Isatin-based benzyloxybenzene derivatives as monoamine oxidase inhibitors with neuroprotective effect targeting neurogenerative disease treatment

Benny, Feba; Oh, Jong Min; Kumar, Sunil; Abdelgawad, Mohamed A.; Ghoneim, Mohammed M.; Abdel-Bakky, Mohamed Sadek; Kukerti, Neelima; Jose, Jobin; Kim, Hoon; Mathew, Bijo

doi:10.1039/d3ra07035b

RSC Adv.

2023

DOI: 10.1039/d3ra07035b

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Isatin-based benzyloxybenzene derivatives as monoamine oxidase inhibitors with neuroprotective effect targeting neurogenerative disease treatment

Feba Benny,

Jong Min Oh,

Sunil Kumar

et al.

Abstract: Eighteen isatin-based benzyloxybenzaldehyde derivatives from three subseries, ISB, ISFB, and ISBB, were synthesized and their ability to inhibit monoamine oxidase (MAO) was evaluated.

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Cited by 2 publications

References 74 publications

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Isatin derived morpholine and piperazine derivatives as acetylcholinesterase inhibitors

Thomas,

Trisciuzzi,

Sudevan

et al. 2025

Journal of Molecular Structure

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Isatin derived morpholine and piperazine derivatives as acetylcholinesterase inhibitors

Thomas,

Trisciuzzi,

Sudevan

et al. 2025

Journal of Molecular Structure

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Synthesis, biochemistry, and in silico investigations of isatin-based hydrazone derivatives as monoamine oxidase inhibitors

Maliyakkal,

Oh,

Kumar

et al. 2024

Appl Biol Chem

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Ten isatin-based hydrazone derivatives were synthesized using two subseries, IA (isatin + acetophenone) and IB (isatin + benzaldehyde), and evaluated for their monoamine oxidases (MAOs) inhibitory activity. All the compounds showed stronger MAO-A inhibition than MAO-B, and the IB series showed more effective MAO-A inhibitory activity than IA series. Compound IB4 most potently inhibited MAO-A (half maximal inhibitory concentration IC50 = 0.015 µM), followed by IB3 (IC50 = 0.019 µM). On the contrary, compound IB3 showed the highest MAO-B inhibition (IC50 = 0.068 µM), followed by IB4 (IC50 = 1.87 µM). Compound IB3 and IB4 had low selectivity indices of 3.68 and 8.50, respectively. Structurally, the methyl group of IA series decreased the inhibition of both MAO-A and MAO-B. Among them, IB3 and IB4 (4-Cl and 4-Br in B-ring, respectively) showed higher MAO-A and MAO-B inhibition than the other substitutions. Inhibition constant Ki values of IB3 and IB4 for MAO-A were 0.0088 and 0.0063 µM, respectively, and those for MAO-B were 0.048 and 0.060 µM, respectively. IB3 and IB4 were competitive, reversible inhibitors of MAO-A and MAO-B. Molecular docking analysis predicted that IB3 and IB4 formed stable hydrogen bonds between Asn181 and the NH atom of isatin in the ligand-protein complex. Dynamic analysis revealed that IB3 and IB4 are stable with both MAO isoforms. These observations suggest IB3 and IB4 are potent and reversible MAO-A and MAO-B inhibitors and both compounds can be used as therapeutic agents for neurological disorders.

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Isatin-based benzyloxybenzene derivatives as monoamine oxidase inhibitors with neuroprotective effect targeting neurogenerative disease treatment

Abstract: Eighteen isatin-based benzyloxybenzaldehyde derivatives from three subseries, ISB, ISFB, and ISBB, were synthesized and their ability to inhibit monoamine oxidase (MAO) was evaluated.

Cited by 2 publications

References 74 publications

Isatin derived morpholine and piperazine derivatives as acetylcholinesterase inhibitors

Isatin derived morpholine and piperazine derivatives as acetylcholinesterase inhibitors

Synthesis, biochemistry, and in silico investigations of isatin-based hydrazone derivatives as monoamine oxidase inhibitors

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