Antibacterial studies of hydroxyspiro[indoline-3, 9-xanthene]trione against spiro[indoline3, 9-xanthene]trione and their use as acetyl and butyrylcholinesterase inhibitors. (May 2019)

• Record Type: Journal Article
• Authors: Barmak, Alireza; Niknam, Khodabakhsh; Mohebbi, Gholamhossein; Pournabi, Hamid
• Is Part Of: Microbial pathogenesis. Volume 130(2019)
• Page Start: 95
• Page End: 99
• Publication Date: 2019-05
• Subjects: Xanthenes -- Antimicrobial -- Anticholinesterases activities -- Docking studies -- Alzheimer's disease; Pathogenic microorganisms -- Periodicals; Pathology, Molecular -- Periodicals; Communicable Diseases -- microbiology -- Periodicals; Communicable Diseases -- parasitology -- Periodicals; Micro-organismes pathogènes -- Périodiques; Pathologie moléculaire -- Périodiques; Electronic journals; 616.9041
• DOI: 10.1016/j.micpath.2019.03.002
• Languages: English
• ISSNs: 0882-4010

Abstract

Abstract: Xanthene derivatives are well known for their effective biological activities. In search of effective antibacterial agents, the spiro[indoline3, 9-xanthene]-trione (A ) and hydroxy-spiro[indoline-3, 9-xanthene]-trione (B ), were synthesized and tested for in vitro antibacterial activity against Staphylococcus aureus and Escherichia coli . Furthermore, the synthesized compounds were tested in vitro and in silico for their anticholinesterase activities. The anticholinesterase activities for six substitutes of the hydroxy derivative (B1 -B6 ) were also studied through the molecular docking. All concentrations of compounds presented a dose-dependent antibacterial activity. The docking results showed that all compounds are more constant than the galantamine. Amongst, compoundB1 exhibited the minimum binding energy in both AChE and BChE enzymes. Results indicate the importance of xanthene derivatives as potential antibacterial and anticholinesterases agents. Graphical abstract: Image 1 Highlights: The antibacterial activities of xanthenes against Staphylococcus aureus and Escherichia coli are evaluated. The activities of hydroxyl-xanthenes in gram-positive bacteria are more than the gram-negative bacteria. The hydroxyl group was increased the antibacterial properties.