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Medicinal Chem

test 1

isolation of pure substances began with solvent extractions in 19th cent
solvent extraction: Andreas Marggraf German chemist- observed that brandy could extract a crystalline substance(sucrose) from beetroot
Solvent extraction: CArl Wilhelm Scheele (1742-1786) applied solvent extraction to the isolation of acids from plant juices. Isolated citric, malic, oxalic, and gallic acids in 1780s
Opium used in ancient civil for med purpose and religion. Produced by drying the latex taht exudw from the capsules of poppy
Friedrich Wilhelm Serturner isolation of crystallin from poppy latex... admin to dogs made them sleepy
Alexander Wood 1853 Invented the hypodermic syringe...true power of morphine pain relief was disc. his wife became first known morphine addict and died of overdose.. dosing not estab many civil war people died
Heroin treat morphine with acetic anhydride--> diacetylmorphine (dimorphine) (marketed by bayer pharmaceutical)
J Masson Gulland and Robert Robinson deciphered the chem structure of morphine robert won the nobel prize in 1947
morphine today Morphine, and related opioid alkaloids, remain the most effective method for the treatment of severe pain.action of morphine is due to its agonism of the mu (m) opioid receptor in the CNS
Cinchona Bark Jesuits in 17th cen SA used it to cure malaria. cure brought to europe ROBERT TALBOR used it to cure kings
Joseph Pelletier and Joseph Bienaime Caventou isolated the active principle of cinchona--> QUININE in 1820. they opened 2 factories 3600kg of yearly quinine sulfate.
Paul Rabe proposed the correct structure of quinine (1907) .. later confirmed by a total synthesis by robert b woodward
Robert Woodward formal synthesis of quinine... maser of the art of organic synthesis. led to nobel prize 1965
quinine today no longer used due to parasitic resistance related derivatives are used. prohoylacticatlly and for treatment of the diease (chloroquine and Mefloquin)
Epinephrine (adrenaline) 1900-1910vasoconstrictor injected intramuscularly or intravenously to raise blood pressure or relieve anaphylaxis in the case allergic It is also injected subcutaneously to locally constrict blood vessels and thus prolong the action of local anesthetics
Jokichi Takamine able to precipitate the free base of adrenaline from aqueous solution by addition of aqueous ammonia solution to raise the pH developed a collaboration with the pharmaceutical company Parke, Davis and Company
Arsphenamine (salvarsan) antisyphillitic
Paul Ehrlich library of organoarsenic compounds.. one became treatment for syphilis from 1910-1944 until penicillin came about. nobel prize 1908
Phenobarbital (luminal) used to treat epilepsy anticonvulsant
Barbituric Acid drug used to treat insomnia until 1950 phenobarbital made my emil fischer as a sedative nobel in 1902
Adolph von Baeyer first prepared barbituirc acid-->nobel prize in 1905
sedatives today As sedatives, the barbituates were displaced by the benzodiazepines in the 1950s, but they are still utilized to treat seizures.
Insulin (treatment of diabetes mellitus) peptide horm secreted by the pancreas, regulates the uptake of glucose from the blood, FIRST HORM TO BE ISOLATED
frederick grant banting and john james rickard macleod nobel in 1923 for the discovery of insulin
Dorothy Crowfoot Hodgkin used xray crystallography to obtain the 1st crystal structure of insulin. nobel 1964 for work on the xray crys techniq
Suldanilamide (antiinfective)The sulfa drugs represented the first highly effective antibiotics and saved thousands of lives
sulfa drugs today very old antibiotics but still used today used by forming combo mixture co-trimoxazole
target of penicillins target of the penicillins are the PBPs (penicillin binding proteins) transpeptidases responsible for cross-linking peptidoglycan strands
chlorpromazine (thorazine)..antipsychotic, treatment for schiz
Norethynodrel/ mestranol (enovid) ...use birth control (1st oral contraception)
contraceptive medicine now alternat to oral pills: patches--> admin hormones transdermally
Propranolol (inderal) ..beta receptor antagonist, a beta blocker, antihypertensive block the action of adrenalin and developed the first of the ‘beta-blockers’ which block the action of adrenalin at the beta-adrenergic receptors.
James W Black developed propranolol nobel 1988
Cimetidine (tagamet) H2 receptor antagonist, treat heartburn, GERD
captopril (capoten) Inhibitor of angiotensin converting enzyme ..antihypertensive
fluoxetine (prozac) serotonin reuptake inhibitor (antidepressant)
atorvastatin (lipitor) cholesterol reduction
saquinavir (fortovase) HIV protease inhibitor (treat HIV)
sildenafil (viagra) treat erectile disfunction , inhibitor of PDE5
Trastuzumab (herceptin) monoclonal antibody to the HER2 protein... treat breast cancer
Imantinib (Gleevec) inhibitor of the ABL tyrosine kinase... treatment of selected cancers
Created by: Demimartinez01



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