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

Authors : Berihu Tekluu, Siddaiah Vidavalur, Sunanda Kumari Kadiri

Pages : 11-18

Doi:10.18596/jotcsa.1334005

View : 60 | Download : 66

Publication Date : 2024-02-04

Article Type : Research Paper

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