6-O-Acyl ketolide antibacterials of the formula:
1
wherein R
1
, R
2
, R
3
, R
4
, W, X, X′, Y, and Y′ are as described herein and in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.
6-O-Carbamoyl ketolide antibacterials of the formula:
1
wherein R
1
, R
2
, R
3
, R
4
, R
5
, R
6
, X, X′, Y, and Y′ are as described herein and in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.
The antimicrobial activities of twenty-two substances structurally related to staurosporine, aglycone in the indolocarbazole and bis-indole series were examined against Streptomyces chartreusis and Streptomyces griseus, Bacillus cereus, Escherichia coli, Candida albicans and Botrytis cinerea. Inhibition of sporulation was examined also on the two species of Streptomyces. Unlike literature reports for efficient protein kinase inhibitors, staurosporine and K-252a, no evident correlation could be found either between protein kinase inhibitory potencies and inhibition of sporulation of the Streptomyces species, or protein kinase inhibitory potencies and growth of all microorganisms tested. A weak activity against C. albicans was observed for the chloro-indolocarbazole compounds as already reported for structurally related substances from the cyanobacterium Tolypothrix tjipanasensis.
[EN] 6-O-ACYL KETOLIDE DERIVATIVES OF ERYTHROMYCINE USEFUL AS ANTIBACTERIALS<br/>[FR] DERIVES DE 6-O-ACYL CETOLIDE D'ERYTHROMYCINE UTILES COMME AGENTS ANTI-BACTERIENS
申请人:ORTHO MCNEIL PHARM INC
公开号:WO2003050132A1
公开(公告)日:2003-06-19
6-O-Acyl ketolide antibacterials of formula (I): wherein R?1, R2, R3, R4¿, W, X, X', Y, and Y' are as described herein and in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.
[EN] 6-0-CARBAMOYL KETOLIDE DERIVATIVES OF ERYTHROMYCIN USEFUL AS ANTIBACTERIALS<br/>[FR] DERIVES 6-0-CARBAMOYLCETOLIDE DE L'ERYTHROMYCINE UTILES COMME ANTIBACTERIENS
申请人:ORTHO MCNEIL PHARM INC
公开号:WO2002046204A1
公开(公告)日:2002-06-13
6-0-carbamoyl ketolide antibacterials of the formula: wherein R?1, R2, R3, R4, R5¿, R6, X, X', Y, and Y' are as described herein and in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.