38-decarboxy-38-hydroxymethyl derivatives of teiocoplanin antibiotics and a process for preparing them
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United States of America Patent
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Feb 9, 1999
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N/A
app pub date -
Jun 10, 1997
filing date -
Dec 5, 1990
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Abstract
The present invention is directed to novel 38-decarboxy-38-hydroxymethyl derivatives of teicoplanin antiobiotics and a process for preparing them which includes submitted the corresponding lower alkyl ester precursor to a reduction reaction in the presence of an alkali metal borohydride. The compounds of the invention show an improved antibacterial activity against some clinical isolates of Staphylococci somewhat resistant to teicoplanin. The teicoplanin derivatives of the present invention are represented by the following formula: ##STR1## wherein: X represents hydroxymethyl; R represents hydrogen or --N?(C.sub.9 -C.sub.12)aliphatic acyl!-.beta.-D-2-deoxy-2-aminoglucopyranosyl; R.sub.1 represents hydrogen or N-acetyl-.beta.-D-2-deoxy-2-aminoglucopyranosyl; R.sub.2 represents hydrogen of alpha-D-mannopyranosyl; R.sub.3 represents hydrogen or a protecting group of the amino function; and the acid addition salts thereof; with the proviso that R.sub.1 represents hydrogen only when R and R.sub.2 are simultaneously hydrogen.
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