SOURCES,STRUCTURE AND PROPERITES OF DURG SUBSTANCE Flashcards
what are the different sources of lead compound?
plant sources- marine sources microorganisms venoms and toxins animals
what are examples of plant derived lead compounds? which plants were they derived from?
morphine-opium poppy
digoxin-foxglove
quinine-cinchona bark
how are plant active component identified in the past and recently?
Past- ‘trial and error’ approach with the establishing of written records
recent- ‘Bioprospecting’ approach which is collecting and screening samples |(for commercial purposes) along with indigenous knowledge to asist in discovery of plant resources. lead compound discovery with traditional knowledge is 1 in 5000 sucess rate
give examples of marine lead compound source for
Eribulin- marine sponge used as an anti-cancer
Example of clinically used drugs extracted from microorganisms
Antibiotics- Penicillin
hypolipidemic - lovastatin
Immunosuppersant- ciclosporin
when is ciclosporin used and what does it I/C with?
immunosuppressant in organ transplantation and it is extensively metabolised therefore the use of grape fruit as a cyp450 inhibitor allows it to recirculate.
venom and toxin example of drugs and function
captopril - reduces blood pressure
extracted from brazilian pit vipe
extracted from teprotide
why is animal sources lead compound have limited potential in drug development?
compound instability in vivo and limited duration of action
what is the definition of semi-synthetic drug?
The chemical manipulation of the structure of the natural lead compound as it is usually complex, to improve their human activity, substrate selectivity, toxicology and bioavaliablity.
what type of molecules does semi-synthetic drugs produce?
compound that can easily convert to natural product once metabolized
or
analogues with better biological activity
Example of analogue derived from a lead compound
6 APA intermediate from Pencillin G (inactive antibiotic) derived from fermentation, produced analogues such as amoxicillin ,ampicillin and flucloxacilin.
what are synthesised drugs molecules that are starting points? example?
endogenous ligands
adrenaline to salbutamol
why are existing drugs used as a lead compound for development of new drugs?
1- biological testing, clinical trials and regulatory data is all avaliable
2-compound with similar/improved properties can be produced
example of modified existing drug
Tolbutamide from sulphonamides for diabetes (reduces blood sugar)
what is serendipity?
Discovered by chance observation which has given rise to new lead compound and drugs derived from it.
