9-dihydro-9-O-alkyldesmycosin derivatives

Details 9-dihydro-9-O-alkyldesmycosin derivatives 9-dihydro-9-O-alkyldesmycosin derivatives

1989-12-14

1991-06-25

Peselev, Elli

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

Organic compounds

Carbohydrates or derivatives

514 30, A61K 3170, C07H 1708

Patent

active

050268325

ABSTRACT:
9-Dihydro-9-O-alkyldesmycosin derivatives and their salts are disclosed. The 9-dihydro-9-O-alkyldesmycosin derivatives are represented by the following formula (I), ##STR1## --wherein X represents an --O-- mycinose or a di-lower alkylamino group, R.sup.1 represents a hydrogen atom or a lower alkanoyl group, R.sup.2 represents a lower alkyl group, a cycloalkyl-lower group, or phenyl-lower alkyl group which may have a substituent, and R.sup.3 represents a hydrogen atom or a hydroxyl group. The compounds and the salts are useful as an antimicrobial agent. Unlike known desmycosin derivatives, the compounds give a high blood concentration by oral administration.

REFERENCES:
J. Med. Chem., 31, 1988, pp. 1631-1641, H. A. Kirst, et al., "Synthesis and Evaluation of Tylosin-Related Macrolides Modified at the Aldehyde Function: A New Series of Orally Effective Antibiotics".

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