Imidazole-pyrazole hybrids: Synthesis,characterization and in-vitro bioevaluation against α-glucosidase enzyme with molecular docking studies |
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| Institution: | 1. Institute of Chemistry, University of the Punjab, Lahore 54590, Pakistan;2. Department of Chemistry, Kinnaird College for Women, Lahore 54000, Pakistan;3. Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan;4. Department of Chemistry, Forman Christian College (A Chartered University), Ferozepur Road, Lahore 54600, Pakistan;1. Department of Chemistry, Kinnaird College for Women, Lahore 54000, Pakistan;2. Department of Biotechnology, Kinnaird College for Women, Lahore 54000, Pakistan;3. Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan;4. Department of Chemistry, Forman Christian College (A Chartered University), Ferozepur Road, Lahore 54600, Pakistan;5. Institute of Chemistry, University of the Punjab, Lahore 54590, Pakistan;1. Jinnah University for Women, 5-C, Nazimabad, Karachi 74600, Pakistan;2. H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan;3. Deparment of Chemistry, Karakoram International University, Gilgit, Pakistan;4. Department of Biochemistry and Biotechnology, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan;5. Department of Biochemistry, Shankar Campus, Abdul Wali Khan University, Mardan, Khyber Pukhtoonkhwa, Pakistan;6. PCSIR Laboratories Complex, Karachi, Shahrah-e-Dr. Salimuzzaman Siddiqui, Karachi 75280, Pakistan;7. Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor D. E., Malaysia;8. Faculty of Applied Science Universiti Teknologi MARA, Shah Alam 40450, Selangor D. E., Malaysia;1. Institute of Chemistry, University of the Punjab, Lahore 54590, Pakistan;2. Applied Chemistry Research Center, PCSIR Laboratories Complex, Lahore, Pakistan;3. Department of Chemistry, Stony Brook University, Long Island, NY 11794-3400, USA;4. Department of Biochemistry and Biotechnology, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan;5. Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan;6. Department of Chemistry, Forman Christian College (A Chartered University), Ferozepur Road, Lahore 54600, Pakistan;7. Department of Chemistry, Kinnaird College for Women, Lahore 54000, Pakistan;1. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt;2. Pharmaceutical Sciences Department, Ibn Sina National College for Medical Studies, Jeddah 21418, Saudi Arabia;3. Pharmacology Department, Faculty of Veterinary, Cairo University, Cairo, Egypt;4. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Assuit 71524, Egypt;5. Anatomy Department, Faculty of Veterinary Medicine, Kafrelshiekh University, Kafrelshiekh, 33516, Egypt;1. Interdisciplinary Research Center in Biomedical Materials, COMSATS Institute of Information Technology, Lahore 54000, Pakistan;2. Faculty of Chemistry, University of Warsaw, Pasteura 1, 02-093 Warsaw, Poland;3. Department of Physicochemical Drug Analysis, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Cracow, Poland;4. Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan;5. Department of Chemistry, King Fahd University of Petroleum and Minerals, Dhahran 31261, Saudi Arabia;6. Department of Chemical Engineering, COMSATS Institute of Information Technology, Lahore 54000, Pakistan;7. Department of Biochemistry & Biotechnology, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan;1. Laboratory of Applied Chemistry & Environment, Faculty of Science, Mohammed First University, Oujda, Morocco;2. Laboratory of Biochemistry and Biotechnology, Faculty of Sciences, Mohammed First University, BP 717, Oujda, 60000, Morocco;3. Institut des Sciences Chimiques de Rennes, UMR 6226 CNRS-Université de Rennes, “Organométalliques: Matériaux et Catalyse”, Campus de Beaulieu, 35042 Rennes, France |
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| Abstract: | Herein, substituted imidazole-pyrazole hybrids (2a-2n) were prepared via a multi component reaction employing pyrazole-4-carbaldehydes (1a-1d), ammonium acetate, benzil and arylamines as reactants. All the new compounds were characterized through their spectral and elemental analyses. Further these compounds were tested against α-glucosidase enzyme. The compounds 2k, 2l and 2n possessed good inhibition potencies, however, compounds 2f (IC50 value: 25.19 ± 0.004 μM) and 2m (IC50 value: 33.62 ± 0.03 μM) were the most effective compounds of the series. Furthermore, molecular docking helped to understand the binding interactions of 2f and 2m with the understudy yeast’s α-glucosidase enzyme. |
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| Keywords: | Multicomponent reactions Tetrasubstituted imidazoles Molecular modeling |
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