Studies on Semisynthesis and Antibacterial Activity of7β-Heterocyclocamido-3-heterothiomethyl Cephalosporins

Chem. J. Chinese Universities ›› 2000, Vol. 21 ›› Issue (12): 1844.

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Studies on Semisynthesis and Antibacterial Activity of7β-Heterocyclocamido-3-heterothiomethyl Cephalosporins

HUI Xin-Ping¹, HAO Lan¹, ZHANG Zi-Yi¹, WANG Qin², WANG Fang², GUAN Zuo-Wu³

1. College of Chemistry and Chemical Engineering, National Laboratory of Applied Organic Chemistry;
2. Department of Biology, Lanzhou University, Lanzhou 730000, China;
3. Institute of Applied Pharmacy, Beijing Medical University, Beijing 100083, China

Received:1999-11-15 Online:2000-12-24 Published:2000-12-24

Abstract

Abstract: New cephalosporin derivatives5a_5b and6a_6h were prepared by condensation of2a_2f with aminothiazoleoxime active ester3 and1-ryl-5-methyl1-H-1,2,3 triazol3-formyl chloride4a_4e, respectively.The intermediate2a_2f were synthesized by reaction of2-substituted-1,3,4 oxadiazol-5-thiols1a-1f with 7-ACA.The structures of the compounds synthesized were confirmed by IR, ¹H NMRand MSspectra.The preliminary results of antibacterial activities revealed that5a_5b showed significant antibacterial activities against both Gram-positive and Gram-negative bacteria, and6a_6h had moderate antibacterial activities against these bacteria

Key words: Cephalosporin, Semisynthesis, Antibacterial activity, Centrifugal-TLC

CLC Number:

R914

TrendMD:

HUI Xin-Ping, HAO Lan, ZHANG Zi-Yi, WANG Qin, WANG Fang, GUAN Zuo-Wu. Studies on Semisynthesis and Antibacterial Activity of7β-Heterocyclocamido-3-heterothiomethyl Cephalosporins[J]. Chem. J. Chinese Universities, 2000, 21(12): 1844.

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Studies on Semisynthesis and Antibacterial Activity of7β-Heterocyclocamido-3-heterothiomethyl Cephalosporins

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