OCR F335 Medicines by Design

HideShow resource information
  • Created by: Bethany.
  • Created on: 13-05-16 20:28
Preview of OCR F335 Medicines by Design

First 395 words of the document:

F335 Chemistry by Design: Medicines by Design
Bonding and Structure
(a) describe and explain the structure and action of a given pharmacologically active material in terms of:
(i) the pharmacophore and groups that modify it
Pharmacophore ­ the part of the substrate that binds to the receptor site. It is the part of the drug that gives it
its activity.
It is possible to modify the pharmacophore to make a drug more effective or to reduce its side effects. For
example, noradrenaline is naturally found in the body and has been modified to treat different disorders.
Noradrenaline Salbutamol Isoprenaline
Expands airways and increases your Treats asthma symptoms, without Used to increase heart rate for
heart rate and blood pressure. the raised heart rate and blood some heart problems.
(ii) its interaction with receptor sites
Active Site ­ the part of the enzyme where the substrate forms intermolecular bonds with functional groups of
the enzyme, aka receptor site.
Pharmacophores are designed to be complementary to the shape of specific receptor sites. To design a drug you
need to consider if you want the drug to increase the response that happens naturally, or decrease it.
If you want a drug to increase the natural response you use an agonistic drug ­ binds to the receptor and
triggers a response .
If you a drug to decrease the response you use an antagonistic drug ­ binds to the receptor and blocks it.
(iii) the ways that species interact in three dimensions (size, shape, bond formation, orientation)
The `fit' of a pharmacophore into a receptor site depends on:
Size and shape ­ it must be complementary to the receptor site.
Bond formation ­ functional groups in the pharmacophore form temporary bonds with the functional
groups in the receptor. These are mostly ionic interactions or intermolecular forces , e.g. hydrogen
bonding. Covalent bonding is permanent so would irreversibly block the receptor.
Orientation ­ pharmacophores capable of optical or E/Z isomerism will only have one isomer that will fit
into the receptor site.
Organic Functional Groups
(b) recognise and draw structures for individual functional groups mentioned everywhere in the
specification (AS and A2) within a polyfunctional molecule (synoptic) hence make predictions about its

Other pages in this set

Page 2

Preview of page 2

Here's a taster:

F335 Chemistry by Design: Medicines by Design
(c) recall and use systematic nomenclature for naming and interpreting names of compounds met earlier in
the specification (AS and A2) (synoptic)
Name General Formula Example Nomenclature
Acid Anhydride RCOOCOR' oic anhydride
Acyl Chloride RCOCl yl chloride
Alcohol ­ C
Alcohol ­ CnH2n+1OH ol
Alcohol ­ C
Aldehyde C
Alkane C
Alkene CnH2n
Amide RCONH2
Amine RNH2
Arene C6H5X benzene
Carboxylic Acid RCOOH…read more

Page 3

Preview of page 3

Here's a taster:

F335 Chemistry by Design: Medicines by Design
Ketone C
Organic Reactions
(d) recall organic reactions and reaction conditions mentioned elsewhere in the specification (AS and A2)
(synoptic); use these with any further given reactions, to suggest and explain synthetic routes for
preparing organic compounds including simple examples of retrosynthesis
Retrosynthesis ­ working backwards from the target product to determine the reactants involved in the
Example: Ethyl ethanoate is a solvent that has a fruity odour.…read more

Page 4

Preview of page 4

Here's a taster:

F335 Chemistry by Design: Medicines by Design
Hydrolysis Involves using water to split apart a molecule creating two smaller ones. It is the opposite of
Reaction Mechanisms
(f) use and explain the following terms:
Radical An atom, molecule or ions that has an unpaired electron.
Electrophil A positive ion or molecule with a partial positive charge that will be attracted to a negatively
e charged region and react by accepting a lone pair of electrons to form a covalent bond.…read more

Page 5

Preview of page 5

Here's a taster:

F335 Chemistry by Design: Medicines by Design
Nucleophilic 1. The cyanide ion is the
Addition nucleophile and is attracted to
the carbon atom in the carbonyl
group, which carries a partial
positive charge.
2. A new CC bond forms, and pair
of electrons in the C=O bond
moves onto the oxygen atom, which then carries a negative charge.
3. The new negatively charged ion then takes up a proton from the solvent, water.
4. Cyanohydrin is formed.…read more

Page 6

Preview of page 6

Page 7

Preview of page 7

Here's a taster:

F335 Chemistry by Design: Medicines by Design
being offered as an incentive, but this could be seen as taking advantage of the poor who need the money. Some
people think that pharmaceutical companies have too much influence over the drug approval process, claiming
that test results can easily be skewed to obtain the desired result and that the companies use marketing tricks to
push their products to market.…read more

Page 8

Preview of page 8


No comments have yet been made

Similar Chemistry resources:

See all Chemistry resources »See all resources »