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Javeria Shaikh
Waqas Jamil
Sehar Zahid
Samreen Zainalabdin



Flavone Hydrazide Sulfonyl derivatives 1-20 has synthesized and structural properties has confirmed by spectroscopic techniques. These compounds were also found to be active against α-glucosidase enzyme. Among these, Compound 6 (IC50=7.5 ± 1.98µM), 9 (IC50=9.2 ± 1.87µM) and 4 (IC50=9.3 ± 1.67µM) showed marvelous inhibition activity.

All the synthesized compounds were subject for in silico studies.

The molecular docking analysis revealed that these molecules have high potential to interact with the enzyme. According to the physicochemical and pharmacokinetics studies these compound have excellent parameters required for drug likeness. The derivatives have ability of GI absorption.

In addition, all the synthesized Flavone Hydrazide derivatives 1-20 were also evaluated for their ant-oxidant (DPPH Radical scavenging) activity. All these computed showed very promising anti-oxidant activity IC50 ranges 15.25-58.38µM respectively.

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[1] L. Chen, D. J. Magliano, and P. Z. Zimmet, “The worldwide epidemiology of type 2 diabetes mellitus - Present and future perspectives,” Nature Reviews Endocrinology, vol. 8, no. 4. pp. 228–236, Apr. 2012. doi: 10.1038/nrendo.2011.183.
[2] M. Finucane et al., “National, regional, and global trends in fasting plasma glucose and diabetes prevalence since 1980: systematic analysis of health examination surveys and epidemiological studies with 370 country-years and 2·7 million participants,” Lancet, vol. 378, pp. 31–40, 2011, doi: 10.1016/S0140.
[3] World Health Organization and International Diabetes Federation, Definition and diagnosis of diabetes mellitus and intermediate hyperglycaemia : report of a WHO/IDF consultation.
[4] Y. Zheng, S. H. Ley, and F. B. Hu, “Global aetiology and epidemiology of type 2 diabetes mellitus and its complications,” Nature Reviews Endocrinology, vol. 14, no. 2. Nature Publishing Group, pp. 88–98, 2018. doi: 10.1038/nrendo.2017.151.
[5] R. Malek, S. Hannat, A. Nechadi, F. Z. Mekideche, and M. Kaabeche, “Diabetes and Ramadan: A multicenter study in Algerian population,” Diabetes Research and Clinical Practice, vol. 150. Elsevier Ireland Ltd, pp. 322–330, Apr. 01, 2019. doi: 10.1016/j.diabres.2019.02.008.
[6] Y. J. Choi and Y.-S. Chung, “Type 2 diabetes mellitus and bone fragility: Special focus on bone imaging,” Osteoporos. Sarcopenia, vol. 2, no. 1, pp. 20–24, 2016, doi: 10.1016/j.afos.2016.02.001.
[7] A. K. Picke, G. Campbell, N. Napoli, L. C. Hofbauer, and M. Rauner, “Update on the impact of type 2 diabetes mellitus on bone metabolism and material properties,” Endocrine Connections, vol. 8, no. 3. BioScientifica Ltd., pp. R55–R70, 2019. doi: 10.1530/EC-18-0456.
[8] R. M. Carrillo-Larco, N. C. Barengo, L. Albitres-Flores, and A. Bernabe-Ortiz, “The risk of mortality among people with type 2 diabetes in Latin America: A systematic review and meta-analysis of population-based cohort studies,” Diabetes. Metab. Res. Rev., vol. 35, no. 4, pp. 1–11, 2019, doi: 10.1002/dmrr.3139.
[9] H. Ali, P. J. Houghton, and A. Soumyanath, “α-Amylase inhibitory activity of some Malaysian plants used to treat diabetes; with particular reference to Phyllanthus amarus,” J. Ethnopharmacol., vol. 107, no. 3, pp. 449–455, 2006, doi: 10.1016/j.jep.2006.04.004.
[10] M. R. Bhandari, N. Jong-Anurakkun, G. Hong, and J. Kawabata, “α-Glucosidase and α-amylase inhibitory activities of Nepalese medicinal herb Pakhanbhed (Bergenia ciliata, Haw.),” Food Chem., vol. 106, no. 1, pp. 247–252, 2008, doi: 10.1016/j.foodchem.2007.05.077.
[11] S. A. Adefegha and G. Oboh, “Inhibition of key enzymes linked to type 2 diabetes and sodium nitroprusside-induced lipid peroxidation in rat pancreas by water extractable phytochemicals from some tropical spices,” Pharm. Biol., vol. 50, no. 7, pp. 857–865, 2012, doi: 10.3109/13880209.2011.641022.
[12] S. Poovitha and M. Parani, “In vitro and in vivo α-amylase and α-glucosidase inhibiting activities of the protein extracts from two varieties of bitter gourd (Momordica charantia L.),” BMC Complement. Altern. Med., vol. 16, no. Suppl 1, pp. 1–8, 2016, doi: 10.1186/s12906-016-1085-1.
[13] O. Trott and A. J. Olson, “AutoDock Vina: Improving the speed and accuracy of docking with a new scoring function, efficient optimization, and multithreading,” J. Comput. Chem., vol. 31, no. 2, p. NA-NA, 2009, doi: 10.1002/jcc.21334.
[14] J. Eberhardt, D. Santos-Martins, A. F. Tillack, and S. Forli, “AutoDock Vina 1.2.0: New Docking Methods, Expanded Force Field, and Python Bindings,” J. Chem. Inf. Model., vol. 61, no. 8, pp. 3891–3898, 2021, doi: 10.1021/acs.jcim.1c00203.
[15] A. Allouche, “Software News and Updates Gabedit — A Graphical User Interface for Computational Chemistry Softwares,” J. Comput. Chem., vol. 32, pp. 174–182, 2012, doi: 10.1002/jcc.
[16] A. M. Dar and S. Mir, “Molecular Docking: Approaches, Types, Applications and Basic Challenges,” J. Anal. Bioanal. Tech., vol. 08, no. 02, pp. 8–10, 2017, doi: 10.4172/2155-9872.1000356.
[17] A. Daina and V. Zoete, “A BOILED-Egg To Predict Gastrointestinal Absorption and Brain Penetration of Small Molecules,” ChemMedChem, pp. 1117–1121, 2016, doi: 10.1002/cmdc.201600182.
[18] A. Daina, O. Michielin, and V. Zoete, “SwissADME: A free web tool to evaluate pharmacokinetics, drug-likeness and medicinal chemistry friendliness of small molecules,” Sci. Rep., vol. 7, Mar. 2017, doi: 10.1038/srep42717.