chirality

Descripción

chirality in drug design
Sam Watkins
Test por Sam Watkins, actualizado hace más de 1 año
Sam Watkins
Creado por Sam Watkins hace alrededor de 8 años
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Resumen del Recurso

Pregunta 1

Pregunta
enantiomers are non identical mirror images with a plane of symettry
Respuesta
  • True
  • False

Pregunta 2

Pregunta
enantiomers are a pair of stereoisomers that are non identical mirror images of eachother
Respuesta
  • True
  • False

Pregunta 3

Pregunta
diastereoisomers are
Respuesta
  • a pair of non identical stereoisomers that are not mirror images of eachother
  • a pair of non identical stereoisomers that are mirror images of eachother
  • a pair of identical mirror images with a plane of symettry

Pregunta 4

Pregunta
when describing chiral centres.. (select all that are true)
Respuesta
  • R/S classifies a chiral centre by the groups around it
  • D/L classifies a chiral centre by comparison to a reference compound glyceraldehyde
  • d/l classifies a molecule by the direction it rotates polarised light d is clockwise
  • +/- is the same as R/S. R = + S = -

Pregunta 5

Pregunta
Biosynthesis (synthesis of molecules in a biological system) is often stereoselective
Respuesta
  • True
  • False

Pregunta 6

Pregunta
Chiral synthesis in the laboratory is often very [blank_start]difficult[blank_end]. It is even harder to scale up to industrial scale. Two approaches to obtaining pure chiral molecules are [blank_start]Chiral separation[blank_end] (use a physical method e.g chromatography to separate the desired stereoisomer from a mixture) and [blank_start]The Chiral Pool[blank_end] (use a starting material that already contains a chriral centre.)
Respuesta
  • difficult
  • straightforward
  • fast
  • Chiral separation
  • chiral synthesis
  • HPLC/MS
  • The Chiral Pool
  • The chemical pool
  • chiral separation
  • chiral splitting

Pregunta 7

Pregunta
about 25% of drugs are administered as a racemate - an equal mixture of stereoisomers
Respuesta
  • True
  • False

Pregunta 8

Pregunta
some drugs are given as a single isomer which means a larger dose is required
Respuesta
  • True
  • False

Pregunta 9

Pregunta
which of the following is FALSE
Respuesta
  • for a pair of stereoisomers the one with the greater activity is the eutomer
  • for a pair of stereoisomers the one with the lesser activity is the distomer
  • the ratio between the distomer and the eutomer is the disumic ratio

Pregunta 10

Pregunta
select which apply about the ADME of stereoisomers:
Respuesta
  • during ABSORPTION by transmembrane proteins stereoisomers of chiral drugs can absorb differently
  • during ABSORPTION by passive diffusion stereoisomers of chiral drugs absorb differently
  • DISTRIBUTION leads to the stereoisomers having different effects because they bind to the plasma proteins
  • METABOLISM causes stereoisomers to be the broken down same as the same enzymes are used for both R and S forms of the drug

Pregunta 11

Pregunta
The development of a [blank_start]single[blank_end] isomer drug from a previously marketed [blank_start]racemate[blank_end] is known as the [blank_start]chiral switch[blank_end]
Respuesta
  • single
  • R-
  • multi
  • racemate
  • eutomer
  • tablet
  • distomer
  • chiral switch
  • chiral pool
  • chiral centre

Pregunta 12

Pregunta
which are advantages of the chiral switch?
Respuesta
  • improved biological activity
  • opportunity to market a new product
  • reduced side effects
  • simpler pharmacokinetics
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