Fusidic acid derivatives

Details Fusidic acid derivatives Fusidic acid derivatives

1976-11-24

1978-07-11

Roberts, Elbert L.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

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

2602395, 26023955, 2603971, 424242, A61K 3156, C07J 900

Patent

active

041002768

ABSTRACT:
The invention relates to a new series of fusidic acid derivatives, to salts and easily hydrolyzable esters thereof, to the preparation of these compounds and to pharmaceutical compositions containing the compounds, the new compounds having the general formula: ##STR1## in which Q.sub.1 and Q.sub.2 stand for the group ##STR2## or oxygen, A represents oxygen or sulphur, and R.sub.1 stands for a straight or branched alkyl radical having from 1 to 12 carbon atoms, R.sub.1 can further be an alkenyl or alkynyl radical having from 3 to 6 carbon atoms, a cycloalkyl radical having from 3 to 7 carbon atoms in the alicyclic ring, an aralkyl or aryl radical, R.sub.1 can also be a heterocyclic radical having 5 or 6 ring atoms and containing oxygen, sulphur and/or nitrogen atoms, R.sub.1 optionally being further substituted, and in which formula I the dotted line between C-24 and C-25 indicates that the carbon atoms in question are connected by either a double bond or a single bond, and the asterix at C-20 indicates that the compounds exist in two diastereomeric forms, and thus the invention comprises the pure diastereomers as well as mixtures of these.
The compounds of the present invention possess antibacterial properties and show further interesting antimicrobial and pharmacokinetic properties.

REFERENCES:
patent: 3867413 (1975-02-01), VON Daehne et al.
patent: 4004004 (1977-01-01), VON Daehne et al.

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