Synthesis of benzotriazoles derivatives and their dual potential as α-amylase and α-glucosidase inhibitors in vitro: Structure-activity relationship, molecular docking, and kinetic studies.

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ID: 81926
2019
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Abstract
Benzotriazoles (4-6) were synthesized which were further reacted with different substituted benzoic acids and phenacyl bromides to synthesize benzotriazole derivatives (7-40). The synthetic compounds (7-40) were characterized via different spectroscopic techniques including EI-MS, HREI-MS, H-, and C NMR. These molecules were examined for their anti-hyperglycemic potential hence were evaluated for α-glucosidase and α-amylase inhibitory activities. All benzotriazoles displayed moderate to good inhibitory activity in the range of IC values of 2.00-5.6 and 2.04-5.72 μM against α-glucosidase and α-amylase enzymes, respectively. The synthetic compounds were divided into two categories "A" and "B", in order to understand the structure-activity relationship. Compounds 25 (IC = 2.41 ± 1.31 μM), (IC = 2.5 ± 1.21 μM), 36 (IC = 2.12 ± 1.35 μM), (IC = 2.21 ± 1.08 μM), and 37 (IC = 2.00 ± 1.22 μM), (IC = 2.04 ± 1.4 μM) with chloro substitution/s at aryl ring were found to be most active against α-glucosidase and α-amylase enzymes. Molecular docking studies on all compounds were performed which revealed that chloro substitutions are playing a pivotal role in the binding interactions. The enzyme inhibition mode was also studied and the kinetic studies revealed that the synthetic molecules have shown competitive mode of inhibition against α-amylase and non-competitive mode of inhibition against α-glucosidase enzyme.
Reference Key
hameed2019synthesiseuropean Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Hameed, Shehryar;Kanwal, ;Seraj, Faiza;Rafique, Rafaila;Chigurupati, Sridevi;Wadood, Abdul;Rehman, Ashfaq Ur;Venugopal, Vijayan;Salar, Uzma;Taha, Muhammad;Khan, Khalid Mohammed;
Journal European journal of medicinal chemistry
Year 2019
DOI
S0223-5234(19)30821-9
URL
Keywords
Diabetes kinetic studies benzotriazoles in silico studies α-amylase inhibition α-glucosidase inhibition

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