Basic drugs sources

Source From The use of organic modifiers in ion exchange chromatography on alumina. The separation of basic drugs, in Chromatographia. ... 

Fig. 3 Hydrophilic interaction CEC separation of basic drugs spiked in human serum. Colunm fused-silica capillary, 27 cm (20 cm packed with 5 p.m, 300 A PolySULFOETHYL A particles). Mobile phase 80% v/v acetonitrile in 100 mM TEAP buffer. TEAP buffer at pH 2.8. Applied voltage 10 kV. Injection 0.5 psi for 90 sec. Temperature 25°C. Detection UV at 214 nm. Concentration of drugs 40 p,g/ml. Solutes 1, amo-barbital 2, phenobarbital 3, barbital 4, caffeine 5, sulfanilamide 6, theophylline 7, 2,4-dimethylquinoline 8, propranolol. Source From Determination of basic pharmaceuticals in human serum by hydrophilic interaction capilary electrochromatography, in Electrophoresis.

The antimalarial properties of quinine (C20H24N2O2) saved thousands of lives during construction of the Panama Canal. This substance is a classic example of a valuable drug sourced from tropical forests. Both N atoms are qh o basic, but the N (blue) of the 3° amine group is far more basic (pX, = 5.1) than the N within the aromatic ring system (pX, = 9.7). (a) A saturated solution of quinine in water is 1 1.6X 10 M. What is the pH of this solution ... 

Source Moore, C. M. "Solid Phase Cation Exchange Extraction of Basic Drugs from the Urine of Racing Greyhounds." Journal of the Forensic Science Society, 301990,123-129. 

Source Yawney J., et al. "A General Screening Method for Acid, Neutral, and Basic Drugs in Whole Blood Using the Oasis MCX > Column." Journal of Analytical Toxicology, 26 2002,325-332. 

More than 4,000 years old, traditional Chinese medicine continues to be widely practiced in China and in western countries. Traditional Chinese medicine teaches that good health is the result of harmony and balance between five basic elements earth, water, fire, wood and metal. Also important to health are the two types of energy Yin and Yang, constituting a vital substance that circulates through the body. Drug therapy has been one of the means used in Chinese medicine to keep these elements and the flow of energy in balance. Many of the same herbs used thousands of years ago in China could be the source of new pharmaceuticals in Western medicine... 

Basic and clinical research provides a continuous flow of biomedical information that enables practitioners to use medications more effectively and safely. The editors, authors, and publisher of this book have made every effort to ensure accuracy of information provided. However, it is the responsibility of all practitioners to assess the appropriateness of published drug therapy information, especially in light of the specific clinical situation and new developments in the field. The editors and authors have taken care to recommend dosages that are consistent with current published guidelines and other responsible literature. However, when dealing with new and unfamiliar drug therapies, students and practitioners should consult several appropriate information sources. 

Source Opalinska JB, Gewirtz AM. Nucleic-acid therapeutics basic principles and recent applications, Nature Reviews Drug Discovery 1 503-514 (2002). 

There are five basic sources of pharmaceuticals. By dollar value of products, fermentation is probably the most important, whereas by tonnage, chemical synthesis is dominant. Fermentation is used for antibiotics such as penicillins and tetracyclines. Chemical synthesis provides drugs such as the psychotropics and antihistamines. Animal extracts provide hormones. Biological sources lead to vaccines and serums. Vegetable extracts provide steroids and alkaloids. The top ten pharmaceutical companies in order of revenues are the following Merck, Pfizer, Bristol-Myers Squibb, Johnson ... 

Tertiary benzylic nitriles are useful synthetic intermediates, and have been used for the preparation of amidines, lactones, primary amines, pyridines, aldehydes, carboxylic acids, and esters. The general synthetic pathway to this class of compounds relies on the displacement of an activated benzylic alcohol or benzylic halide with a cyanide source followed by double alkylation under basic conditions. For instance, 2-(2-methoxyphenyl)-2-methylpropionitrile has been prepared by methylation of (2-methoxyphenyl)acetonitrile using sodium amide and iodomethane. In the course of the preparation of a drug candidate, the submitters discovered that the nucleophilic aromatic substitution of aryl fluorides with the anion of a secondary nitrile is an effective method for the preparation of these compounds. The reaction was studied using isobutyronitrile and 2-fluoroanisole. The submitters first showed that KHMDS was the superior base for the process when carried out in either THF or toluene (Table I). For example, they found that the preparation of 2-(2-methoxyphenyl)-2-methylpropionitrile could be accomplished h... 

Without penetrating the whole area of critical drug evaluation, which would merit a chapter of its own in this book, there are a few basic questions you will have to ask in relation to any source of drug information ... 

This morning Td like to address basic medicinal chemistry, and specifically, how to manipulate drugs from natural sources. Biosynthetic engineering has recently been exploited in antibacterial drug discovery, but can also be applied to anticancer drugs, antiviral drugs, and others. 

---