MEDORG 2

• Medicinal Chemistry is a science which incorporates different branches of chemistry and biology in the research for the discovery and design of new and better therapeutic chemicals and development of those chemicals into new medicines and drugs.
• The roles of a Medicinal Chemist include making new compounds, determining the effect of the drug on biological processes, altering the structure of the compound for optimum effect and minimum side effects, and studying uptake, distribution, metabolism, and excretion of drugs.
• A functional group is a group of atoms responsible for the characteristic reactions of a particular compound.
• Acidic functional groups are hydrophilic, can form salts when combined with bases, and include carboxylic acids, carboxylic acid derivatives, and carboxylic acid esters.
• Basic functional groups include aliphatic and alicyclic amines, aromatic amines, aromatic, heterocyclic nitrogens, imines, hydrazines, and amidines.
• Examples of aliphatic and alicyclic amines include Lidocaine, Albuterol, Ticlopidine, and Gabapentin.
• Examples of aromatic amines include procainamide.
• Examples of aromatic, heterocyclic nitrogens include Prazosin, Quinidine, and Serotonin.
• Examples of additional basic functional groups include guanethidine, tetrahydrozoline, hydralazine, and hydrazine.
• Eli Lilly's Humulin® was the first synthetic human insulin to be sold in the market and approved by USFDA.
• Mercury, lead, arsenic, and antimony are poisons that were used in the 17th to 20th Century from natural sources.
• Carl Koller realized that cocaine numbed the tongue, realizing that it's an effective, non-irritating anesthetic for the eye.
• Gerhard Domagk discovered 2,4-Diaminoazobenzene-4'-sulfonamide, also known as Prontosil, a red dye that can cure systemic gram-positive bacterial infections.
• 6-MERCAPTOPURINE (Purinethol Ⓡ), a synthetic drug, was developed by George Hitchings and Gertrude Elion.
• Friedrich Sertürner isolated morphine from opium, also known as Papaver somniferum.
• Cocaine (Erythroxylon coca), a naturally-occurring alkaloid, was isolated by Albert Niemann and its structure was determined by Richard Willstatter.
• Henri Laborit noted distinctive psychotropic effects in man.
• CISPLATIN is an inorganic molecule with a simple structure and second-generation compounds such as carboplatin are also available.
• It depends only upon the dose whether a poison is a poison or not.
• Frederick Banting and Charles Best isolated insulin from a dog's pancreas and, together with James Collip and John Macleod, produced a pure form from the pancreases of cattle.
• Pierre Deniker and Jean Delay published a clinical trial treatment in psychotic patients.
• Benzocaine, procaine, tetracaine, and lidocaine are structural analogs of cocaine.
• Pierre-Joseph Pelletier isolated emetine from ipecacuanha.
• Diazepam (Valium®) was synthesized through the structural modification of benzodiazepine derivatives.
• Chlorpromazine, also known as Thorazine, was first synthesized by Paul Charpentier and observed distinctive effects on animal behavior by Simone Courvoisier.
• Accidental discovery of mephenesin, also known as Chlordiazepoxide (Librium®), was made by Lowell Randall.
• William Withering used digitalis for the treatment of edema and heart conditions, also known as Digitalis purpurea, also known as Lady's glove plant.
• Paul Ehrlich produced compound 606/Arsphenamine/Salvarsan, also known as antisyphilis, also known as "magic bullet", also known as proposed selective toxicity, also used until the 1940s when it was replaced by penicillins, also known as Father of Chemotherapy.
• Carl Wilhelm Scheele discovered lactic acid, citric acid, and tartaric acid.
• Albert Niemann isolated cocaine, also known as Erythroxylum coca.
• Anxiolytics are benzodiazepines, including Meprobamate, also known as Miltown.
• Stereochemistry deals with the spatial arrangement of atoms and groups in a compound and its relation to the properties of the compound.
• Conformation is any of the spatial arrangements of a molecule that can be obtained by rotation of the atoms about a single bond.
• Configuration is the stable structural makeup of a chemical compound especially with reference to the space relations of the constituent atoms.
• Constitutional isomers are compounds whose atoms are connected differently.
• Connectivity refers to how atoms are attached to one another.
• Absorption rate and extent of disappearance of drug from the site of administration (physiologic definition) and rate and extent of drug entry into the systemic circulation (pharmacologic definition) are important in drug absorption.
• Methylprednisolone is slightly water insoluble, Methylprednisolone acetate is water insoluble, and Methylprednisolone Na Succinate is water soluble.
• Drugs administered orally as a solid or in suspension must dissolve in the aqueous gastric fluid before they can be absorbed.
• Polar groups either ionize or are capable of hydrogen bonding with water, altering the solubility characteristics of drugs.