1. In cultures of Staphylococus aureus in a synthetic medium nicotinamide and cozymase were shown to block the bacteriostatic action of chemically unrelated sulfonamide drugs as well as the chemically related compound sulfapyridine. The antibacterial properties of organic dyes totally unrelated to the sulfonamide compounds (methylene blue and thionine) were also nullified by the addition of coz...

The mechanism of sulfonamide cleavage of PNU-109112, a potent HIV-1 protease inhibitor, by glutathione-S-transferase (GST) was investigated in the presence of reduced GSH. GST-catalyzed sulfonamide cleavage takes place via the nucleophilic attack of GSH on the pyridine moiety of the substrate with formation of the GS-para-CN-pyridinyl conjugate, the corresponding amine, and sulfur dioxide. Stru...

DHPS (dihydropteroate synthase) catalyses an essential step in the biosynthesis of folic acid and is the target for the sulfonamide group of antimicrobial drugs. In the present paper we report two crystal structures of DHPS from the respiratory pathogen Streptococcus pneumoniae: the apoenzyme at 1.8 A (1 A=0.1 nm) resolution and a complex with DHPP (6-hydroxymethyl-7,8-dihydropterin monophospha...

In view of recent reports suggesting a possible relationship between ionization and the bacteriostatic action of the sulfonamides, it was thought that it might be of interest to study the activity of several sulfonamide derivatives as well as that of p-aminobenzoic acid under a widely varying pH range of the culture medium. Therefore, experiments were carried out with a strain of Staph. aureus ...

Co(II); Zn(II) and Cu(II) complexes of two new sulfonamide carbonic anhydrase (CA) inhibitors, derivatives of thienothiopyran-2-sulfonamide, were prepared and characterized by analytic, spectroscopic, magnetic and conductimetric measurements. The new complexes are more potent CA inhibitors than the parent sulfonamides, with IC(50) values around 0.1 nM, against isozyme CA II.

The design of novel supramolecular synthons for functional groups relevant to drugs is an essential prerequisite for applying crystal engineering in the development of novel pharmaceutical cocrystals. It has been convincingly shown over the past decade that molecular level control and modulation can influence the physicochemical properties of drug cocrystals. Whereas considerable advances have ...

Herein, a straightforward synthesis of novel class polymers, that is, poly(N-(4-vinylphenyl)sulfonamide)s, and their monomers is reported. A set with varying electron densities, fine-tuned by different substituents on the aromatic sulfonamide moiety, polymerized free radical polymerization featuring low molar masses (2300 ≤ Mn 3200 g mol−1) dispersities (1.15 Đ 1.47). Further, post-polymerizati...