26206-42-8Relevant articles and documents
Characterization, solution behavior, and microstructure of a hydrophobically associating nonionic copolymer
Zhong, Chuanrong,Huang, Ronghua,Xu, Jinyong
, p. 1227 - 1243 (2008)
To obtain an oil-displacement polymer with good thermal stability and solution properties, self-assembling acrylamide (AM)/4-butylstyrene (BST) copolymers (PSA) were synthesized by the micellar copolymerization technique. The resulting polymer was charact
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus
Song, Di,Bi, Fangchao,Zhang, Nan,Qin, Yinhui,Liu, Xingbang,Teng, Yuetai,Ma, Shutao
supporting information, (2020/09/11)
Antibiotic resistance among clinically significant bacterial pathogens, such as methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant S. aureus (VRSA) is becoming a prevalent threat to public health, and new antibacterial agents with novel mechanisms of action hence are in an urgent need. As a part of continuing effort to develop antibacterial agents, we rationally designed and synthesized two series of 4,5-dihydroisoxazol-5-yl and 4,5-dihydroisoxazol-3-yl-containing benzamide derivatives that targeted the bacterial cell division protein FtsZ. Evaluation of their activity against a panel of Gram-positive and -negative pathogens revealed that compound A16 possessing the 4,5-dihydroisoxazol-5-yl group showed outstanding antibacterial activity (MIC, ≤0.125–0.5 μg/mL) against various testing strains, including methicillin-resistant, penicillin-resistant and clinical isolated S. aureus strains. Besides, further mouse infection model revealed that A16 could be effective in vivo and non-toxic to Hela cells. Finally, a detailed discussion of structure-activity relationships was conducted, referring to the docking results. It is worth noting that substituting a 4,5-dihydroisoxazole ring for the isoxazole ring not only broadened the antibacterial spectrum but also resulted in a significant increase in antibacterial activity against S. aureus strains. Taken together, these results suggest a promising chemotype for the development of new FtsZ-targeting bactericidal agents.
Regio-specific polyacetylenes synthesized from anionic polymerizations of template monomers
Zhang, Yang,Li, Jia,Li, Xiaohong,He, Junpo
, p. 6260 - 6269 (2015/02/19)
Substituted polyacetylenes with alkylphenyl side groups and head-to-head regioregularity were prepared through anionic living polymerization of template monomers and subsequent dehydrogenation process. The template monomers have the structure of 2, 3-disubstituted-1, 3-butadienes prepared by palladium-catalyzed Kumada coupling of the corresponding vinyl bromides. Anionic polymerizations of the template monomers produced narrow disperse substituted polybutadiene precursors with exclusive 1, 4-enchainment. The precursors were converted into soluble polyacetylene derivatives via two methods, e.g., bromination followed by elimination of HBr, and direct dehydrogenation by 2, 3-dichloro-5, 6-dicyano-1, 4-benzoquinone (DDQ), both resulting in dark colored products with significant red shift in UV spectra. The obtained head-to-head polyacetylene derivatives exhibited highly thermal stability, possibly due to trans-rich and/or head-to-head chain configurations. The microstructures of the poly(2, 3-dialkylphenyl butadiene) precursors were analyzed in detail using NMR spectroscopy with regard to the solvent effect during polymerization. Block copolymers containing substituted polyacetylene segments were prepared through sequential anionic polymerization of different monomers, followed by dehydrogenation transformation. The present synthesis may serve as a new strategy for tailoring molecular structures of polyacetylene-based polymers by virtue of anionic living polymerization techniques.
