Quiz
L12 Structure Activity Relationships
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Fragen in diesem Quiz (14)
1Choose the correct statement about structure activity relationships.
- AThey are the relationship between chemical structure and pharmacological activity for a series of molecules.
- BThey are the relationships between chemical structure and pharmacological activity for a molecule.
2The defined pharmacological activity can [blank_start]vary[blank_end] greatly. It could be a binding interaction with a [blank_start]specific[blank_end] receptor, a functional readout of compound [blank_start]activity[blank_end], toxicity, drug adsorption, and much more.
- Avary
- Bspecific
- Cactivity
3Generally SAR analysis is [blank_start]qualitative[blank_end]. however, the field of research to mathematically quantify SARs is known as QSAR – [blank_start]quantitative[blank_end] structure activity relationships
- Aqualitative
- Bquantitative
4Choose the incorrect statement about QSARs.
- AIt is a statistical algorithm that quantitatively defines the relationship between the chemical structure of a drug and its effect on an organism
- BQSARs save money because they can be done without cost of synthesis and biological assays
- CQSARs do not promote green chemistry because they are done on computers
5By rationalising the mechanisms of action within a series of drugs we can a) design new drugs or b) make better drug choices from a class of drugs to:
(select all correct)- AIncrease drug potency
- BDecrease stability of drug
- CDecrease toxicity of drug
- DIncrease or decrease duration of action
- EIncrease selectivity
6The ‘pattern’ of what a pharmacophore is can be found from SAR studies
- ARichtig
- BFalsch
7What can we use to quantify the relationships between functional groups in the 3D pharmacophore(QSAR)?
- AVectors
- BAngles
- CDescriptive terms
8For a flexible molecule with many conformations, it is easier to identify the pharmacophore.
- ARichtig
- BFalsch
9Molecular structure and biological activity are correlated by observing the [blank_start]experimental[blank_end] results of systematic structural [blank_start]modification[blank_end] on defined biological endpoints. The relevance of a functional group to binding can be determined by synthesising analogues where the functional group is slightly [blank_start]modified or removed[blank_end], then this molecule tested to [blank_start]compare[blank_end] the difference.
- Aexperimental
- Bmodification
- Cmodified or removed
- Dcompare
10Steric bulk influences binding. You can [blank_start]change[blank_end] the steric bulk gradually, test each iteration, and develop an understanding of the [blank_start]optimal[blank_end] structure for the desired biological activity. For ligand-receptor interactions, sometimes [blank_start]bulky[blank_end] is better, sometimes it's worse; it’s about finding the optimal ligand-receptor fit.
- Achange
- Boptimal
- Cbulky
11Choose the incorrect statement about lipophilicity.
- AThe more lipophilic, the lower the logP number, i.e. the more molecules in the octanol versus water layer
- BclogP is the calculated logP, using a computer program
- CLipophilicity is quantified using logP, the measured partition coefficient of a molecule between octanol (lipophilic phase) and water (hydrophilic phase) in equilibrium at constant temp
12For un-ionisable compounds, logP is approximately equal to logD at any pH.
- ARichtig
- BFalsch
13When pH is involved, instead of logP we use [blank_start]logD[blank_end], the measured [blank_start]distribution[blank_end] constant of a molecule between octanol and a [blank_start]defined pH aqueous solution[blank_end].
- AlogD
- BlogpH
- Cdistribution
- Ddefined pH aqueous solution
14Comparing [blank_start]isosteres[blank_end] helps establish [blank_start]SARs[blank_end] by identifying the key physical requirements
- Aisosteres
- BSARs
Informationen
- Beschreibung
- PHCY211 (Molecules) Quiz am L12 Structure Activity Relationships, erstellt von Mer Scott am 10/04/2018.
- Autor
- Mer Scott
- Sprache
- English
- Aufrufe
- 12
- Schlagwörter
- Bewertung
- Noch keine Bewertungen Bewerte dieses Quiz