Medicines by design

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  • Created by: Sabina
  • Created on: 22-04-16 14:24
What triggers biochemical reactions?
When chemicals fit into receptors and temporarily bond with them
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What is a drug?
A molecule that is able to interact with a receptor
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What is a pharmacophore?
Fragment of a molecule that binds to the active site of an enzyme (the part of the drug that gives it its activity)
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What does the fit of a pharmacophore into a receptor site depend on?
1.Size and fit-must have particular structure to fit into receptor 2.Bond formation-functional groups in pharmacophore form temporary bonds with functional groups in the receptor 3.Orientation-If pharmacophore has optical of E/Z isomers only 1 fit
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What needs to be considered when designing a drug?
Whether you want the drug to increase the body's natural response or decrease it
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What type of drug would you use to increase the body's natural response?
Agonistic drug
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What does an agonistic drug do?
Binds to the receptor and triggers a response
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What type of drug would you use to decrease the body's response?
Antagonistic drug
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What does an antagonistic drug do?
Binds to the receptor and blocks it
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What do chemists need to think about when they are trying to make a new drug to treat a disease?
1.Is there a natural compound already used to treat the disease? 2.Is there a compound in the body that is involved in the process 3.Molecule screening to see if any bind to target receotor
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How can molecule screening and rational drug design be speed up?
Using computer 3D modelling and rational drug design
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What is computer 3D modelling and how does it speed up drug design?
Database of 3D models of compounds that can be searched that can be searched to find the compound that may fit the 3D model of the target receptor site.This cuts down the number of compounds that need to be tested in the lab
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What is rational drug design
When a new compound is built from scratch using a 3D model of the receptor site
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What is the role noradrenaline?
Expands airways and increases your heart rate and blood pressure
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What is the role of salbutamol?
Treats asthma symptoms, without the raised heart rate and blood pressure
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What is the role of isoprenaline?
Used to increase heart rate for some heart problems
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What questions must be asked when testing a drug?
1.Is it safe? 2. Does the drug work? 3.Is it more effective than existing treatment?
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What is an addition reaction?
When two molecules join together to form a single product. This involves breaking a double bond (alkene,ketone and aldehyde)
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What is an elimination reaction?
Removing a functional group which is released as part of a small molecule.Often a double bond is formed (alcohol,phenol, halogenoalkane)
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What is a substitution reaction?
When a functional group on a molecule is swapped for a new one (halogen, benzene, alcohol and phenol)
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What is a condensation reaction?
When two molecules join together with the loss of a small molecule (carboxylic acid, acyl chloride and amide)
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What is a hydrolysis reaction?
When water is used to split apart a molecule creating two smaller ones (ester, acid anhydride, polyamide and polyester)
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What is a radical?
An atom, molecule or ion that has an unpaired electron
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What is an electrophile?
Attracted to molecules with areas of high electron density where is accepts electrons
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What is a nucleophile?
Attracted to regions of partially positive charge density.It can donate a pair of electrons to form a dative covalent bond
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What is a carbocation?
An organic ion with a positively charged carbon atom. They form when a bond breaks and the electrons move away from the carbon atom
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Describe radical substitution
INITIATION:A molecule splits into two free radicals PROPAGATION:The radicals react with a molecule to form a radical+molecule TERMINATION:Radicals react together to form molecule
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Describe electrophilic addition
The partially positive charge of a polar molecule or positive ion is attracted to the electrons in a double bond. The double bond opens up and the molecule is added
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Describe nucleophilic substitution
The partially negative charge of a polar molecule or a negative ion is attracted to the partially positive charge of a polar bond in a molecule.The nucleophile replaces the atom or functional group
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Describe electrophilic substitution
Usually occurs in aromatic compounds.The partially positive charge of a polar molecule or a positive ion is attracted to an electron rich region and is substituted for an existing group
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Describe nucleophilic addition
The partially negative charge of a polar molecule or a negative ion is attracted to the partially positive charge of a polar double bond.The double bond opens up and the nucleophile is added
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What is NMR?
Nuclear magnetic resonance spectroscopy which tells us how many hydrogens there is in a organic molecule and how they are arranged
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What is nuclear spin?
What allows the nuclei of some atoms to make them behave as if they were tiny magnets
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What happens if nuclei with nuclear spin are placed in a strong external magnetic field?
Some align themselves in the direction of the field while others align themselves against the field
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What affect does the position of the nuclei alignment have on the energy of the nuclei?
The nuclei that are aligned in the direction of the field are at a slightly lower energy than those aligned against the field
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What happens to nuclei if they are given a pulse of radio frequency radiation?
The nuclei in the lower energy state are promoted to the higher energy state-this is called resonance.The excited nuclei return to their original state by loosing the same amount of energy-this energy lost can be detected
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Why are deuterated solvents used in NMR is the sample needs to be in a solution?
They don't contain H atoms, and so do not interfere with the spectrum produced
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How does NMR spectroscopy work?
The sample is subjected to pulses of radio frequency radiation.The energy released when the nuclei resonates is detected and converted to an NMR spectrum on the recorder
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What is the technique called when the H atom is being investigated by NMR and what information does it provide us with?
Proton NMR. Gives us information on the chemical environment in which hydrogen nuclei are found
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What is common in all proton NMR spectra?
1.Absorption is plotted on the y-axis 2.Chemical shift is plotted on the x-axis 3.The chemical shift scale runs from 0ppm at the right-hand side to around 10ppm
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What is a deuterium solvent?
A solvent that has their hydrogen atoms replaced by deuterium (an isotope of hydrogen that has two nucleons a proton and a neutron so there is no overall spin on the nucleus
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Other cards in this set

Card 2

Front

What is a drug?

Back

A molecule that is able to interact with a receptor

Card 3

Front

What is a pharmacophore?

Back

Preview of the front of card 3

Card 4

Front

What does the fit of a pharmacophore into a receptor site depend on?

Back

Preview of the front of card 4

Card 5

Front

What needs to be considered when designing a drug?

Back

Preview of the front of card 5
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