Tetrahedron

Synthesis and anti-MRSA activity of novel cephalosporin derivatives

…, JJ Bronson, J Clark, K Denbleyker, J Fung-Tomc…

Index: D'Andrea, Stan V.; Bonner, Daniel; Bronson, Joanne J.; Clark, Junius; Denbleyker, Ken; Fung-Tomc, Joan; Hoeft, Shelley E.; Hudyma, Thomas W.; Matiskella, John D.; Miller, Raymond F.; Misco, Peter F.; Pucci, Michael; Sterzycki, Roman; Tsai, Yuan; Ueda, Yasutsuga; Wichtowski, John A.; Singh, Janak; Kissick, Thomas P.; North, Jeffery T.; Pullockaran, Annie; Humora, Michael; Boyhan, Brenda; Vu, Truc; Fritz, Alan; Heikes; Fox, Rita; Godfrey, Jollie D.; Perrone, Robert; Kaplan, Murray; Kronenthal, David; Mueller, Richard H. Tetrahedron, 2000 , vol. 56, # 31 p. 5687 - 5698

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Citation Number: 14

Abstract

Cephalosporin derivatives containing a unique combination of lipophilic C-7 sidechains and polar C-3 thiopyridinium groups were synthesized and found to exhibit potent anti-MRSA activity in vitro and in vivo. The optimum C-7 sidechains utilized were 2, 5- dichlorophenylthioacetamido and 2, 6-dichloropyrid-4-ylthioacetamido. The C-3 thiopyridinium rings were substituted at nitrogen with amino acid and pyruvic acid groups ...