Studies on Semisynthesis and Antimicrobial Activity of 7β-Heterocyclicamido Cephalosporins

Abstract

Abstract: Nine new 7 β-(1-aryl-5-methyl-1H-1,2,3-triazolyl-4-formamido)cephalosporins 3a-3j were synthesized by acylation of 7 β-amino group of 7-ACA, 7-ADCAand 7-ACT, with 1-aryl-5 methyl-1H-1,2,3-triazolyl-4 formyl chloride 2a-2c. Two new 7 β-(1,2,3-benzotriazolyl-1-acetamido) cephalosporins 6a 6b and two new 7 β-(5-methyl isoxazolyl-3-formamido) cephalosporins 9a-9b were obtained with the same acid choride. Isolation and purification of the new compounds were fulfilled with Sephadex LH-20 column chromatography and centrifugal TLCtechnique. The structure of the compounds were confirmed by elementary analysis, IR, ¹HNMRand FAB MS, some of them showed a significant antibacterial activity.

Key words: Cephalosporins, Vicinal triazole, Semisynthesis, Antibacterial activity, Centrifugal TLC

CLC Number:

R914

TrendMD:

ZHANG Zi-Yi, LIANG Yu-Xiang, HAO Lan, GUAN Zuo-Wu . Studies on Semisynthesis and Antimicrobial Activity of 7β-Heterocyclicamido Cephalosporins[J]. Chem. J. Chinese Universities, 1998, 19(9): 1411.

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Studies on Semisynthesis and Antimicrobial Activity of 7β-Heterocyclicamido Cephalosporins

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