteres?

What are some examples of cyclic steric isosteres?

What is an example of an antibiotic that is a cyclic steric isostere?

What are the 2 properties of an agonist/stimulant?

What kind of drugs are being pushed to be developed because they promise precise control over diseases mediated by G-protein coupled receptors? (type of binding)

The receptor occupancy theory states that the response observed is a function of what?

A drug + a receptor bind and form a complex that leads to the production of.....?

_____ ______ _______ reveal the affinity and effective concentration of a series of drug analogs?

What theory states that the agonist/stimulant activity is proportional to the rate of drug-receptor combo rather than the # of occupied receptors?

_____ have a high association rate but a low rate of dissociation?

Which theory best explains partial agonist or antagonist properties and that small molecule binding produces specific or non-specific conformational perturbations in a macromolecule?

Which theory states that a substrate or drug binding to the receptor induces 3D conformational changes in the macromolecule positioning catalytic groups in the correct position to conduct productive chemistry or altering membrane behavior? (ex opens channels for calcium)

___ needs bioactivation to remove the negative modifier?

_______, the active drug, needs metabolic inactivation by removing the positive modifier to eliminate or minimize unwanted systemic effects?

______ contains both negative and positive modifiers where the negative modifier is removed first at the site of action (as in prodrug) and the positive modifier is removed later when reach systemic circulation after its activity (as in antedrug)?

What is drug latentiation?

Approximately how many marketed prodrugs are activated by hydrolysis?

a compound that contains a structural characteristic required for pcol activity but is NOT susceptible to metabolism?

these compounds are designed and synthesized as active compounds that readily undergo metabolic inactivation to nontoxic products?

Waht are the 5 objectives for improving bioavailability using a prodrug?

drugs that are attached through a metabolically labile chemical linkage to another molecule designated as the "promoiety"?

What are the advantages of carrier-linked prodrugs?

What is an example of a carrier-linked prodrug?

What is the most common type of prodrug?

What two types of beta-lactam antibiotics cause a prodrug esterification problem?

How do we counteract the beta lactam prodrug ester problem?

What drug uses a double ester to increase absorption and avoid acid catalyzed decomposition?

What is the most common amine derivative used as a prodrug?

Why do we not use amines as much for prodrugs?

Where does the 'azo' linkage as a prodrug usually occur in the body?

What drug utilizes the azo linkage as a prodrug to its advantage?

Which prodrug forms a formaldehyde as a byproduct to treat chronic UTIs?

Which class of prodrugs does not contain a carrier or promoiety?

What is an example of a bioprecursor prodrug that undergoes oxidation?

What is an example of a bioprecursor prodrug that undergoes reduction?

What is an example of a bioprecursor prodrug that undergoes phosphorylation?

What are some types of carriers that have been used in chemical delivery of drugs?

What do Warfarin, Irinotecan, and Atomoxetine all have in common?

What is a common drug that will enhance metabolism?