1977 年 25 巻 6 号 p. 1624-1629
The structure-activity relationship was studied on 9-acyl derivatives of midecamycin, and 9-acyl and 9-acetyl-4 “-acyl derivatives of 4” -depropionylmidecamycin. Acyl substitution at position 9 of the lactone ring of midecamycin resulted in general in a decrease of in vitro activity, but some of derivatives were superior in in vivo activity. 9-Acyl substitution of 4 “-depropionylmidecamycin retained in vitro bioactivity equal to that of the starting material, and showed improved in vivo activity.
4” -Acyl substitution of 9-acetyl-4″-depropionylmidecamycin resulted in an equal or slight decrease of in vitro activity, but an increase of in vivo activity. High survival rates of acyl derivatives were correlated with high blood concentration.
