23-O-Acyl-23-demycinosyldesmycosin derivatives

Details 23-O-Acyl-23-demycinosyldesmycosin derivatives 23-O-Acyl-23-demycinosyldesmycosin derivatives

1983-01-24

1984-12-25

Brown, Johnnie R.

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

Organic compounds

Carbohydrates or derivatives

536115, C07H 1708

Patent

active

044905246

ABSTRACT:
Compounds of the formula ##STR1## wherein R.sub.1 is optionally substituted phenyl, thienyl, 2-amino-4-thiazolyl or 2-chloroacetamido-4-thiazolyl; A is lower alkylene, lower alkenylene, or lower alkylene substituted by lower alkyl, amino, lower alkoxyimino or phenyl-Z-group wherein Z is a single bond or --S-- or --SO.sub.2 --, but when R.sub.1 is 2-amino-4-thiazolyl or 2-chloroacetamido-4-thiazolyl then A is lower alkylene substituted by lower alkoxyimino; R.sub.2 is hydrogen or hydroxyl; X is oxygen or sulfur and n=0 or 1, or a non-toxic salt thereof. These compounds have a stronger antibacterial activity against Gram positive bacteria as compared with known macrolide antibiotics such as erythromycin and tylosin, and also have an equivalent level of antibacterial activity against Gram negative bacteria as compared with that of erythromycin, and hence may be useful for clinical use. These compounds are also useful for feed additives and growth stimulants.

REFERENCES:
patent: 4141971 (1979-02-01), Krausz et al.
Tetrahedron Letters, No. 54, pp. 4737-4740, 1970, "The Structure of Tylosin.sup.1,2 ", by R. B. Morin et al.
The Journal of Antibiotics, vol. XXXIV, No. 10, pp. 1374-1376, "Synthesis of 4'-Deoxymycaminosyl Tylonolide".

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