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Benzamide sulfonamide derivatives: potent inhibitors of carbonic anhydrase-II

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Abstract

Benzamide sulfonamide and its derivatives were identified as potent inhibitors of carbonic anhydrase-II (bovine carbonic anhydrase-II (bCA-II) and human recombinant carbonic anhydrase-II (hCA-II)) with IC50 values 0.06–0.28 μM and 0.09–0.58 μM, respectively. Different kinetics parameter, such as V max, K m , and K i , were determined. Molecular docking simulation studies on the lead compounds were carried out by AutoDock Vina docking software. The compounds were also evaluated for their cytotoxicity against 3T3 (Normal Cell Lines Mouse Fibroblast) cell line. All the compounds have shown non-cytotoxic effect toward 3T3 cell lines. This study has identified novel scaffolds for further hit-to-lead optimization for the discovery of effective drugs against carbonic anhydrase-II-associated disorder, such as glaucoma, leukemia, cystic fibrosis, and epilepsy.

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Acknowledgment

The authors gratefully acknowledge the HEC (Higher Education Commission of Pakistan), for financial support.

Author contributions

The manuscript was written through the contributions of all authors. All authors have given approval to the final version of the manuscript.

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Authors and Affiliations

  1. H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, 75270, Pakistan

    Muhammad Saleem,  Atia-tul-Wahab, Waqasuddin Khan & M. Iqbal Choudhary

  2. Department of Chemistry, Quaid-i-Azam University, Islamabad, 45320, Pakistan

    Aamer Saeed

  3. Department of Chemistry, COMSATS Institute of Information Technology, Abbottabad, 22060, Pakistan

    Ajmal Khan

  4. Center of Excellence for Advanced Materials Research (CEAMR), Department of Chemistry, Faculty of Science, King Abdulaziz University, Jeddah, 21589, Saudi Arabia

    Sher Bahadar Khan

  5. Department of Biochemistry, Faculty of Science, King Abdulaziz University, Jeddah, 21412, Saudi Arabia

    Sanaullah Abbasi & M. Iqbal Choudhary

  6. Department of Chemistry, Ghazi University, Dera Ghazi Khan, 32200, Punjab, Pakistan

    Muhammad Saleem

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  1. Muhammad Saleem
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  2. Aamer Saeed
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  3. Atia-tul-Wahab
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Correspondence to Aamer Saeed or M. Iqbal Choudhary.

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Saleem, M., Saeed, A., Atia-tul-Wahab et al. Benzamide sulfonamide derivatives: potent inhibitors of carbonic anhydrase-II. Med Chem Res 25, 438–448 (2016). https://doi.org/10.1007/s00044-015-1493-7

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  • DOI: https://doi.org/10.1007/s00044-015-1493-7

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