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
A series of pyrrolopyrazinone-chalcone hybrids（12a-12q） was designed,synthesized and screened for their antitumor activity against SKOV-3,A549 and HeLa cell lines in vitro.Compared with the pyrrolopyrazinone（10a） ...A series of pyrrolopyrazinone-chalcone hybrids（12a-12q） was designed,synthesized and screened for their antitumor activity against SKOV-3,A549 and HeLa cell lines in vitro.Compared with the pyrrolopyrazinone（10a） and 5-fluorouracil（5-FU）,nearly all the tested compounds showed significantly-improved antitumor activities.The most promising compounds 12e and 12k（IC50=0.25 and 0.88 μmol/L） respectively show activities of 123and 35 times that of compound 10a（IC50=30.74 μmol/L） against HeLa cell line.The result reveals that the presence of chalcone moiety is beneficial to their activity and selectivity.展开更多
文摘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.
文摘A series of pyrrolopyrazinone-chalcone hybrids（12a-12q） was designed,synthesized and screened for their antitumor activity against SKOV-3,A549 and HeLa cell lines in vitro.Compared with the pyrrolopyrazinone（10a） and 5-fluorouracil（5-FU）,nearly all the tested compounds showed significantly-improved antitumor activities.The most promising compounds 12e and 12k（IC50=0.25 and 0.88 μmol/L） respectively show activities of 123and 35 times that of compound 10a（IC50=30.74 μmol/L） against HeLa cell line.The result reveals that the presence of chalcone moiety is beneficial to their activity and selectivity.
