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Open AccessArticle

Synthesis of Novel Triazinoindole-Based Thiourea Hybrid: A Study on α-Glucosidase Inhibitors and Their Molecular Docking

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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
2
Neurology Department, King Fahad hospital of University, Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 34211, 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 31441, Saudi Arabia
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Department of Chemistry, Hazara University, Mansehra-21300, Khyber Pakhtunkhwa, Pakistan
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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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Faculty of Applied Sciences, Universiti Teknologi MARA, 40450 Shah Alam, Selangor D.E., Malaysia
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H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan
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Department of Chemistry, Jinnah University for Women, 5-C, Nazimabad, Karachi 74600, Pakistan
*
Authors to whom correspondence should be addressed.
Molecules 2019, 24(21), 3819; https://doi.org/10.3390/molecules24213819
Received: 12 September 2019 / Revised: 17 October 2019 / Accepted: 21 October 2019 / Published: 23 October 2019
(This article belongs to the Section Bioorganic Chemistry)
A new class of triazinoindole-bearing thiosemicarbazides (125) was synthesized and evaluated for α-glucosidase inhibitory potential. All synthesized analogs exhibited excellent inhibitory potential, with IC50 values ranging from 1.30 ± 0.01 to 35.80 ± 0.80 μM when compared to standard acarbose (an IC50 value of 38.60 ± 0.20 μM). Among the series, analogs 1 and 23 were found to be the most potent, with IC50 values of 1.30 ± 0.05 and 1.30 ± 0.01 μM, respectively. The structure–activity relationship (SAR) was mainly based upon bringing about different substituents on the phenyl rings. To confirm the binding interactions, a molecular docking study was performed. View Full-Text
Keywords: synthesis; triazinoindole; thiosemicarbazide; alpha-glucosidase; molecular docking study; SAR synthesis; triazinoindole; thiosemicarbazide; alpha-glucosidase; molecular docking study; SAR
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MDPI and ACS Style

Taha, M.; Alshamrani, F.J.; Rahim, F.; Hayat, S.; Ullah, H.; Zaman, K.; Imran, S.; Khan, K.M.; Naz, F. Synthesis of Novel Triazinoindole-Based Thiourea Hybrid: A Study on α-Glucosidase Inhibitors and Their Molecular Docking. Molecules 2019, 24, 3819.

AMA Style

Taha M, Alshamrani FJ, Rahim F, Hayat S, Ullah H, Zaman K, Imran S, Khan KM, Naz F. Synthesis of Novel Triazinoindole-Based Thiourea Hybrid: A Study on α-Glucosidase Inhibitors and Their Molecular Docking. Molecules. 2019; 24(21):3819.

Chicago/Turabian Style

Taha, Muhammad; Alshamrani, Foziah J.; Rahim, Fazal; Hayat, Shawkat; Ullah, Hayat; Zaman, Khalid; Imran, Syahrul; Khan, Khalid M.; Naz, Farzana. 2019. "Synthesis of Novel Triazinoindole-Based Thiourea Hybrid: A Study on α-Glucosidase Inhibitors and Their Molecular Docking" Molecules 24, no. 21: 3819.

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