76967-92-5Relevant articles and documents
Design, synthesis and activity against Staphylococcus epidermidis of 5-chloro-2- or 5-chloro-4-methyl-9H-xanthen-9-one and some of its derivatives
Mazur, Gabriela,Skiba-Kurek, Iwona,Karczewska, El?bieta,Pańczyk-Straszak, Katarzyna,Jaworska, Joanna,Waszkielewicz, Anna M.
, p. 674 - 685 (2020/10/23)
Ten new xanthone derivatives have been designed and synthesized for their potential antibacterial activity. All compounds have been screened against Staphylococcus epidermidis strains ATCC 12228 and clinical K/12/8915. The highest antibacterial activity was observed for compound 3: 5-chloro-2-((4-(2-hydroxyethyl)piperazin-1-yl)methyl)-9H-xanthen-9-one dihydrochloride, exhibiting MIC of 0.8?μg/ml against ATCC 12228 strain, compared to linezolid (0.8?μg/ml), ciprofloxacin (0.2?μg/ml) or trimethoprim and sulfamethoxazole (0.8?μg/ml). For the most active compound 3, genotoxicity assay with use of Salmonella enterica serovar Typhimurium revealed safety in terms of genotoxicity at concentration 75?μg/ml and antibacterial activity against Salmonella at all higher concentrations. A final in silico prediction of skin metabolism of compound 3 seems promising, indicating stability of the xanthone moiety in the metabolism process.
