7-N-Heterocyclyl 1-oxa, 1-aza, and 1-carbadethiacephalosporins

Details 7-N-Heterocyclyl 1-oxa, 1-aza, and 1-carbadethiacephalosporins 7-N-Heterocyclyl 1-oxa, 1-aza, and 1-carbadethiacephalosporins

1979-04-27

1981-03-10

Randolph, John D.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Bacterium or component thereof or substance produced by said...

544 90, 544263, 544333, 544335, 546112, 546263, 546347, 42424852, 42424853, A61K 3144, C07D21128

Patent

active

042554241

ABSTRACT:
Disclosed are antibiotic cephalosporins (I) of the formula: ##STR1## Wherein the stylized radical attached to the 7-amino nitrogen of the cephalosporin moiety represents a nitrogen-containing heterocyclic group (mono- or polycyclic); R is, inter alia, hydrogen, alkyl, heterocyclylalkyl, aryl, alkenyl, aralkyl, --NR.sub.2, --OR, COOR, CONR.sub.2 or CN; A is conventionally known in the cephalosporin art; and R.sup.2 is H, or loweralkoxyl; X is O, CH.sub.2, or NR.sup.7 (R.sup.7 is, inter alia, hydrogen, alkyl or aralkyl. Also disclosed are the pharmaceutically acceptable salt and ester derivatives of I; processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.

REFERENCES:
Firestone et al., J. Med. Chem. vol. 20, pp. 551-556 (1977).
Kim et al., Tetrahedron Letters, vol. 5, pp. 409-412 (1978).
Cama et al., J. Am. Chem. Soc. vol. 96, pp. 7582 to 7584 (1974).
Guthikonda et al., J. Am. Chem. Soc. vol. 96, 7584-7585 (1975).
Lednicer et al., The Organic Chemistry of Drug Synthesis, pp. 416 to 422, John Wiley and Sons, NY 1977.
Degering, An Outline of Organic Chemistry, 6th ed., p. 142, Barnes & Noble, Inc., NY (1951).

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