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...

Acetylcholine activates nicotinic acetylcholine receptors (nAChRs) by binding to an extracellular site located at the interface of two adjacent subunits. In contrast, recent studies have provided evidence that positive allosteric modulators (PAMs) such as TQS (4-(naphthalen-2-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide) and allosteric agonists such as 4BP-TQS (4-(4-bromophe...

EB (electron beam) irradiation of sulfonamide within a beta-cyclodextrin (beta-CD) inclusion complex in the solid state induced the solvent-free Fries rearrangement, which proceeded at a shorter reaction time with reversed regioselectivity by inclusion into the beta-CD, compared with that of sulfonamide crystals; the beta-CD as a restricted nanospace had a large effect on the reactivity and reg...

www.experimentjournal.com 1254 Synthesis, biological activity and docking studies of N,N'-(3S,4S)bis(3,4-disubstituted pyrrolidine)-1-sulfonamide derivatives as β-gluscosidase inhibitors Abstract Starting with L-tartaric acid the chiral 3,4-disubstituted pyrrolidine analogue sulfonamide derivatives were prepared. These compounds were examined for anti-bacterial and anti-fungal activity. Further...

Specific isoforms from the carbonic anhydrase (CA) family of zinc metalloenzymes have been associated with a variety of diseases. Isoform-specific carbonic anhydrase inhibitors (CAIs) are therefore a major focus of attention for specific disease treatments. Classical CAIs, primarily sulfonamide-based compounds and their bioisosteres, are examined as antiglaucoma, antiepileptic, antiobesity, ant...