Literature DB >> 20926301

Indapamide-like benzenesulfonamides as inhibitors of carbonic anhydrases I, II, VII, and XIII.

Edita Čapkauskaitė1, Lina Baranauskienė, Dmitrij Golovenko, Elena Manakova, Saulius Gražulis, Sigitas Tumkevičius, Daumantas Matulis.   

Abstract

A series of novel 2-chloro-5-[(1-benzimidazolyl- and 2-benzimidazolylsulfanyl)acetyl]benzene-sulfonamides were designed and synthesized. Their binding to recombinant human carbonic anhydrase (hCA) isozymes I, II, VII, and XIII was determined by isothermal titration calorimetry and thermal shift assay. The designed S-alkylated benzimidazole derivatives exhibited stronger binding than the indapamide-like N-alkylated benzimidazoles, with the K(d) reaching about 50-100 nM with drug-targeted hCAs VII and XIII. The cocrystal structures of selected compounds with hCA II were determined by X-ray crystallography, and structural features of the binding event were revealed.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20926301     DOI: 10.1016/j.bmc.2010.09.016

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  4 in total

1.  Direct alkylation of heteroaryls using potassium alkyl- and alkoxymethyltrifluoroborates.

Authors:  Gary A Molander; Virginie Colombel; Valerie A Braz
Journal:  Org Lett       Date:  2011-03-10       Impact factor: 6.005

2.  Intrinsic thermodynamics of ethoxzolamide inhibitor binding to human carbonic anhydrase XIII.

Authors:  Lina Baranauskienė; Daumantas Matulis
Journal:  BMC Biophys       Date:  2012-06-07       Impact factor: 4.778

3.  N-Phenacyldibromobenzimidazoles-Synthesis Optimization and Evaluation of Their Cytotoxic Activity.

Authors:  Anna Kowalkowska; Konrad Chojnacki; Maciej Multan; Jan K Maurin; Edyta Łukowska-Chojnacka; Patrycja Wińska
Journal:  Molecules       Date:  2022-07-07       Impact factor: 4.927

4.  Significant reduction in errors associated with nonbonded contacts in protein crystal structures: automated all-atom refinement with PrimeX.

Authors:  Jeffrey A Bell; Kenneth L Ho; Ramy Farid
Journal:  Acta Crystallogr D Biol Crystallogr       Date:  2012-07-17
  4 in total

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