Replacing sulfa drugs with novel DHPS inhibitors

Granulopenia and Sulfa Drugs

Synthesis of Novel Mutual Pro-drugs by coupling of Ibuprofen (NSAID) with Sulfa drugs

Non-steroidal anti-inflammatory drugs (NSAIDs) commonly used for the treatment of chronic inflammatory diseases suffering from several undesired side effects, the most important being gastrointestinal (GI) irritation and ulceration. The Pro-drug designing is one of the several strategies used to overcome this drawback. However, mutual pro-drug concept also can be exploited for this purpose. The...

Sulfa Drugs as Inhibitors of Carbonic Anhydrase: New Targets for the Old Drugs

Sulfa drugs are well-known antibacterial agents containing N-substituted sulfonamide group on para position of aniline ring (NH2RSO2NHR'). In this study 2,4-dichloro-1,3,5-triazine derivatives of sulfa drugs, sulfamerazine (1b), sulfaquinoxaline (2b), sulfadiazine (3b), sulfadimidine (4b), and sulfachloropyrazine (5b) (1a-5a) were synthesized and characterized. Their carbonic anhydrase inhibiti...

Methylfolate Trap Promotes Bacterial Thymineless Death by Sulfa Drugs

The methylfolate trap, a metabolic blockage associated with anemia, neural tube defects, Alzheimer's dementia, cardiovascular diseases, and cancer, was discovered in the 1960s, linking the metabolism of folate, vitamin B12, methionine and homocysteine. However, the existence or physiological significance of this phenomenon has been unknown in bacteria, which synthesize folate de novo. Here we i...

Adverse reactions to sulfa drugs: implications for malaria chemotherapy.

National adverse drug reaction registers in Sweden and the United Kingdom provided data on the type, severity and frequency of reported adverse reactions attributed to sulfa drugs. Reactions to the ten principal drugs were examined in terms of their half-lives and usual indications for use. Of 8339 reactions reported between 1968 and 1988, 1272 (15%) were blood dyscrasias, 3737 (45%) were skin ...