Pharmaceuticals sulfonamides

This is a traditional titration that is still often used to determine compounds containing primary amino groups on the aromatic ring, with the endpoint being monitored with a Pt indicator electrode. This method, applied to the determination of pharmaceuticals (sulfonamide-based compounds, benzocaine, procaine, etc.), is rapid, and the results are in good agreement with official methods of analysis. ... 

Cyclothia2ide [2259-96-3] is another example of a duorine-free pharmaceutical (diuretic, antihypertensive) based on y -chloroduoroben2ene [625-98-9] where duorine activation is subsequentiy provided by two sulfonamide groups (156). 

Sulfur dioxide, sulfites, and metabisulfites have had extensive use as antimicrobial preservatives in the food industry. In pharmaceuticals they have had a dual role, acting as preservatives and antioxidants. The sulfa dmgs, or sulfonamides, the first effective chemotherapeutic agents to be employed... 

In 1975, SAR studies involving actinonin investigated an analogue in which the orientation of the Pl -P2 amide bond was reversed (13), but the compound was found to lack antibacterial activity. Since then, however, descriptions of some /i-aminohydroxamic acids and /i-amino-A-formyl-A-hydroxylamines as PDF inhibitors have appeared in the patent literature. Patent applications from Senju [97] and De Novo [98] pharmaceuticals cover Pl -P2 amides (14), ureas (15, 16) and sulfonamides (17). 

Farng and Nelson [1] applied the capillary method to the determination of the diffusion coefficient of salicylic acid in the presence of polyelectrolytes. The reported variability in terms of the coefficient of variation ranged from 0.89% to 8.3%. Stout et al. [2] showed the tube method to be useful for determining diffusion coefficients of water-insoluble pharmaceuticals such as sulfonamides and steroids. The coefficient of variation associated with the diffusion coefficient for sulfisoxazole is 5.5%. 

Among pharmaceuticals, antibiotics have become of special concern in recent years. The reason is that these substances are continuously being introduced into the environment and may spread and maintain bacterial resistance in the different compartments. Sulfonamides are very commonly used antimicrobials in humans but mainly in veterinary medicine, due to their broad spectrum of activity and low cost, being the second most widely used veterinary antibiotic in the EU. Their occurrence has been reported in all kinds of water matrices their high excretion rates (after their intake by humans of livestock) and high water solubility make them very ubiquitous and persistent pollutants in the environment. 

Nieto A, Borrull F, Marce RM, Pocurull E (2007) Selective extraction of sulfonamides, macrolides and other pharmaceuticals from sewage sludge by presurized liquid extraction. J Chromatogr A 1174 125-131... 

Treatment of 2-benzoylpyridine 81 with p-toluene-sulfonamide gave 1-amino-2-benzoylpyridinium tosylate 82 (X = OTs), which was cyclized with formamide in the presence of triethylamine hydrobromide to give 83 (82FRP2486942). The reaction of the perchlorate 82 (X = C104) with urea in polyphosphoric acid afforded 3-hydroxy-l-phenylpyrido[2,l-/][l,2,4]triazinium perchlorate 84. Treatment of this salt with base led to the zwitterionic l-phenylpyrido[2,l-/][l,2,4]triazin-5-ium-3-olate 85 (86JHC375). Pharmaceutical compositions contain 83 (82FRP2486942). 

Sulfa- dimethoxine o / —, N—l H N— )—S02NH— Veterinary medicine Human medicine - US streams 0.06 pg L 1 [20] - GW of a landfill from waste pharmaceutical production 5 mg L 1 (total sulfonamides) [23] Non degradable in sewage treatment... 

Fig. 1 Main entrance pathways of sulfonamides (and pharmaceutical products) into the environment...

Thiele-Bmhn S., T. Seibicke, H.-R. Schulten, and P. Leinweber (2004). Sorption of sulfonamide pharmaceutical antibiotics on whole soils and particle-size fractions. Journal of Environmental Quality 33 1331-1342. 

It is of historical interest that Fowler s solution, which contains 1% potassium arsenite, was widely used as a medicine for many conditions from the eighteenth century through the mid-twentieth century. Organic arsenicals were the first pharmaceutical antimicrobials and were widely used for the first half of the twentieth century until supplanted by sulfonamides and other more effective and less toxic agents. 

Some 10,000 structurally dilferent sulfonamides have been synthesized as a result of the discovery of the antibacterial properties of sulfanilamide. The practice of synthesizing numerous structurally related compounds in an elfort to find some that are more efficient or have fewer side effects than those already available is very important to the pharmaceutical industry. However, as is usually the case, of the many known sulfonamides only about thirty have the proper balance of qualities to be clinically useful. 

H. Salomies, Quantitatives HPTLC of Sulfonamides in Pharmaceutical preparations, Dr. Alfred Huethig Publishers, 1993. 

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