| Literature DB >> 10560728 |
A Denis1, C Agouridas, J M Auger, Y Benedetti, A Bonnefoy, F Bretin, J F Chantot, A Dussarat, C Fromentin, S G D'Ambrières, S Lachaud, P Laurin, O Le Martret, V Loyau, N Tessot, J M Pejac, S Perron.
Abstract
In the search for new ketolides with improved activities against erythromycin-resistant S. pneumoniae and H. influenzae we synthesized a new 11,12 carbamate ketolide substituted by an imidazo-pyridyl side chain: HMR 3647. This compound demonstrated a potent activity against erythromycin susceptible and resistant pathogens, including penicillin G/erythromycin A-resistant S. pneumoniae and H. influenzae. In vivo, HMR 3647 displayed good pharmacokinetic parameters (Cmax = 2.9 microg/ml, bioavailability=49%, AUC0.8 = 17.2 microg.h/l, t1/2=1h) and was shown to have a high therapeutic efficacy in mice infected by various respiratory pathogens, including multi-resistant S. pneumoniae and Gram negative bacteria such as H. influenzae. HMR 3647 appears to be a very promising agent for the treatment of respiratory infections and is currently in clinical trials.Entities:
Mesh：
Substances：
Year: 1999 PMID： 10560728 DOI： 10.1016/s0960-894x(99)00534-x
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823