Formimidoyl A and B useful as semi-synthetic aminoglycosidic antibiotics
AssigneeZaidan Hojin Biseibutsu Kagaku Kenkyu Kai
InventorsHamao Umezawa, Yoshiro Okami, Shinichi Kondo
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Abstract
New, useful derivatives of istamycins A and B are provided, which are formimidoylistamycins A and B of formula (I) having a toxicity significantly lower than those of istamycins A and B with an antibacterial activity higher than that of fortimicin A and of the same level as those of istamycins A and B. These compounds may be prepared by reacting 1,2',6'-tri-N-protected istamycins A and B of formula (V) with an iminoether.
Claims5
Formimidoylistamycins A and B of formula (I):
- ##STR8## wherein X represents an amino group and Y represents a hydrogen atom for formimidoylistamycin A or X represents a hydrogen atom and Y represents an amino group for formimidoylistamycin B, and their acid addition salts.
Formimidoylistamycin A and an acid addition salt thereof.
Formimidoylistamycin B and an acid addition salt thereof.
A pharmaceutical composition comprising a safe and effective antibacterial amount of at least one of formimidoylistamycin A, formimidoylistamycin B and pharmaceutically acceptable acid-addition salts thereof, in combination with a pharmaceutically acceptable carrier.
A method for inhibiting the bacterial growth which comprises administering an antibacterially effective amount of at least one of formimidoylistamycin A, formimidoylistamycin B and pharmaceutically acceptable acid-addition salts thereof to an animal susceptible to the bacterial growth.
Dependencies are inferred from the claim text.