3-ammoniopropenyl cephalosporin compounds as antibacterial agent

Details 3-ammoniopropenyl cephalosporin compounds as antibacterial agent 3-ammoniopropenyl cephalosporin compounds as antibacterial agent

1995-09-01

1997-10-07

Shah, Mukund J.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

540222, 540224, C07D50118, C07D50124

Patent

active

056750030

ABSTRACT:
A 3-ammoniopropenyl cephalosporin of the following formula (I): ##STR1## wherein P is hydroxylated alicyclic or aliphatic amines such as meso-3,4-dihydroxy-1-methylpyrrolidine, (3S,4S)-3,4-dihydroxy-1-methylpyrrolidine, (3R,4R)-3,4-dihydroxy-1-methylpyrrolidine, rac-3,4-trans-dihydroxy-1-methylpyrrlidine, (2S,4R)-4-hydroxy-1-methyl-2-pyrrolidinemethanol, N-methyl-bis(2-hydroxyethyl)amine, 3,4-cis-dihydroxy-1-methylpiperidine, 3,4-trans-dihydroxypiperidine, 4-hydroxy-1-methylpiperidine, 2-hydroxymethyl-1-methylpiperidine, or tropine, or a pharmaceutically acceptable salt thereof, exhibits good anti-bacterial activities against a wide variety of Gram-positive and Gram-negative bacteria; and a process for the preparation thereof.

REFERENCES:
patent: 4278671 (1981-07-01), Ochiai et al.
patent: 4912212 (1990-03-01), Ochiai et al.
Drugs of the Future, 10:805-808 (1985).
Naito et al., "Synthesis and Structure-Activity Relationships of a New Series of Cephalosporins, BMY-28142 and Related Compounds", J. of Antibiotics, 8:1092-1107 (Aug. , 1986).
Drugs of the Future, 13:369-371 (1988).
Kamachi et al., "Synthesis of a New Series of Cephalosporins Having 3-Substituted-Ammonio-1-Propenyl Group as the C-3 Side Chain", J. of Antibiotics, 5:533-543 (May, 1990).
Naito et al., The Journal of Antibiotics, Aug. 1986 ; vol. XXXIX No. 8 p. 1093.

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