Activities of HMR 3787, a new 2-fluoroketolide, and its (des)-fluor derivative, RU 64399, were tested against 111 Haemophilus influenzae and 26 H. parainfluenzae strains and compared with those of telithromycin, erythromycin, azithromycin, and clarithromycin. HMR 3787 and RU 64399 MICs were comparable with those of azithromycin but were less affected by incubation in CO(2). Time-kill studies of 12 strains showed that HMR 3787, RU 64399, and telithromycin were bactericidal against all strains after 24 h at two times the MIC.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC149015 | PMC |
| http://dx.doi.org/10.1128/AAC.47.1.405-407.2003 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Interaction of macrolides and ketolides with the phagocytic cell line PLB-985.
J Chemother
August 2003
Faculté des Sciences 1, Ain Chock, BP 5366, Maarif, Casablanca, Morocco.
Interactions between antibacterial agents and polymorphonuclear neutrophils (PMNs) are a major focus of investigation. Owing to the variable drug susceptibility of PMNs from different individuals, in vitro studies require samples from large panels of healthy volunteers to reach statistical significance. Here, we used a phagocytic cell line, PLB-985, which can differentiate into mature PMNs in vitro, for the study of cellular interactions (drug uptake and antioxidant effects) of two macrolides (azithromycin and roxithromycin) and four ketolides [HMR 3004, HMR 3647 (telithromycin), HMR 3562 and HMR 3787].
View Article and Find Full Text PDFActivities of HMR 3787 and RU 64399 compared with those of four other agents against Haemophilus influenzae and Haemophilus parainfluenzae.
Antimicrob Agents Chemother
January 2003
Hershey Medical Center, Hershey, Pennsylvania 17033, USA.
Activities of HMR 3787, a new 2-fluoroketolide, and its (des)-fluor derivative, RU 64399, were tested against 111 Haemophilus influenzae and 26 H. parainfluenzae strains and compared with those of telithromycin, erythromycin, azithromycin, and clarithromycin. HMR 3787 and RU 64399 MICs were comparable with those of azithromycin but were less affected by incubation in CO(2).
View Article and Find Full Text PDFHMR-3562. Aventis Pharma.
Curr Opin Investig Drugs
December 2001
Infectious Disease Research, Abbott Laboratories, Abbott Park, IL 60064-3537, USA.
Aventis Pharma (formerly Hoechst Marion Roussel) is investigating the ketolides HMR-3562 and HMR-3787 as potential antibacterial agents. The compounds belong to a series of 2-fluoroketolides. They have exhibited potency against a range of gram-positive bacteria and other respiratory tract pathogens including Haemophilus influenzae in vitro and in vivo.
View Article and Find Full Text PDFActivities of a new fluoroketolide, HMR 3787, and its (des)-fluor derivative RU 64399 compared to those of telithromycin, erythromycin A, azithromycin, clarithromycin, and clindamycin against macrolide-susceptible or -resistant Streptococcus pneumoniae and S. pyogenes.
Antimicrob Agents Chemother
November 2001
Hershey Medical Center, Hershey, Pennsylvania 17033, USA.
Activities of HMR 3787 and RU 64399 were compared to those of three macrolides, telithromycin, and clindamycin against 175 Streptococcus pneumoniae isolates and 121 Streptococcus pyogenes isolates. HMR3787 and telithromycin were the most active compounds tested against pneumococci. Telithromycin and RU 64399 were equally active against macrolide-susceptible (MICs, 0.
View Article and Find Full Text PDFCellular uptake of two fluoroketolides, HMR 3562 and HMR 3787, by human polymorphonuclear neutrophils in vitro.
Antimicrob Agents Chemother
October 2001
INSERM U479, CHU Xavier Bichat, 16 rue Henri Huchard, 75018 Paris, France.
We analyzed the cellular accumulation of two new fluoroketolides, HMR 3562 and HMR 3787, by human polymorphonuclear neutrophils (PMN) in vitro. Both compounds were rapidly taken up by PMN, with a cellular-to-extracellular concentration ratio (C/E) of about 141 (HMR 3562) and 117 (HMR 3787) at 5 min, and this was followed by a plateau at 60 to 180 min, with a C/E of >300 at 180 min. Both ketolides were mainly located in PMN granules (about 75%) and egressed slowly from loaded cells (about 40% at 60 min), owing to avid reuptake.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!