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CHEN Guo-hua, REN Zhong, YANG Yang, WU Fei-hua. Synthesis and antibacterial activity of novel fourth-generation cephalosporin compounds[J]. Journal of China Pharmaceutical University, 2009, 40(5): 395-399.
Citation: CHEN Guo-hua, REN Zhong, YANG Yang, WU Fei-hua. Synthesis and antibacterial activity of novel fourth-generation cephalosporin compounds[J]. Journal of China Pharmaceutical University, 2009, 40(5): 395-399.

Synthesis and antibacterial activity of novel fourth-generation cephalosporin compounds

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  • Aim :To study the synthesis and antibacterial activity of new fourth-generation cephalosporin compounds. Methods :Starting with 7-ACA,the target compounds were obtained by 3-substitution with nitrogen-containing aromatic heterocyclic compounds using TMSI as a catalyst,salt exchange with hydrochloric acid and condensation with 2-(2-substituted aminothiazol-4-yl)-(Z)-2-methoxyiminoacetic acid thiobenzothiazole active esters in the presence of Et3N.Their antibacterial activity in vitro were evaluated by double broth dilution method. Results and Conclusion :Nine new compounds were synthesized,and their structures were confirmed by IR,ESI-MS,1H NMR and elemental analysis.Preliminary results of antibacterial activities in vitro showed that compounds 4c and 4h possessed approximately equivalent antibacterial activity against Gram-positive bacteria in comparison with cefozopran.
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