Designing Click One-Pot Synthesis and Antidiabetic Studies of 1,2,3-Triazole Derivatives
In the present study, a new series of 1,2,3-triazole derivatives was synthesized via a click one-pot reaction. The synthesized compounds were found to be active during molecular docking studies against targeted protein 1T69 by using the Molecular Operating Environment (MOE) software. The designed an...
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| Format: | Article |
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MDPI AG
2023-03-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/28/7/3104 |
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| author | Kainat Shafique Aftab Farrukh Tariq Mahmood Ali Sumera Qasim Laila Jafri Hisham S. M. Abd-Rabboh Murefah mana AL-Anazy Saima Kalsoom |
| author_facet | Kainat Shafique Aftab Farrukh Tariq Mahmood Ali Sumera Qasim Laila Jafri Hisham S. M. Abd-Rabboh Murefah mana AL-Anazy Saima Kalsoom |
| author_sort | Kainat Shafique |
| collection | DOAJ |
| description | In the present study, a new series of 1,2,3-triazole derivatives was synthesized via a click one-pot reaction. The synthesized compounds were found to be active during molecular docking studies against targeted protein 1T69 by using the Molecular Operating Environment (MOE) software. The designed and synthesized compounds were characterized by using FT-IR, <sup>1</sup>H-NMR and LC-MS spectra. The synthesized triazole moieties were further screened for their α-amylase and α-glucosidase inhibitory activities. The preliminary activity analysis revealed that all the compounds showed good inhibition activity, ranging from moderate to high depending upon their structures and concentrations and compared to the standard drug acarbose. Both in silico and in vitro analysis indicated that the synthesized triazole molecules are potent for DM type-II. Out of all the compounds, compound K-1 showed the maximum antidiabetic activity with 87.01% and 99.17% inhibition at 800 µg/mL in the α-amylase and α-glucosidase inhibition assays, respectively. Therefore these triazoles may be further used as promising molecules for development of antidiabetic compounds. |
| first_indexed | 2024-03-11T05:29:39Z |
| format | Article |
| id | doaj.art-5b8b7fa5c25043309930f0a401d14494 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-11T05:29:39Z |
| publishDate | 2023-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-5b8b7fa5c25043309930f0a401d144942023-11-17T17:13:35ZengMDPI AGMolecules1420-30492023-03-01287310410.3390/molecules28073104Designing Click One-Pot Synthesis and Antidiabetic Studies of 1,2,3-Triazole DerivativesKainat Shafique0Aftab Farrukh1Tariq Mahmood Ali2Sumera Qasim3Laila Jafri4Hisham S. M. Abd-Rabboh5Murefah mana AL-Anazy6Saima Kalsoom7SA-Center for Interdisciplinary Research in Basic Sciences, International Islamic University, Islamabad 44000, PakistanDepartment of Physics, PMAS-Arid Agriculture University, Rawalpindi 44000, PakistanHealth Services Academy, Islamabad 44000, PakistanDepartment of Pharmacology, College of Pharmacy, Jouf University, Sakaka 72431, Saudi ArabiaDepartment of Life Sciences, Abasyn University, Islamabad Campus, Islamabad 44000, PakistanChemistry Department, Faculty of Science, King Khalid University, P.O. Box 9004, Abha 61413, Saudi ArabiaDepartment of Chemistry, College of Sciences, Princess Nourah bint Abdulrahman University (PNU), P.O. Box 84428, Riyadh 11671, Saudi ArabiaDepartment of Chemistry, PMAS-Arid Agriculture University, Rawalpindi 44000, PakistanIn the present study, a new series of 1,2,3-triazole derivatives was synthesized via a click one-pot reaction. The synthesized compounds were found to be active during molecular docking studies against targeted protein 1T69 by using the Molecular Operating Environment (MOE) software. The designed and synthesized compounds were characterized by using FT-IR, <sup>1</sup>H-NMR and LC-MS spectra. The synthesized triazole moieties were further screened for their α-amylase and α-glucosidase inhibitory activities. The preliminary activity analysis revealed that all the compounds showed good inhibition activity, ranging from moderate to high depending upon their structures and concentrations and compared to the standard drug acarbose. Both in silico and in vitro analysis indicated that the synthesized triazole molecules are potent for DM type-II. Out of all the compounds, compound K-1 showed the maximum antidiabetic activity with 87.01% and 99.17% inhibition at 800 µg/mL in the α-amylase and α-glucosidase inhibition assays, respectively. Therefore these triazoles may be further used as promising molecules for development of antidiabetic compounds.https://www.mdpi.com/1420-3049/28/7/3104triazole derivativesdiabetes mellitusantidiabetic assay molecular docking |
| spellingShingle | Kainat Shafique Aftab Farrukh Tariq Mahmood Ali Sumera Qasim Laila Jafri Hisham S. M. Abd-Rabboh Murefah mana AL-Anazy Saima Kalsoom Designing Click One-Pot Synthesis and Antidiabetic Studies of 1,2,3-Triazole Derivatives Molecules triazole derivatives diabetes mellitus antidiabetic assay molecular docking |
| title | Designing Click One-Pot Synthesis and Antidiabetic Studies of 1,2,3-Triazole Derivatives |
| title_full | Designing Click One-Pot Synthesis and Antidiabetic Studies of 1,2,3-Triazole Derivatives |
| title_fullStr | Designing Click One-Pot Synthesis and Antidiabetic Studies of 1,2,3-Triazole Derivatives |
| title_full_unstemmed | Designing Click One-Pot Synthesis and Antidiabetic Studies of 1,2,3-Triazole Derivatives |
| title_short | Designing Click One-Pot Synthesis and Antidiabetic Studies of 1,2,3-Triazole Derivatives |
| title_sort | designing click one pot synthesis and antidiabetic studies of 1 2 3 triazole derivatives |
| topic | triazole derivatives diabetes mellitus antidiabetic assay molecular docking |
| url | https://www.mdpi.com/1420-3049/28/7/3104 |
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