Synthesis and antibacterial activity of C6-carbazate ketolides
摘要:
A novel series of ketolides containing heteroaryl groups that are linked to the erythronolide ring via a C6-carbazate functionality has been successfully synthesized. Careful modulation of the heteroaryl groups, the length and degree of saturation of the C6-carbazate linker, and the substituents present on each of the carbazate nitrogens led to compounds with potent activity against key bacterial respiratory pathogens. The best analogs of this series had in vitro and in vivo (sc dosing) profiles that were comparable to telithromycin. (c) 2006 Elsevier Ltd. All rights reserved.
DOI:
10.1016/j.bmcl.2006.09.036
作为产物:
描述:
碘代三甲硅烷 、 2-[4-[(E)-2-methoxyethenyl]phenyl]-pyrazine 、 碳酸氢钠 在
碳酸氢钠 、 二氯甲烷 、 Sodium sulfate-III 作用下,
以
二氯甲烷 为溶剂,
反应 18.0h,
以to give 110 mg (68%) of the title compound的产率得到4-pyrazinylbenzeneacetaldehyde
[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.