Abstract
Abstract In this paper, we have screened a library of two different series of compounds to identify potent lipoxygenase (LOX) inhibitors. A number of new biphenyl bis(benzenesulfonamides) 2-3, indol-3-yl-benzenesulfonyl and acetohydrazides 4-5 and indol-3-yl-hydrazinecarboxylate 6 were synthesized and evaluated in vitro for LOX inhibitory activity. Compounds biphenyl bis(benzenesulfonamide) 2a and indol-3-yl-benzenesulfonylhydrazide 4e presented the best anti-LOX activity within these series with IC50 values 96.31 ± 0.18 and 81.21 ± 2.14 μM, respectively. The results were confirmed with docking studies.
| Original language | English |
|---|---|
| Article number | 573 |
| Pages (from-to) | 1123-1130 |
| Number of pages | 8 |
| Journal | Journal of the Iranian Chemical Society |
| Volume | 12 |
| Issue number | 6 |
| DOIs | |
| State | Published - 1 Jun 2015 |
Bibliographical note
Publisher Copyright:© Iranian Chemical Society 2014.
Keywords
- Arachidonic acid
- Baicalein
- Indole derivatives
- LOX inhibitors
- Protein 1RRH
ASJC Scopus subject areas
- General Chemistry