Erythromycin series. XII. Antibacterial in vitro evaluation of 10-dihydro-10-deoxo-11-azaerythromycin A: Synthesis and structure-activity relationship of its acyl derivatives.
- 1 January 1987
- journal article
- research article
- Published by Japan Antibiotics Research Association in The Journal of Antibiotics
- Vol. 40 (7) , 1006-1015
- https://doi.org/10.7164/antibiotics.40.1006
Abstract
Antibacterial in vitro evaluation of 10-dihydro-10-deoxo-11-azaerythromycin A (5), the new 15-membered semi-synthetic macrolide antibiotic with nitrogen as additional atom in the aglycone ring of erythromycin A (1), was reported. Although amine (5) and its 13,14-cyclic carbonate (14) were less active than 1 against erythromycin-sensitive Staphylococcus aureus strains they showed advantageous properties against Gram-negative test organisms and clinical isolates. Also, a large number of acyl derivatives of 5 were synthesized and evaluated. N-11 monoacyl compounds exhibited 2 to 50 times lower in vitro antibacterial efficacy than the parent amine (5).This publication has 3 references indexed in Scilit:
- Erythromycin series. Part 11. Ring expansion of erythromycin A oxime by the Beckmann rearrangementJournal of the Chemical Society, Perkin Transactions 1, 1985
- Erythromycin VI: Kinetics of Acid-Catalyzed Hydrolysis of Erythromycin Oxime and ErythromycylamineJournal of Pharmaceutical Sciences, 1978
- ILOTYCIN, A NEW ANTIBIOTIC1952