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MTC > Drugs and Chirality > Flashcards

Drugs and Chirality Flashcards

Week 1

1
Q

What is the composition of a pharmaceutical and its %?

A

AP(8-10), fillers (80%), disintegration (, disaggregation and dissolution (10%)

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2
Q

what are pharmaceuticals?

A

Solids, liquids and gas formulations that treat, cure and prevent disease

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3
Q

What is the basis of many drugs and why?

A

carbon, has 4 valence electrons so can have covalent bonding.

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4
Q

What are the properties of API?

A

Carbon/Hydrogen backbone with functional groups that create a biologically active substance.

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5
Q

What is the role of functional groups?

A

Determines the role of action of the pharmaceutical through binding and the given properties.

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6
Q

What properties do functiocal groups determine?

A

Chemical (acid/base, solubility, reactivity) , physical (something that is measured) and chemical stability.

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7
Q

What is drug likeliness?

A

Predictor of drug’s biological activeness.

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8
Q

what is needed for water solubility?

A

H bonding and ion-dipole interaction. AThe drug must have polar functional groups (hydrophobic and philic molecules)

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9
Q

what does drug likeliness depend on?

A

water solubility and binding

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10
Q

What is Lipinski’s rule?

A

HBD less than 5, HBA less than 10, MM less than 500 and coefficient Log P less than 5.

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11
Q

What is needed in a H bond?

A

a polarised H-X bond where the H is sharing the electron and hetero atom with lone pair of electrons (negative)

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12
Q

What is a dipole-dipole bond?

A

attraction between positive and negative poles as electrons are shared and tried to be pulled to each other.

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13
Q

what creates a greater polarity?

A

Greater difference in electronegativity

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14
Q

when is EN considered a Non-Polar Covalent

A

EN between 0.2 and 0.4

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15
Q

when is EN considered a Polar Covalent

A

En between 0.6 and 2.0

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16
Q

when is EN considered Ionic?

A

2.2-3.2

17
Q

What makes something more polar in water?

A

Polar bonds

18
Q

What are the stages of drug action?

A

absorption, distribution to target, binding at target, metabolism and excretion.

19
Q

What are the properties that are crucial to drug binding ability?

A

3D Shape and Polarisation of functional groups

20
Q

what are the crucial properties of drug absorption?

A

Hydrophobicity (across cell membrane) and hydrophilicity (through blood)

21
Q

What are the two types of enzyme inhibitors?

A

reversible and irreversible

22
Q

What is the geometry of a molecule with single, double and triple bond?

A

tetrahedral, trigonal planar and linear

23
Q

what are the three types of constitutional isomers?

A

skeletal, functional group and positional isomers

24
Q

What is a chiral centre

A

Carbon atom with four different functional groups that is not superimposable on its mirror image.

25
Q

How do you determine chilarity?

A
  1. find centre
  2. prioritise according to atomic number
  3. oriented so lowest priority number is going away from you
  4. determine of r or s
26
Q

what does r and s mean respectively?

A

r= clockwise
s= anticlockwise

27
Q

What are enantiomers?

A

Non superimpsobale mirror images

28
Q

What is chiral recognition?

A

enzymes that are drug targets are chiral and so usually only occur as a single enantiomer. drugs should only recognise one.

29
Q

diastereoisomers

A

stereoisomers that are not mirror images (differ three-dimensionally)

30
Q

How do you deterine the diastereoisomers of a molecule?

A

reverse the chilarity of any chiral centre (not all of them though)

31
Q

What does the wedge represent?

A

Towards me (out of the page)

32
Q

What does the dotted wedge mean?

A

Going away from me (into the page)

33
Q

What is the acronym for identifying HBA and HBD

A

A(acceptors)N(not)D(donors)Y(yes)

34
Q

Why in lipinski’s rule can there be 10 HBA but only 5 HBA?

A

Because all donors are also acceptors, except for amides

35
Q

What are incompatbilities?

A

antacids

36
Q

what do antacids do?

A

Alter the pH of the stomach via neutralisation, ionise drugs based on the relationship of pH and pKA and affect absorption and distribution.

37
Q

what is pKA?

A

Acid dissociation constant to the negative base log 10. Determines acids strentth

38
Q

The smaller the pKa, the. … the acid

A

stronger

39
Q

what are some antacid drugs?

A

Maalox, Tums and Rennie

MTC (14 decks)

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