Design and development of 5-(4H)-oxazolones as potential inhibitors of human carbonic anhydrase VA: towards therapeutic management of diabetes and obesity

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dc.contributor.author Mahapatra, Amarjyoti Das
dc.contributor.author Queen, Aarfa
dc.contributor.author Yousuf, Mohd
dc.contributor.author Khan, Parvez
dc.contributor.author Hussain, Afzal
dc.contributor.author Rehman, Md. Tabish
dc.contributor.author Alajmi, Mohamed F.
dc.contributor.author Datta, Bhaskar
dc.contributor.author Hassan, Md. Imtaiyaz
dc.date.accessioned 2020-12-02T15:27:05Z
dc.date.available 2020-12-02T15:27:05Z
dc.date.issued 2020-11
dc.identifier.citation Mahapatra, Amarjyoti Das; Queen, Aarfa; Yousuf, Mohd; Khan, Parvez; Hussain, Afzal; Rehman, Md. Tabish; Alajmi, Mohamed F.; Datta, Bhaskar and Hassan, Md. Imtaiyaz, "Design and development of 5-(4H)-oxazolones as potential inhibitors of human carbonic anhydrase VA: towards therapeutic management of diabetes and obesity", Journal of Biomolecular Structure and Dynamics, DOI: 10.1080/07391102.2020.1845803, Nov. 2020. en_US
dc.identifier.issn 0739-1102
dc.identifier.issn 1538-0254
dc.identifier.uri https://doi.org/10.1080/07391102.2020.1845803
dc.identifier.uri https://repository.iitgn.ac.in/handle/123456789/5908
dc.description.abstract Inhibitors of carbonic anhydrase (CAIs) hold promise for addressing various diseases, including cancer, diabetes, and other metabolic syndromes. CAV is the only isoform present in the mitochondria and is considered a potential drug target for obesity. In this work, we have developed C2, and C4 substituted oxazole-5(4H)-one derivatives as a new scaffold for the selective inhibition of human carbonic anhydrase VA (hCAVA). Synthesized compounds were characterized by 1H NMR, 13C NMR, and LC-MS mass spectrometry and subsequently evaluated for in vitro hCAVA inhibition. Two compounds, 4 and 5 showed a considerably higher binding affinity for hCAVA in comparison to the hCAII. Further, cell-based studies showed that these compounds decrease the expression of CAVA and GLUT4 in adipocytes and non-toxic to HEK293 cells. The present work opens a platform for the use of oxazole-5(4H)-ones and holds promise for further refinement of potent and selective hCAVA inhibitors.
dc.description.statementofresponsibility by Amarjyoti Das Mahapatra, Aarfa Queen, Mohd Yousuf, Parvez Khan, Afzal Hussain and Md. Tabish Rehman
dc.language.iso en_US en_US
dc.publisher Taylor and Francis en_US
dc.subject Carbonic Anhydrase Inhibitors en_US
dc.subject Carbonic Anhydrase VA en_US
dc.subject Oxazolone Derivatives en_US
dc.subject Obesity en_US
dc.subject Drug Discovery en_US
dc.title Design and development of 5-(4H)-oxazolones as potential inhibitors of human carbonic anhydrase VA: towards therapeutic management of diabetes and obesity en_US
dc.type Article en_US
dc.relation.journal Journal of Biomolecular Structure and Dynamics


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