SYNTHESIS AND BIOLOGICAL EVALUATION OF 1H-(INDOLE-5-YL)-3-SUBSTITUTED-1,2,4-OXADIAZOLES AS NOVEL 5-LOX INHIBITORS

Year 2024, Volume: 11 Issue: 1, 11 - 18, 04.02.2024

Berihu Tekluu , Siddaiah Vidavalur , Sunanda Kumari Kadiri

https://doi.org/10.18596/jotcsa.1334005

Abstract

: A series of indolyloxadiazoles were synthesized from amidoxime and indole 3-carboxaldehyde using CAN as a catalyst and PEG as a solvent. In vitro, a 5-LOX inhibitory assay has been performed for all the synthesized compounds. Among the tested compounds, 4bf showed the highest potency (IC50 18.78 µg/ml). The synthesized compound carried out docking on the 5-LOX enzyme protein crystal structure. Compound (4bf) docked snugly into the receptor site with a score of -9.1 Kcal/mol, and it showed strong hydrogen bond interactions with two key amino acids, His368 and Asn555.

Keywords

1-2-4-oxadiazoles, Indolyloxadiazoles, 5-LOX inhibitors

Supporting Institution

Aksum University and Ministry of Education, Ethiopia for financial support

Thanks

The authors thank Aksum University and Ministry of Education, Ethiopia for financial support

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