The invention provides new macrolides antibiotics of formula I with
improved biological properties and improved stability of the formula
##STR1##
wherein
R.sup.1 is hydrogen, cyano, --S(L).sub.m R.sup.2, --S(O)(L).sub.m R.sup.2,
or --S(O).sub.2 (L).sub.m R.sup.2 ;
L represents --(CH.sub.2).sub.n -- or --(CH.sub.2).sub.n Z(CH.sub.2).sub.n'
--;
m is 0 or 1;
n is 1, 2, 3, or 4;
n' is 0, 1, 2, 3, or 4;
Z is O, S or NH;
R.sup.2 is hydrogen, alkyl, heterocyclyl or aryl; which heterocyclyl and
the aryl groups may be further substituted;
* indicates a chiral center which is in the (R) or (S) form,
as well as a pharmaceutically acceptable acid addition salts or in vivo
cleavable esters thereof.
De uitvinding voorziet nieuwe macrolides antibiotica van formule I van betere biologische eigenschappen en betere stabiliteit van de formule ## STR1 ## waarin R.sup.1 waterstof, cyano, -- S(L).sub.m R.sup.2, -- S(O)(L).sub.m R.sup.2, of -- S(O).sub.2 (L).sub.m R.sup.2 is; L vertegenwoordigt -- (CH.sub.2).sub.n -- of -- (CH.sub.2).sub.n Z(CH.sub.2).sub.n ' ; m is 0 of 1; n is 1..2..3, of 4; n ' is 0..1..2..3, of 4; Z is O, S of NH; R.sup.2 is waterstof, alkyl, heterocyclyl of aryl; welke heterocyclyl en aryl groepen kan worden gesubstitueerd verder; * wijst op een chiral centrum dat in (R) of (S) vorm, evenals een farmaceutisch aanvaardbare zure toevoegingszouten of levende splijtbare esters daarvan zijn.
