| abstract |
"MACROLIDS WITH ANTIBACTERIAL ACTIVITY". The invention provides novel macrolide antibiotics of formula (I) with improved biological properties and stability of formula (I): wherein R1 is hydrogen, cyano, -S (L) -M-R2A2, -S (O) (L) ~ m ~ R ^ 2 ^, or -S (O) ~ 2 ~ (L) ~ m ~ R ^ 2 ^; L represents - (CH ~ 2 ~) ~ n ~ - or - (CH ~ 2 ~) ~ n ~ Z (CH ~ 2 ~) ~ 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; R2 is hydrogen, alkyl, heterocyclyl or aryl; whose heterocyclyl and aryl groups may be further substituted; * denotes a chiral center which is in (R) or (S) form and pharmaceutically acceptable acid addition salts or in vivo cleavable esters thereof. |