Primary mono- and bis-sulfonamides obtained via regiospecific sulfochlorination of N-arylpyrazoles: inhibition profile against a panel of human carbonic anhydrases.

A diverse set of mono- and bis-sulfonamide was obtained via a direct, chemoselective sulfochlorination of readily available yet hitherto unexplored N-arylpyrazole template. Biochemical profiling of compounds thus obtained against a panel of human carbonic anhydrases (CA I, CA II, CA IV and CA VII) revealed a number of leads that are promising from the isoform selectivity prospective and exhibit potent inhibition profile (from nanomolar to micromolar range). The observed SAR trends have been rationalized by docking of selected compounds into the active site of all four isoforms.

[Nosospecific anxiety and a spectrum of anxiolytic activity of psychotropic drugs].

The article discusses the pathogenetic mechanisms of anxiety in different psychiatric disorders. The influence of anxiety on the course, pharmacotherapeutic treatment with respect to the pathogenesis and the possible neurochemical imbalance in the definite type of anxiety are discussed. An anti-anxiety effect in the action of psychotropic drugs is described.