Drug classes according to their Pharmacophores

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  • Created by: Rscottqub
  • Created on: 03-03-20 18:36
SAR
structure activity relationship
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Types of chemicals in disease
antibacteria. antiviral. antineoplastics, anti diabetic, CNS agents , respiratory agents
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Antibacterials 5 MOAs
1. Inhibit metabolism 2. inhibit cell wall synthesis 3. Interact with plasma membrane 4. Inhibit protein synthesis 5. Inhibit NA transport and replication
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Why are bacteria good targets
cells bare little resemblance to human cells
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Inhibition of metabolism - Sulfonamide analgoes
para sub = vital for activity , the sulfonamide N must be either primary or secondary . the only place where variation is possible is at R2
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Inhibition of cell wall synthesis
Pencillins inhibit transpeptidase- which is responsiible for peptidoglycan cross linking in the cell wall
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Interactions with the plasma membrane
example - vancomycyin - allows uncontrolled movement of ions acorss CM
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Disruption of proteinsynthesis
ie tetracyclines , macrolides - bind to and block ribosomes preventing PS. need to be able to recognise
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Inhibition of NA transport and rep
quinolones and fluroquinolones prevent replication and transport of NAs
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Antivirals may act via
inhibition of Reverse transcriptase, inhibiton of post transcription phase . ion channel disrupters. inhition of neuronidase
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neuronidase
enzyme which cleaves sialic acid - degrading the mucus layer allowing virus to reach epithelial cells
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Anti diabetic agents
Insulinotropic agents. Insulin sensitizing agents (Metformin) a-glucoside inhibitors
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a-glucoside inhibitors
delay digestion of carbs - therfore delayed absorption so hence reduced blood sugar levels
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Anti neoplastic
prevent tumour development. - alklating agents, ant metabolites , ant mitosis, free radical generation
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CNS agents
ie opiod analgesics - see diagram - be able to recognise
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Benzodiazepines
also CNS agents - enhance effect of GABA at the GABAa receptor - sedative, muscle relaxant, anxiety
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Barbituates
for hypnotic activity -
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lipid solubility of barbituares
increases activtity
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branching of barbituates
increases solubility and therefore activity
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polar groups in barbituates
decrease lipid sol and therfore decrease activity
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Drugs for neurodegenerative disease- Alzeimers
Anti AChE- more Ach available to reactive receptors
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Drugs for neurodegenerative disease- parkinsons
ie levadopa - precursor for dopamine, adrenaline and NA
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Respiratory agents
ephedrine(adrenaline) are agonists of the a and B adreno receptors
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salbutamol
B2 selective - short acting
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salmeterol
longer acting
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Other cards in this set

Card 2

Front

Types of chemicals in disease

Back

antibacteria. antiviral. antineoplastics, anti diabetic, CNS agents , respiratory agents

Card 3

Front

Antibacterials 5 MOAs

Back

Preview of the front of card 3

Card 4

Front

Why are bacteria good targets

Back

Preview of the front of card 4

Card 5

Front

Inhibition of metabolism - Sulfonamide analgoes

Back

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