B13 analogues are being considered as therapeutic agents for cancer cells, since B13 is a ceramide analogue and inhibits ceramidase to promote apoptosis in cancer cells. B13 sulfonamides are assumed to have biological activity similar to B13, since they are made by bioisosterically substituting the carboxyl moiety of B13 with sulfone group. Twenty B13 sulfonamides were evaluated for their in vi...

,YIn a previous study (Sevag and Gots, 1948) on the effects of various drugs on the pneumococcal dehydrogenase systems it was found that, whereas acriflavine, atabrine, propamidine, and optochin could inhibit these systems, high concentrations of sulfonamides had no effect. Other investigators (Mellon aind Bambas, 1937; Brazda and Rice, 1942; Fox, 1942; Clifton and Loewinger, 1943) have reporte...

Sulfonamide drugs enter the environment in different ways, eg through wastewater, creating the potential risk of the generation of drug resistant strains of microorganisms. This risk increases when drugs are resistant to degradation and remain in the environment for a long time. Therefore, it is particularly important to know biodegradability of sulfa drugs since the literature data on this sub...

Plant activators are agrochemicals that protect crops from diseases by activating the plant immune system. To isolate lead compounds for use as practical plant activators, we screened two different chemical libraries composed of various bioactive substances by using an established screening procedure that can selectively identify immune-priming compounds. We identified and characterized a group...

Carbonic anhydrases (CAs, EC 4.2.1.1) are metalloenzymes which catalyze the hydration of carbon dioxide to bicarbonate and protons. Many pathogenic bacteria encode such enzymes belonging to the α-, β-, and/or γ-CA families. In the last decade, enzymes from some of these pathogens, including Legionella pneumophila, have been cloned and characterized in detail. These enzymes were shown to be effi...

A new amidation of azoxybenzenes with sulfonamides catalyzed by a rhodium(III) salt has been developed. This sulfonamidation proceeds efficiently under mild reaction conditions to generate new C– N bonds through C–H bond activation and functionalization, affording the corresponding 2-sulfonamidoazoxybenzenes in good yields with high regioselectivity.

Commercial brilliant green (BG)-sulfa agar was found to be nonselective toward a test series of Enterobacteriaceae. Various formulations of BG were prepared by using Trypticase soy agar (BBL) as a base. Results were more reproducible when BG dye was added after sterilization than before. Sulfonamides improved selectivity as compared with brilliant green alone. Sulfanilamide (SN) was slightly mo...

We report a series of 4-sulfamoylphenyl-ω-aminoalkyl ethers as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. The structure-activity relationship was drawn for the inhibition of four physiologically relevant isoforms: hCA I, II, IX, and XII. Many of these compounds were highly effective, low nanomolar inhibitors of all CA isoforms, whereas several isoform-selective were also identified. X-ray ...

We investigated a series of sulfonamide boronic acids that resulted from the merging of two unrelated AmpC β-lactamase inhibitor series. The new boronic acids differed in the replacement of the canonical carboxamide, found in all penicillin and cephalosporin antibiotics, with a sulfonamide. Surprisingly, these sulfonamides had a highly distinct structure-activity relationship from the previousl...