2'-Hydroxy-2'-desamino-4,6-di-O-(aminoglycosyl)-1,3-diaminocycli

Details 2'-Hydroxy-2'-desamino-4,6-di-O-(aminoglycosyl)-1,3-diaminocycli 2'-Hydroxy-2'-desamino-4,6-di-O-(aminoglycosyl)-1,3-diaminocycli

1978-06-05

1980-07-15

Brown, Johnnie R.

Drug, bio-affecting and body treating compositions

Conjugate or complex of monoclonal or polyclonal antibody,...

Conjugated via claimed linking group, bond, chelating agent,...

536 10, 536 17R, A61K 3171, C07H 1522

Patent

active

042128595

ABSTRACT:
2'-Hydroxy-2'-desamino-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols having a 6'-amino function exhibit antibacterial activity and are prepared by reaction of the corresponding N-protected (except the 2'-amino)-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitol with hydrogen peroxide in the presence of tungstate ion, followed by cleavage of the thereby formed 2'-oximino derivative, thence reduction of the resulting 2'-oxo derivative and removal of the N-protecting groups.
Preferred compounds are 1-N-(.omega.-amino-.alpha.-hydroxyalkanoyl)-2'-hydroxy-2'-desamino-4,6-di- O-(aminoglycosyl)-1,3-diaminocyclitols which exhibit antibacterial activity against bacteria resistant to the parent aminoglycoside.

REFERENCES:
patent: 3828021 (1974-08-01), Beattie et al.
patent: 4066752 (1978-01-01), Mallams et al.
patent: 4085208 (1978-04-01), Mallams et al.

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