MTC Flashcards
(42 cards)
Competitive binding (in regards to drugs) means
That a drug is competing with a natural substrate for an active site
Reversible inhibition occurs when a drug binds via which type of bonds
Non-covalent intermolecular
Irreversible inhibition occurs when a drug binds via which type of bonds
Covalent
Esters hydrolyse into what
Carboxyllic acids
True/False: Drugs that irreversibly bind are not-toxic
False, drugs that bind irreversibly are usually toxic
Toxic/irreversibly binding agents are useful as what type of agent/drug
Chemotherapeutic, invading pathogen killing agents
Lipinski’s rule of 5 (relating to oral drugs) is
- Less than 5 H-bond donors (OH, NH)
- Less than 10 H-bond acceptors (O, N)
- Molecular weight less than 500 g/mol
- Partition co-efficient (Log P) less than 5
Enteral route means
Via oral administration
Parenteral route means
Via intravenous injection
What type of molecule passes through lipid bilayer
Small, uncharged, non-polar molecules
What are prodrugs
Inactive compounds that are converted into active drugs within the body
What is a conformer
Different geometry resulting from rotation around a C-C single bond
What are two examples of conformations
Staggered and eclipsed
What are constitutional isomers
Compounds with the same molecular formula but different structural formulas
What are stereoisomers
Compounds with the same molecular formula but different 3d arrangement (e.g. cis/trans groups)
What are diastereoisomers
Stereoisomers that are not complete mirror images of one another
What are chiral compounds/enantiomers
Compounds that are non-superimposable mirror images of one another
Which protein derived amino acid is NOT chiral
Glycine
What kind of configuration do all naturally derived amino acids (except glycine) have
L-configuration
What is the CIP system used for
Specifying configuration around a stereocentre
What is the Fischer system used for
Specifying configuration of an amino acid
In terms of protein structure, what does primary/secondary/tertiary/quaternary mean
Primary: amino acid chain
Secondary: a-helices or b-sheets
Tertiary: multiple secondary structures
Quaternary: multiple tertiary structure subunits
What determines the overall chirality of aldohexoses
The position of the OH group on the penultimate carbon
What kind of configuration do all naturally derived aldohexoses have
D-configuration at the penultimate carbon