36685-46-8Relevant articles and documents
Aurone derivatives as promising antibacterial agents against resistant Gram-positive pathogens
Olleik, Hamza,Yahiaoui, Samir,Roulier, Brayan,Courvoisier-Dezord, Elise,Perrier, Josette,Pérès, Basile,Hijazi, Akram,Baydoun, Elias,Raymond, Josette,Boumendjel, Ahcène,Maresca, Marc,Haudecoeur, Romain
, p. 133 - 141 (2019)
A set of variously substituted aurones was synthesized and evaluated against Methicillin-Resistant S. aureus (MRSA) and P. aeruginosa. Several analogues were found active against MRSA, but no effect was recorded against P. aeruginosa. Compounds 27, 30 and 33 showed low cytotoxicity, and were tested against a full range of bacterial (Gram-positive and Gram-negative) and fungal species, including resistant strains. These aurones displayed a selective inhibition of Gram-positive bacteria with excellent Therapeutic Index values, while showing no significant action on several Gram-negative strains, H. pylori and V. alginolyticus being the only susceptible strains among the Gram-negative bacteria tested. A permeabilization assay showed that the antibacterial activity of at least some of the aurones could be linked to alterations of the bacterial membrane. Overall, this study endorses the use of the aurone scaffold for the development of new potent and selective antibacterial agents.
Practical, modular, and general synthesis of 3-coumaranones through gold-catalyzed intermolecular alkyne oxidation strategy
Shu, Chao,Liu, Rongfu,Liu, Shuang,Li, Jian-Qiao,Yu, Yong-Fei,He, Qiao,Lu, Xin,Ye, Long-Wu
, p. 91 - 95 (2015/02/19)
A gold-catalyzed intermolecular alkyne oxidation for the preparation of 3-coumaranones has been developed. Using 8-isopropylquinoline N-oxides as oxidants, the reactions of o-ethynylanisoles afford versatile 3-coumaranones in moderate to good isolated yields. The synthetic utility of this chemistry is also indicated by the synthesis of the natural product sulfuretin.
