Novel penicillin compounds and process for preparation thereof

Details Novel penicillin compounds and process for preparation thereof Novel penicillin compounds and process for preparation thereof

1977-06-29

1978-07-25

Schwartz, Gerald A.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

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

128272, 424271, 2602391, A61K 3143, C07D49968

Patent

active

041030117

ABSTRACT:
A penicillin compound of the formula ##STR1## wherein R is a formyl or acetyl group, and a nontoxic pharmaceutically acceptable salt thereof. The penicillin compound is prepared by (A) reacting a compound of the formula ##STR2## or its salt or its reactive derivative at the carboxyl group, with 6-.alpha.-amino-p-hydroxybenzylpenicillin or its salt or its derivative, or reacting a compound of the formula ##STR3## or its salt or its reactive derivative at the carboxyl group, with 6-aminopenicillanic acid or its salt or its derivative, (B) optionally hydrolyzing or catalytically hydrogenolyzing the reaction product, and (C) optionally converting the reaction product to a nontoxic pharmaceutically acceptable salt. The penicillin compound has low toxicity and superior antibacterial activity especially against bacteria of the genus Pseudomonas and is suitable for parenteral administration, especially for an intramuscular, intravenous or subcutaneous injection.

REFERENCES:
patent: 3433784 (1969-03-01), Long et al.
patent: 3887557 (1975-06-01), Minami et al.
patent: 3939150 (1976-02-01), Murakami et al.
patent: 3953428 (1976-04-01), Murakami et al.
patent: 3954734 (1976-05-01), Doub et al.
patent: 3992371 (1976-11-01), Tobiki et al.
patent: 4003887 (1977-01-01), Tobiki et al.

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