Acyl derivatives of 16-membered macrolides. II. Antibacterial activities and serum levels of 3"-O-acyl derivatives of leucomycin.
- 1 January 1981
- journal article
- research article
- Published by Japan Antibiotics Research Association in The Journal of Antibiotics
- Vol. 34 (8) , 1011-1018
- https://doi.org/10.7164/antibiotics.34.1011
Abstract
3''''-O-Acylation of leucomycin A5 increased its in vitro antibacterial activity against sensitive microorganisms and also some resistant ones. An increased effect was particularly noted when an acetyl or propionyl group was introduced. Acylation of the C-3 and C-9 hydroxyl groups reduced the antibacterial activity in vitro. Introduction of an acyl group at the C-3'''' hydroxyl group increased the serum level of the compound. The increase in [amimal] serum level from 3''''-O-acylation is higher than that from 3-O-acylation. The serum level of the 3''''-O-propionyl derivative of leucomycin A5 was higher than that of the 3''''-O-acetyl derivative. 3''''-O-Propionylleucomycin A5 (5) was the derivative that showed the highest antibacterial activity and yielded the higest serum level among the derivatives examined.This publication has 1 reference indexed in Scilit:
- Acyl derivatives of 16-membered macrolides. I. Synthesis and biological properties of 3"-O-propionylleucomycin A5 (TMS-19-Q).The Journal of Antibiotics, 1981