A series of novel 3-((4-(t-buty-)-2-(2-benzylidenehydrazinyl)thiazol-5-yl)methyl)quinolin-2(1H)-ones (7a--7z) were designed, synthesized and evaluated for their ability of inhibiting neuraminidase (NA) o...A series of novel 3-((4-(t-buty-)-2-(2-benzylidenehydrazinyl)thiazol-5-yl)methyl)quinolin-2(1H)-ones (7a--7z) were designed, synthesized and evaluated for their ability of inhibiting neuraminidase (NA) of influenza H1N1 virus. Some compounds displayed moderate influenza NA inhibitory activity. Compound 71 with the scaffold of 2-(2-(2-methoxybenzylidene)hydrazinyl)thiazole was the best one, exhibiting moderate NA inhibitory activity with ICs0 of 44.66 ~tmol/L. Structure-activity relationship showed that compounds with methoxy or hydroxy groups at the ortho position, fluorine and nitro groups at the meta position and chlorine and bromine groups at the para posi- tion of phenyl ring were more active. Docking study indicated that compound 71 has important interactions with some key residues (including Asp151, Glu119, Arg292, Tyr406, and Asn347) and binds to 430-cavity adjacent to NA active site.展开更多
采用失重法和电化学方法研究了2-氨基(1-苯基-3-氧代丁基)-5-甲基-噻唑(ABT)和2-氨基(1,4-二苯基-3-氧代丁基)-5-甲基-噻唑(ADT)在1 mol/L HC l溶液中对A3钢的缓蚀性能和吸附行为。结果表明,在1 mol/L HC l溶液中2种化合物对A3钢均有较...采用失重法和电化学方法研究了2-氨基(1-苯基-3-氧代丁基)-5-甲基-噻唑(ABT)和2-氨基(1,4-二苯基-3-氧代丁基)-5-甲基-噻唑(ADT)在1 mol/L HC l溶液中对A3钢的缓蚀性能和吸附行为。结果表明,在1 mol/L HC l溶液中2种化合物对A3钢均有较好的缓蚀性能,其最佳浓度均为400 mg/L,并且ADT的缓蚀性能比ABT的缓蚀性能好。2种化合物在A3钢表面上的吸附过程为放热过程,其在A3钢表面上的吸附行为服从Langmu ir吸附等温式,A3钢对ABT、ADT的吸附主要属于物理吸附。展开更多
文摘A series of novel 3-((4-(t-buty-)-2-(2-benzylidenehydrazinyl)thiazol-5-yl)methyl)quinolin-2(1H)-ones (7a--7z) were designed, synthesized and evaluated for their ability of inhibiting neuraminidase (NA) of influenza H1N1 virus. Some compounds displayed moderate influenza NA inhibitory activity. Compound 71 with the scaffold of 2-(2-(2-methoxybenzylidene)hydrazinyl)thiazole was the best one, exhibiting moderate NA inhibitory activity with ICs0 of 44.66 ~tmol/L. Structure-activity relationship showed that compounds with methoxy or hydroxy groups at the ortho position, fluorine and nitro groups at the meta position and chlorine and bromine groups at the para posi- tion of phenyl ring were more active. Docking study indicated that compound 71 has important interactions with some key residues (including Asp151, Glu119, Arg292, Tyr406, and Asn347) and binds to 430-cavity adjacent to NA active site.
基金Supported by the National Natural Science Foundation of China(51462030)the Science and Technology Program of Guizhou Province(QKHJC2016-1149)+3 种基金the Research Fund for the Doctoral Program of Tongren University(trxy DH1510)Guizhou Provincial Department of Education Foundation(QJHKYZ2016-105)the Opening Project of Sichuan University of Science and Engineering(2016CL06)and the student's platform for innovation and entrepreneurship training program(2016106665)~~
文摘采用失重法和电化学方法研究了2-氨基(1-苯基-3-氧代丁基)-5-甲基-噻唑(ABT)和2-氨基(1,4-二苯基-3-氧代丁基)-5-甲基-噻唑(ADT)在1 mol/L HC l溶液中对A3钢的缓蚀性能和吸附行为。结果表明,在1 mol/L HC l溶液中2种化合物对A3钢均有较好的缓蚀性能,其最佳浓度均为400 mg/L,并且ADT的缓蚀性能比ABT的缓蚀性能好。2种化合物在A3钢表面上的吸附过程为放热过程,其在A3钢表面上的吸附行为服从Langmu ir吸附等温式,A3钢对ABT、ADT的吸附主要属于物理吸附。