Novel 16-membered macrolides modified at C-12 and C-13 positions of midecamycin A1 and miokamycin. Part 1: Synthesis and evaluation of 12,13-carbamate and 12-arylalkylamino-13-hydroxy analogues.

摘要: Abstract Design and synthesis of 16-membered macrolides modified at the C-12 13 positions are described. The compounds we report here have an arylalkylamino group attached to position macrolactone. Both types derivatives, 12,13-cyclic carbamates non-carbamate analogues, were synthesized via 12-amino-13-hydroxy intermediates derived from 12,13-epoxide that was prepared by selective epoxidation C-13 positions. 4′-Hydroxyl analogues also acidic hydrolysis a neutral sugar. These evaluated for in vitro antibacterial activity against respiratory tract pathogens. Some these exhibited improved compared with corresponding parent compound.