Sulfonamides and Derivatives

Saccharin is a drug product that consists of saccharin N-isopropyl ester and an impurity standard. Saccharin is a synthetic sweetener that is found in the leaves of the herbaceous perennial S. dulcis, which has been used as a natural sweetener for centuries. Saccharin can be metabolized by humans to form 2-acetic acid and 4-methyl-1,2,3-thiadiazole (MTT) as a byproduct. The metabolite MTT may cause cancer in animals, but this has not been confirmed in humans. The pharmacopoeia specifies the purity of saccharin as 98% or greater. Metabolite standards are also provided for research purposes.

3-[4-(2-Pyridylsulfamoyl)phenyl] sulfasalazine is an analytical standard and a metabolite of sulfasalazine. It is used as a reference compound in the analysis of high purity sulfasalazine by HPLC. 3-[4-(2-Pyridylsulfamoyl)phenyl] sulfasalazine is also used as an impurity in the drug product, API, and drug development. The CAS number for 3-[4-(2-Pyridylsulfamoyl)phenyl] sulfasalazine is 1391062-34-2.

Acetaminophen acetate is a cholinergic amine that binds to the active site of the enzyme acetylcholine esterase, preventing it from breaking down acetylcholine. Acetaminophen is used as a pain reliever and antipyretic agent. It is also used for its anti-inflammatory effects in the treatment of rheumatoid arthritis and other inflammatory conditions. Acetaminophen has been shown to have anticancer properties, which may be due to its ability to bind to cancer cells, inhibit their growth, and induce apoptosis. Acetaminophen acetate is also an acylation reaction product that can be isolated by liquid chromatography in phase with fluorescence properties.

Applications α-Hydroxy Trimethoprim is an impurity of Trimethoprim (T795615), an antibacterial agent that is commonly prescribed in conjunction with Sulfametoxazole (S699086) to treat patients afflicted with urinary tract infections. References Dauber-Osguthorpe, P., et al.: Proteins, 4, 31, (1988); Darrell, J., et al.: J. Clin. Pathol., 21, 202 (1968); Zhanel, G., et al.: Antimicrob. Agents Ch., 44, 1089 (2000)

2-(4-Ethylphenyl)-propanoic acid is a supplement that is used to relieve pain and inflammation. It belongs to the group of non-steroidal anti-inflammatory drugs (NSAIDs). This drug has been shown to be efficacious in the treatment of osteoarthritis, rheumatoid arthritis, and bronchitis. 2-(4-Ethylphenyl)-propanoic acid inhibits both prostaglandin synthesis and leukotriene synthesis by inhibiting cyclooxygenase 1, which converts arachidonic acid into prostaglandins, and 5-lipoxygenase, which converts arachidonic acid into leukotrienes. This drug has also been shown to inhibit COX-2 production in human monocytes. The active form of this drug is metabolized through a number of metabolic transformations including hydrolysis by esterases or glucuronidases, oxidation by cytochrome P450 enzymes,

Oxyclozanide (Oxyclozanid) is a salicylanilide anthelmintic used in grazing animals for fasciola and cestode infestations.