Drug formation

Drug name Drug format Main target(s) MoA Indication ... 

Bioerodible polymers having pendant functional groups are of particular interest, since they are capable of covalent pro-drug formation. Acemoglu [60] prepared... 

N and C termini of the peptide are connected via a linker to form a cyclic peptide. The linker can be cleaved by esterase to release the peptide. The cyclic peptide pro-drug formation increases the intramolecular hydrogen bonding and lowers the hydrogen-bonding potential to water molecules as solvent. In addition, the lipophi-licity of the cyclic prodrug increases, which shifts its transport from paracellular to transcellular.48 It has also been reported that cyclic peptides are less susceptible to amino- and carboxypeptidases than linear peptides because the amino and carboxy terminals are protected from these enzymes.44... 

BASF Fine Chemicals Generic Drug Formations 1998... 

Approximately 60% of the elimination of tocainide occurs by hepatic metabolism. The limited data available for stereoselective metabolism of tocainide indicate that a major metabolic pathway of the drug, formation of a glucuronide conjugate of N-carboxytocainide, is stereoselective in favor of R(—)-tocainide [117]. Whereas 45% of the R enantiomer was recovered in urine as the conjugate, only 1.2% of the administered S(-l-)-tocainide was found in the urine as this metabolite [117]. The stereoselectivity in the other metabolic pathways of tocainide in humans is not known at this time. 

Nishiyama N, Kataoka K. Nanostructured devices based on block copolymer assemblies for drug dehvery designing structures for enhanced drug formation. Adv Polym Sci 2006 193 67-101. 

Ecole Nationale Superieure du Petrole et des Moteurs Formation Industrie end point (or FBP - final boiling point) electrostatic precipitation ethyl tertiary butyl ether European Union extra-urban driving cycle volume fraction distilled at 70-100-180-210°C Fachausschuss Mineralol-und-Brennstoff-Normung fluid catalytic cracking Food and Drug Administration front end octane number fluorescent indicator adsorption flame ionization detector... 

When the methyl-phenyl-pyrazolone is heated with methyl iodide in methano-lie solution, it acts in the form (D), the — NH— group undergoing methy lation, with the formation of the hydriodide of 2,3-dimethyl- l-phenyl-5 Pyrazolone, or antipyrine (F), a drug used (either as the free base or as the... 

The vitamin D3 metabolite la,25-dihydroxycholecalciferol is a lifesaving drug in treatment of defective bone formation due to renal failure. Retrosynthetic analysis (E.G. Baggjolint, 1982) revealed the obvious precursors shown below, a (2-cyclohexylideneethyl)diphenylphosphine oxide (A) and an octahydro-4f/-inden-4-one (B), to be connected in a Wittig-Homer reaction (cf. section 1.5). 

A number of compounds of the type represented by compound A were prepared for evalu ation as potential analgesic drugs Their preparation is described in a retrosynthetic format as shown... 

Physiological responses to prostaglandins encompass a variety of effects Some prostaglandins relax bronchial muscle others contract it Some stimulate uterine con tractions and have been used to induce therapeutic abortions PGEj dilates blood vessels and lowers blood pressure it inhibits the aggregation of platelets and offers promise as a drug to reduce the formation of blood clots... 

Enzymic oxidations at the 7-position of pyrido[2,3-oxygenated derivatives and of the 8-N-oxide have been observed in the metabolism of the pyrido[2,3-e/]pyrimidine analogues of the antiepileptic drug methaqualone (75MI21502, 74MI21500). 

Drugs and other chemicals such as food additives or insecticides foreign to the body undergo enzymatic transformations that result in loss of pharmacological activity detoxification), or lead to the formation of metabolites with therapeutic or toxic effects bioactivation). 

Fumigation with ethylene oxide does indeed lead to a considerable reduction in the germ count (and at the same time destruction of insects), but the process, because of the formation of toxic reaction products (ethylene chlorhydrin, ethylene glycol) has been banned throughout the European Community since 01.01.1990 Ionizing irradiation a declaration of the treatment is obligatory, but such drugs find little acceptance by the public who expect nature s products as such. 

Aluminium chloride Resin manufacture by polymerization of low molecular-weight hydrocarbons Friedel-Crafts reactions to manufacture detergent alkylate, agrochemicals, drugs Irritation due to formation of HCI with moisture... 

It is over three centuries since cinchona bark came into use in European medicine, and no other natural drug has had so much written about it. There are the stories, sometimes legendary, of its discovery by Europeans, vigorous early discussions of its therapeutic value, the destruction of the S. American cinchona trees to meet the demand for bark, the labours of botanical explorers in collecting seed for the formation of plantations, the establishment and development of these plantations in Ceylon, India and Java, the competition between them, the gradual emergence of Java as the world s most important source of supply of cinchona bark, and the development of the manufacture of quinine sulphate in Europe, the United States and the Tropics. ... 

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