ru-66647 has been researched along with Neutropenia* in 2 studies
2 other study(ies) available for ru-66647 and Neutropenia
| Article | Year |
|---|---|
Synthesis and SARs of novel lincomycin derivatives Part 5: optimization of lincomycin analogs exhibiting potent antibacterial activities by chemical modification at the 6- and 7-positions.
In order to modify lincomycin at the C-6 and C-7 positions, we prepared target molecules, which have substituted pipecolinic acid at the 6-amino group and a para-substituted phenylthio group at the C-7 position, in application of palladium-catalyzed cross-coupling as a key reaction. As the result of structure-activity relationship (SAR) studies at the 6-position, analogs possessing 4'-cis-(cyclopropylmethyl)piperidine showed significantly strong antibacterial activities against Streptococcus pneumoniae and Streptococcus pyogenes with an erm gene. On the basis of SAR, we further synthesized novel analogs possessing 4'-cis-(cyclopropylmethyl)piperidine by transformation of a C-7 substituent. Consequently, novel derivatives possessing a para-heteroaromatic-phenylthio group at the C-7 position exhibited significantly strong activities against S. pneumoniae and S. pyogenes with an erm gene even when compared with those of telithromycin. Finally, in vivo efficacy of selected two derivatives was evaluated in a rat pulmonary infection model with resistant S. pneumoniae with erm + mef genes. One of them exhibited strong and constant in vivo efficacy in this model, and both compounds showed strong in vivo efficacy against resistant S. pneumoniae with a mef gene. Topics: Animals; Anti-Bacterial Agents; Bacterial Proteins; Drug Resistance, Bacterial; Ketolides; Lincomycin; Membrane Proteins; Microbial Sensitivity Tests; Neutropenia; Pneumonia, Pneumococcal; Rats; Streptococcus pneumoniae; Streptococcus pyogenes; Structure-Activity Relationship | 2018 |
In vitro activities of the new ketolide HMR 3647 (telithromycin) in comparison with those of eight other antibiotics against viridans group Streptococci isolated from blood of neutropenic patients with cancer.
The in vitro activities of the ketolide telithromycin and eight other antibiotics were tested against 77 strains of viridans group streptococci isolated from blood samples of neutropenic patients. Thirty-one (40.3%) of the strains were resistant to penicillin G, and 27 (35.1%) were resistant to erythromycin A. Telithromycin (MIC range of < or =0.03 to 1 microg/ml) was the most active antimicrobial tested. These data suggest that telithromycin could be useful for treatment of viridans group streptococcal bacteremia in neutropenic patients with cancer. Topics: Anti-Bacterial Agents; Humans; Ketolides; Macrolides; Microbial Sensitivity Tests; Neoplasms; Neutropenia; Streptococcus | 2001 |