NOVEL 3-DEOXY-3-DESCLADINOSYL-6-O-METHYL ERYTHROMYCIN-A ANALOGS - SYNTHESIS AND IN-VITRO ACTIVITY

A series of novel 3-deoxy-3-des-cladinosyl-6-O-methyl erythromycin A a nalogues has been synthesized and evaluated in vitro for antibacterial activity. These analogues were readily synthesized by tributyltin hyd ride-mediated radical reduction of a 3-O-xanthyl intermediate to affor d the 3-deoxy macrolide. A number of oxime, carbonate, and carbamate d erivatives were synthesized and evaluated for antibacterial activity. Overall, these analogues had fairly good antibacterial activity agains t gram-positive bacteria, although they were generally less potent tha n the corresponding 3-O-cladinosyl or 3-keto analogues. (C) 1997 Elsev ier Science Ltd. All rights reserved.