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Alpha-glucosidase inhibition and molecular docking studies of 1,2- benzothiazine 1,1-dioxide based carbohydrazides

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dc.contributor.author Saddique, Furqan Ahmad
dc.contributor.author Ahmad, Matloob
dc.contributor.author Ashfaq, Usman Ali
dc.contributor.author Ahmad, Mirza Nadeem
dc.contributor.author Anjum, Muhammad Naveed
dc.contributor.author Mohsin, Noor-ul-Amin
dc.contributor.author Aslam, Sana
dc.date.accessioned 2022-12-05T04:12:44Z
dc.date.available 2022-12-05T04:12:44Z
dc.date.issued 2019-11-09
dc.identifier.citation Saddique, F. A., Ahmad, M., Ashfaq, U. A., Ahmad, M. N., Anjum, M. N., Mohsin, N. U. A., & Aslam, S. (2019). Alpha-glucosidase inhibition and molecular docking studies of 1, 2-benzothiazine 1, 1-dioxide based carbohydrazides. Pakistan Journal of Pharmaceutical Sciences, 32. en_US
dc.identifier.issn 1011-601X
dc.identifier.uri http://142.54.178.187:9060/xmlui/handle/123456789/14594
dc.description.abstract Diabetes mellitus is a chronic disease in which the infected cells do not have the ability to produce sufficient amount of insulin that results in the abnormality of carbohydrates metabolism and an increase in blood glucose level. Long time exposure to diabetes mellitus results in failure or dysfunction of different organs like kidneys, nerves, heart, eyes, etc. A common practice to cure diabetes is the use of α-glucosidase inhibitors which help in lowering the blood glucose level. We presented 1,2-benzothiazine 1,1-dioxide derivatives as novel and more potent α-glucosidase inhibitors via their in vitro and in silico screenings. Excellent enzyme inhibitions were observed for compounds 2, 8, 10 and 12 having IC50 values of 6.91, 14.0, 4.2, 5.9 and 29.2µM respectively which were found better than the reference acarbose (IC50 =38.31µM). Molecular docking studies suggested high binding energies and good binding interactions of these compounds with the active site residues of the receptor protein. A good agreement was found between the results of both modes of evaluation. Moreover, the envisioned candidates have a good potential to treat diabetes. en_US
dc.language.iso en en_US
dc.publisher Karachi: Faculty of Pharmacy & Pharmaceutical Sciences, Karachi en_US
dc.subject 1,2-benzothiazine en_US
dc.subject molecular docking en_US
dc.subject α-glucosidase en_US
dc.subject hyperglycemia en_US
dc.subject diabetes en_US
dc.title Alpha-glucosidase inhibition and molecular docking studies of 1,2- benzothiazine 1,1-dioxide based carbohydrazides en_US
dc.type Article en_US


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