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Carbonic anhydrase inhibitors of primary sulfonamide type, RSO(2)NH(2), have clinical applications as diuretics, antiglaucoma, antiepileptic, antiobesity and antitumor drugs. Here we investigated inhibition of two human cytosolic isozymes, hCA I and II, with a series of secondary/tertiary sulfonamides, incorporating tosyl moieties (CH(3)C(6)H(4)SO(2)NR1R2). Most compounds inhibited both isoforms in low micromolar range, with inhibition constants between 0.181-6.01 μM against hCA I, and 0.209-0.779 μM against hCA II, respectively. These findings point out that substituted benzenesulfonamides may be used as leads for generating interesting CAIs probably possessing a distinct mechanism of action compared to primary sulfonamides. Indeed, classical RSO(2)NH(2) inhibitors bind in deprotonated form to the Zn(II) ion from the CA active site and participate in many other favorable interactions with amino acid residues lining the cavity. The secondary/tertiary sulfonamides cannot bind to the zinc due to steric hindrance and probably are accommodated at the entrance of the active site, in coumarin binding-site.

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Studies on the lethal effects of plants on harmful microorganisms have made them an important and valuable resource for health. Turkey, wherefore the junction center of three phytogeographic regions, is home to numerous medicinal and aromatic plants with its rich flora. In this study, antimicrobial activity of hexane, ethylacetate, methanol and water extracts of aerial parts of L. canescens, which has known as "Topajdarbaşı" in Turkey, was investigated. Plant samples were collected from Pöske Mount in Erzincan. Antimicrobial activities of extracts were evaluated using disc diffusion method against Gram-negative bacterias (Pseudomonas aeruginosa, Klebsiella pneumoniae, colistin-resistant Escherichia coli, Escherichia coli) and Gram-positive bacterias (Enterococcus faecalis, Staphylococcus aureus, Streptococcus pneumoniae). To conclude, hexane, ethylacetate and methanol extracts of L. canescens showed considerable antimicrobial activity against S.aureus, E.faecalis, S.pneumoniae strains.

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