Citation
Sj. Hecker et al., Discovery of RWJ-54428 (MC-02,479), a new cephalosporin active against resistant Gram-positive bacteria, J ANTIBIOT, 53(11), 2000, pp. 1272-1281
Citations number
9
Categorie Soggetti
Microbiology
Journal title
JOURNAL OF ANTIBIOTICS
ISSN journal
00218820
→ ACNP
Volume
53
Issue
11
Year of publication
2000
Pages
1272 - 1281
Database
ISI
SICI code
0021-8820(200011)53:11<1272:DOR(AN>2.0.ZU;2-Z
Abstract
The discovery of RWJ-54428 (MC-02,479), a new cephalosporin displaying prom
ising activity against sensitive and resistant Gram-positive bacteria, is d
escribed. Progressive structural modification from the previously reported
3-phenylthiocephem MC-02,331 afforded an overall increase in potency agains
t MRSA while retaining other key properties such as acceptable solubility a
nd serum binding. Evaluation of the iii vitro potency and lit vivo efficacy
of a series of closely related compounds resulted in selection of RWJ-5442
8 (MC-02,479) for further studies.