New antibacterial erythromycin derivs. - with 12,11-oxycarbonylimino gp. N-substd. by aryl-alkenyl or aryl-alkynyl.

摘要

Erythromycin derivs. of formula (I) and their acid-soln. salts are new: R = (CH2)mCA = CB(CH2)nAr; m and n = 0-6; A and B = H, halogen, or 1-8C alkyl, or A+B = a bond; Ar = aryl or 5- or 6-membered heteroaryl, opt. substd. by COOH (opt. in salt, ester or amide form), CN, NO2, R1, OR1, SR1, NHR1 and/or NR1R2; R1 = opt. halo-substd. 1-12C alkyl, 2-12C alkenyl, or 2-12C alkynyl; R1 and R2 = H or 1-12C alkyl; Z = H or 1-18C carboxylic acyl. A typical cpd. is 1,12-dideoxy-3-de(2,6-dideoxy-3-C-methyl-3-0-methyl-a-L- ribohexopyranosyloxy)-6-0-methyl-3-oxo-12,11-(oxycarbonyl (4-phenyl-3-butenyl)imino)-erythromycin (Ia). USE - (I) are antibacterial agents esp. active against Gram-positive bacteria, e.g. staphylococci, streptococci and pneumococci, and also active against Haemophilus influenzae, Mycoplasma pneumoniae and Rickettsia, Chlamydia, Legionella, Ureaplasma, Toxoplasma and Mycobacterium spp.