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Publikācija: 5-Substituted-Benzylsulfanyl-Thiophene-2-Sulfonamides with Effective Carbonic Anhydrase Inhibitory Activity: Solution and Crystallographic Investigations

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Publikācijas valoda English (en)
Nosaukums oriģinālvalodā 5-Substituted-Benzylsulfanyl-Thiophene-2-Sulfonamides with Effective Carbonic Anhydrase Inhibitory Activity: Solution and Crystallographic Investigations
Pētniecības nozare 1. Dabaszinātnes
Pētniecības apakšnozare 1.4. Ķīmija
Autori Jekaterīna Ivanova
Agnese Balode
Raivis Žalubovskis
Janis Leitans
Andris Kazaks
Daniela Vullo
Kaspars Tārs
Claudiu T. Supuran
Atslēgas vārdi Carbonic anhydrase | Inhibitor | Mercaptan | Thiophene-2-sulfonamide
Anotācija A series of 5-substituted-benzylsulfanyl-thiophene-2-sulfonamides was prepared by reacting 5-bromo-thiophene-2-sulfonamide with 5-substituted-benzyl mercaptans. The new compounds were investigated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. The cytosolic human (h) isoforms hCA I was poorly inhibited by the new sulfonamides (KIs in the range of 683-4250nM), whereas hCA II, and the transmembrane, tumor associated isoforms hCA IX and XII were effectively inhibited in the subnanomolar-nanomolar range. A high resolution X-ray crystal structure of the adduct of hCA II with one of the new sulfonamides allowed us to rationalize the excellent inhibitory activity of these heterocyclic sulfonamides.
DOI: 10.1016/j.bmc.2016.11.045
Hipersaite: http://www.sciencedirect.com/science/article/pii/S0968089616311166 
Atsauce Ivanova, J., Balode, A., Žalubovskis, R., Leitans, J., Kazaks, A., Vullo, D., Tārs, K., Supuran, C. 5-Substituted-Benzylsulfanyl-Thiophene-2-Sulfonamides with Effective Carbonic Anhydrase Inhibitory Activity: Solution and Crystallographic Investigations. Bioorganic and Medicinal Chemistry, 2017, Vol.25, Iss.3, 857.-863.lpp. ISSN 0968-0896. Pieejams: doi:10.1016/j.bmc.2016.11.045
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ID 24048