Medicinal Chemistry
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What is pharmacodynamics?
How the drug effects the body ADME
What is pharmacokinetics ?
How the body effects the drug
What is a lead molecule ?
It’s a chemical compound that is not active and requires modifications to become a usable drug in many years time. It’s toxic dose is well above its therapeutic dose which means it has many side effects
What are the 3 different ways drugs can be synthesised?
Natural Semi synthesis Fully synthetic
What are natural drugs?
These are drugs which are directly extracted from a natural source eg a plant
What are semi synthetic drugs ?
This is when part of the natural source is synthetically modified
Why is synthesis of a drug useful ?
This allows you to inspire a new drug and make modifications so the natural drug is better
What are fully synthetic drugs ?
These are drugs that are entirely produced by chemical synthesis
Taxol
Taxol is a semi synthetic drug which naturally comes from yew trees, however scientists are using yeast cells instead of plant cells as they replicate faster
Aspirin
Aspirin a fully synthetic drug as it comes form salicylic acid with a acetyl group
Diazepam and paracetamol
They both are fully synthetic
Morphine
Morphine is a natural drug as it comes from opium poppies as it’s grown as a crop and extracted
Ethinyl oestradiol
This is semi synthetic as its extracted from the horse urine of pregnant female horses
What are proteins ?
They are polymers of 3 or more amino acids joined by an amide bond by condensation reaction. They are synthesised through the translation of RNA and can be described as peptides, polypeptides and proteins which can be done automatically or manually . Amino acid has backbones and residues
What are the 4 types of proteins that interact with a drug ?
Ion channels Enzymes Receptors Nuclear receptors
Tell me about receptor interactions with a drug ?
Receptors are proteins usually on the cell surface membrane of a cell. The drug receptor interactions takes seconds
Tell me more about enzyme interactions with a drug ?
The drug enzyme reaction usually takes minutes and is normally an inhibition of a molecule
Tell me more about nuclear- receptor drug interactions?
This process usually takes hours as the receptors are within the cells in the nucleus
Tell me more about ion channel drug interactions?
They take milliseconds for a drug to interact
How are molecules drawn and why ?
They are drawn skeletally as they are tetrahedral with an angle of 109 not square planar which metals are. And use dashed lines for functional groups
What are residues ?
They allow binding interactions
What are backbones ?
They ensure that the structure is stable and rigid
What is the primary structure ?
This the number and order of amino acids in a polypeptide chain joined by condensation reaction forming an amide bond which have backbones and residues
What is the secondary structure ?
Folding of the chain of amino acids forming either alpha helix or beta plated sheets with many weak hydrogen bonds