Deformyltylosin derivatives

Details Deformyltylosin derivatives Deformyltylosin derivatives

1980-09-05

1982-08-17

Hazel, Blondel

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

Organic compounds

Carbohydrates or derivatives

C07H 1708

Patent

active

043450695

ABSTRACT:
Deformyltylosin derivatives of the formula ##STR1## wherein A is ##STR2## --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --, R.sub.1 is hydrogen, lower alkanoyl or aryl-lower alkanoyl, X.sub.1 and X.sub.2 are hydrogen or are connected to form a valence bond, Y.sub.1 and Y.sub.2 are hydrogen or are connected to form a valence bond, Q.sub.1 is hydrogen or methyl, Q.sub.2 is hydrogen or ##STR3## R.sub.2 is hydrogen or lower alkanoyl, R is hydrogen or ##STR4## R.sub.3 is hydrogen or C.sub.2-5 alkanoyl, and R.sub.4 is hydrogen or C.sub.2-6 alkanoyl, and when R.sub.3 is not hydrogen, then R.sub.4 is not hydrogen, or a pharmaceutically acceptable salt thereof, have strong antibacterial activities as compared to the known antibiotic tylosin, and also have enhanced antibacterial activities against all macrolide antibiotic-resistant strains such as A, B and C group strains, and have higher blood levels as compared with tylosin.

REFERENCES:
patent: 3321368 (1967-05-01), Whaley et al.
patent: 3769273 (1973-10-01), Massey
"Antimicrobial Agents and Chemotherapy--1963"-Proceedings of the 3rd Interscience Conference on Antimicrobial Agents & Chemotherapy, Wash. D.C., Oct. 28-30, 1963; Editor J. C. Sylvester-American Society for Microbiology, pp. 45-48.
Tylosin, a New Antibiotic: II. Isolation, Properties, and Preparation of Desmycosin, a Microbiologically Active Degradation Product; Authors-Robert L. Hamill et al., "Antibiotics and Chemotherapy", May 1961, vol. XI, No. 5, pp. 328-335.

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