Synthesis and anaerobic activity of novel 1-carba-1-dethiacephalosporins.
The synthesis and biological evaluation of novel 1-carba-1-dethiacephalosporins exhibiting activity against anaerobic pathogens are described. The nitrothiazole substituent was determined to be crucial to maintaining this activity. The pharmacokinetic parameters and initial toxicological profile of the lead compound are discussed.
Ternansky
R J
RJ
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285.
Jordan
C L
CL
Eudaly
J A
JA
Kasher
J S
JS
D000818:Animals; D001421:Bacteria, Anaerobic / Q000187:drug effects*; D002511:Cephalosporins / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley
D002511:Cephalosporins; C026739:carbacephems