Bioactive oxadiazolo-benzodiazepines: synthesis, α amylase inhibition, antioxidant activity, molecular docking and DFT calculation

Both diastereoisomers <b>3</b> and <b>4</b> demonstrated superior activity compared to standard drugs. Compound <b>3</b> showed potent α-amylase inhibition IC<sub>50</sub> = 22.78 µM) compared to Acarbose IC<sub>50</sub> = 123 µM). For antioxidant activity, compounds <b>4</b> and <b>3</b> exhibited strong DPPH scavenging IC<sub>50</sub> = 68.16 and 79.50 μM, respectively), outperforming ascorbic acid. Docking studies confirmed favorable binding interactions within the active sites of target enzymes. The synthesized oxadiazolo-benzodiazepines represent promising multifunctional antidiabetic and antioxidant candidates, warranting further pharmacological investigation.

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Publication Details

Journal
Future Medicinal Chemistry
Published
2026-02-26
DOI
https://doi.org/10.1080/17568919.2026.2636823
Primary Topic
Synthesis and biological activity
Type
article
Field-Weighted Citation Impact
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article

Bioactive oxadiazolo-benzodiazepines: synthesis, α amylase inhibition, antioxidant activity, molecular docking and DFT calculation

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Bioactive oxadiazolo-benzodiazepines: synthesis, α amylase inhibition, antioxidant activity, molecular docking and DFT calculation

My El Abbes Faouzi, Ismail Hdoufane, Marouane Ait Lahcen, Nouhaila Ait Lahcen, A. Baouid, Mohamed Maatallah, Samir Hmaimou, Mohamed Adardour, Driss Cherqaoui, Driss Fadili, Wissal Karfi, Elena Zaballos-García
article en

Abstract

Both diastereoisomers <b>3</b> and <b>4</b> demonstrated superior activity compared to standard drugs. Compound <b>3</b> showed potent α-amylase inhibition IC<sub>50</sub> = 22.78 µM) compared to Acarbose IC<sub>50</sub> = 123 µM). For antioxidant activity, compounds <b>4</b> and <b>3</b> exhibited strong DPPH scavenging IC<sub>50</sub> = 68.16 and 79.50 μM, respectively), outperforming ascorbic acid. Docking studies confirmed favorable binding interactions within the active sites of target enzymes. The synthesized oxadiazolo-benzodiazepines represent promising multifunctional antidiabetic and antioxidant candidates, warranting further pharmacological investigation.

Future Medicinal Chemistry
Cadi Ayyad University (MA), Mohammed V University (MA), Universitat de València (ES), Université Mohammed VI Polytechnique (MA), Instituto Superior da Maia (PT)
Openalex Percentile: Top 38%
Synthesis and biological activity
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