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Open AccessArticle

Synthesis of Chromen-4-One-Oxadiazole Substituted Analogs as Potent β-Glucuronidase Inhibitors

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Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi Arabia
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Department of Chemistry, Hazara University, Mansehra 21300, Khyber Pakhtunkhwa, Pakistan
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Natural and Medical Sciences Research Center, University of Nizwa, P.O. Box 33, Birkat Al Mauz, Nizwa 616, Sultanate of Oman
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Department of Chemistry, COMSATS Institute of Information Technology, University Road, Abbottabad 22060, KPK, Pakistan
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Department of Computer Information Systems, College of Computer Science & Information Technology, Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi Arabia
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Department of Neuroscience Research, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 3144, Saudi Arabia
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Faculty of Pharmacy, Universiti Teknologi MARA Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor D.E., Malaysia
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Atta-ur-Rahman Institute for Natural Products Discovery (AuRIns), Universiti Teknologi MARA Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor D.E., Malaysia
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Department of Pharmaceutical Chemistry, Kulliyyah of Pharmacy, International Islamic University Malaysia, 25200 Kuantan, Pahang DM, Malaysia
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Department of Biomedical Science, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, 43400 Serdang, Selangor, Malaysia
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Halal Institute Research Institute, Universiti Putra Malaysia, 43400 Serdang, Selangor, Malaysia
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Authors to whom correspondence should be addressed.
Molecules 2019, 24(8), 1528; https://doi.org/10.3390/molecules24081528
Received: 26 December 2018 / Revised: 23 January 2019 / Accepted: 2 February 2019 / Published: 18 April 2019
(This article belongs to the Section Medicinal Chemistry)
Chromen-4-one substituted oxadiazole analogs 119 have been synthesized, characterized and evaluated for β-glucuronidase inhibition. All analogs exhibited a variable degree of β-glucuronidase inhibitory activity with IC50 values ranging in between 0.8 ± 0.1–42.3 ± 0.8 μM when compared with the standard d-saccharic acid 1,4 lactone (IC50 = 48.1 ± 1.2 μM). Structure activity relationship has been established for all compounds. Molecular docking studies were performed to predict the binding interaction of the compounds with the active site of enzyme. View Full-Text
Keywords: chromen-4-one; oxadiazole; synthesis; β-glucuronidase inhibition; molecular docking; SAR chromen-4-one; oxadiazole; synthesis; β-glucuronidase inhibition; molecular docking; SAR
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MDPI and ACS Style

Taha, M.; Rahim, F.; Ali, M.; Khan, M.N.; Alqahtani, M.A.; Bamarouf, Y.A.; Gollapalli, M.; Farooq, R.K.; Shah, S.A.A.; Ahmed, Q.U.; Zakaria, Z.A. Synthesis of Chromen-4-One-Oxadiazole Substituted Analogs as Potent β-Glucuronidase Inhibitors. Molecules 2019, 24, 1528.

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