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.
Funder
Aksum University and Ministry of Education, Ethiopia for financial support
Publisher
The Turkish Chemical Society
Reference36 articles.
1. 1. Knölker HJ, Reddy KR. Isolation and synthesis of biologically active carbazole alkaloids. Chemical reviews. 2002 Nov 13;102(11):4303-428. Available from:
2. 2. Tale RH, Rodge AH, Keche AP, Hatnapure GD, Padole PR, Gaikwad GS, Turkar SS. Synthesis and antibacterial, antifungal activity of novel 1, 2, 4-oxadiazole. Journal of Chemical and Pharmaceutical Research. 2011;3(2):496-505. Available from:
3. 3. Pace A, Pierro P. The new era of 1, 2, 4-oxadiazoles. Organic & biomolecular chemistry. 2009;7(21):4337-48. Available from:
4. 4. Borg S, Luthman K, Nyberg F, Terenius L, Hacksell U. 1, 2, 4-Oxadiazole derivatives of phenyl-alanine: potential inhibitors of substance P endopepti-dase. European Journal of Medicinal Chemistry. 1993 Jan 1;28(10):801-10. Available from:
5. 5. Behalo MS, Aly AA, Wasfy AF, Rizk MM. Syn-thesis of some novel 1, 2, 4-triazole derivatives as potential antimicrobial agents. European Journal of Chemistry. 2013 Jun 30;4(2):92-7. Available from: