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Design, Synthesis and Biological Evaluation of Sulfenimine Cephalosporin Analogues as β-Lactamase Inhibitors 被引量:1
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作者 ZHANG Kai DING Huaiwei +3 位作者 SHI Ailong HUANG Qi SONG Hongrui FU Decai 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2015年第3期388-393,共6页
A series of sulfenimine cephalosporin derivatives(6a--6t) was designed, synthesized and evaluated for their inhibitory activity against class A β-lactamase(TEM-1) derived from E. coli, and class C β-lactamase (... A series of sulfenimine cephalosporin derivatives(6a--6t) was designed, synthesized and evaluated for their inhibitory activity against class A β-lactamase(TEM-1) derived from E. coli, and class C β-lactamase (cephalosporinase) derived from wild Bacillus subtilis in cell-free systems. Most of the tested compounds showed enhanced inhibitory activity against class C β-lactamase(cephalosporinase) compared with tazobactam. The most promising compounds 6c and 6o in combination with cefradine(IC50=1.80 and 1.59 gmol/L, respectively) were fur- ther investigated against a series of clinical isolated β-lactamase-producing bacterial strains. The results reveal that compounds 6c and 60 in combination with cefradine show two to four times more activity than cefradine alone against methicillin-sensitive Staphylococcus aureus(MSSA) and Klebsiella pneumoniae. The data suggest that the sulfenimine moiety may be beneficial to the activity and selectivity of inhibitors. 展开更多
关键词 β-Lactamase-inhibitor sulfenimine CEPHALOSPORINS
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Design,synthesis and biological evaluation of sulfenimine cephalosporin sulfoxides as β-lactamase inhibitors 被引量:1
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作者 Kai Zhang Huai-Wei Ding +4 位作者 Hao Ju Qi Huang Li-Juan Zhang Hong-Rui Song De-Cai Fu 《Chinese Chemical Letters》 SCIE CAS CSCD 2015年第6期801-803,共3页
A series of sulfenimine cephalosporin sulfoxide derivatives (Ta-v) were designed, synthesized and evaluated for their inhibitory activity against TEM-1 and cephalosporinase in cell-free systems. Some of the tested c... A series of sulfenimine cephalosporin sulfoxide derivatives (Ta-v) were designed, synthesized and evaluated for their inhibitory activity against TEM-1 and cephalosporinase in cell-free systems. Some of the tested compounds showed enhanced inhibitory activity against class C β-lactamase cephalospor- inase compared with the tazobactam. The most promising compounds 7c and 7n (IC50 ~ 7.6 and 8.6 μmol/L, respectively) were further investigated in combination with cefradine against a variety of clinical isolated fi-lactamase-producing bacterial strains. 展开更多
关键词 β-Lactamase inhibitor sulfenimine Synthesis
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