Preprint Article Version 1 This version is not peer-reviewed

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

Version 1 : Received: 12 September 2019 / Approved: 13 September 2019 / Online: 13 September 2019 (10:54:30 CEST)

How to cite: Taha, M.; Alshamrani, F.J.; Rahim, F.; Hayat, S.; Ullah, H.; Zaman, K.; Imran, S. Synthesis of novel Triazinoindole-Based-Thiourea Hybrid: α-Glucosidase Inhibitors and Their Molecular Docking Study. Preprints 2019, 2019090130 (doi: 10.20944/preprints201909.0130.v1). Taha, M.; Alshamrani, F.J.; Rahim, F.; Hayat, S.; Ullah, H.; Zaman, K.; Imran, S. Synthesis of novel Triazinoindole-Based-Thiourea Hybrid: α-Glucosidase Inhibitors and Their Molecular Docking Study. Preprints 2019, 2019090130 (doi: 10.20944/preprints201909.0130.v1).

Abstract

New class of triazinoindole bearing thiosemicarbazide (1-25) was synthesized and evaluated for α-glucosidase inhibitory potential. All synthesized analogues exhibited excellent inhibitory potential having IC50 values ranging from 1.30 ± 0.01 to 35.80 ± 0.80 µM when compared with the standard acarbose having IC50 value 38.60 ± 0.20 µM. Among series the analogues 1 and 23 was found the most potent having IC50 values 1.30 ± 0.05 and 1.30 ± 0.01 µM respectively. Structure activity relationship (SAR) was mainly based upon by bring about difference of substituents on phenyl rings. To confirm the binding interactions, molecular docking study was performed. Synthesized analogues were characterized through HREI-MS, 1H and 13C-NMR analysis.

Subject Areas

Synthesis; triazinoindole; thiosemicarbazide; alpha-glucosidase; molecular docking study; SAR

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