Aug 2026· Arabian Journal of Chemistry· pp. 1-6· 0 citations
TL;DR
The oxindole-pyrrole-piperazine scaffold represents a promising template to find α-glucosidase inhibitors and elucidated the detailed binding mode of OPP-11 on α-glucosidase.
Abstract
α-Glucosidase acts as one therapeutic target for diabetes. For finding novel α-glucosidase inhibitors, oxindole-pyrrole-piperazine hybrids (
OPP-1∼24
) were synthesized. Inhibition evaluation revealed that all hybrids (
OPP-1∼X24
) demonstrated potent α-glucosidase inhibitory activity with IC
50
values of 6.34 ∼ 27.95 μM, obviously better than that of acarbose. Among them,
OPP-11
, as the strongest inhibitor (IC
50
= 6.34 μM), acted as a mixed-type inhibitor. Fluorescence quenching experiments indicated interaction of
OPP-11
with α-glucosidase following a static quenching mechanism. Circular dichroism and 3D fluorescence results revealed
OPP-11
binding induced α-glucosidase conformation changes. Molecular docking simulations further elucidated the detailed binding mode of
OPP-11
on α-glucosidase. Collectively, the oxindole-pyrrole-piperazine scaffold represents a promising template to find α-glucosidase inhibitors.
Kinetic enzyme assays revealed that compound 9f acts as a competitive inhibitor of α-glucosidase, competing with the natural substrate for binding to the active site, with a Ki value of 100 nM, and pharmacokinetic predictions showed that compound 9f exhibits a bioavailability radar and drug-likeness profile similar to...
Shahab Kermaninia, M. Sayahi, Mohammad Halimi et al.· RSC Advances· 0 citations
The integrated synthetic, kinetic, and biological findings demonstrate the potential of oxindole derivatives as promising lead molecules for developing next-generation antidiabetic agents with improved efficacy and molecular selectivity.
R. Reddy, K. Aruna· SARPS: Journal of Advanced R...· 0 citations
In the present study, new multifunctional imidazoles which contains the synthesis and biological activity experiments have been reported as α-glucosidase inhibitors. The procedure of imidazole-hydrazone derivative compounds (ISA1-5) relies on the condensation reaction of 5-Cl isatin and 2-benzylidenehydrazinecarboximid...
Semiha Köprü· Bitlis Eren Üniversitesi Fen...· 0 citations
Computer-aided drug-design methods are used to investigate thiazole and benzothiazole analogues as potential α-glucosidase inhibitors, followed by synthesis and in vitro evaluation of selected derivatives, identifying preliminary structure–activity patterns for further optimization.
D. Joshi, R. Bhati· Journal of Biomedical and Ph...· 0 citations
The hybrid 4k exhibited maximum inhibition of α-glucosidase enzyme with favorable binding interactions, suggesting this framework is a potential lead motif for future antidiabetic drug discovery.
Anshul Grover, V. Asati, Jayant Sindhu et al.· Future Medicinal Chemistry· 0 citations
Findings highlight green-synthesized polyhydroxy-conjugated piperidine and pyrrolidine derivatives, particularly this compound, as promising scaffolds for antiglycation therapy and modulation of diabetes-associated complications.
Anju Daharia, A. Thakur, Lokkanya Dewangan· Russian journal of general c...· 0 citations
We use cookies to run the site and, with your consent, for analytics and to show ads.
See our Cookie Policy.
