2003-06-01·Antimicrobial Agents and Chemotherapy2区 · 医学
Prodrugs of Cephalosporin RWJ-333441 (MC-04,546) with Improved Aqueous Solubility
2区 · 医学
Article
作者: Calkins, Trevor ; Price, Mary E. ; Dudley, Michael N. ; Huie, Keith ; Chen, Sharon ; Hecker, Scott J. ; Glinka, Tomasz W.
ABSTRACT
To improve the aqueous solubility of anti-methicillin-resistant
Staphylococcus aureus
cephalosporin RWJ-333441 for parenteral administration, acyl derivatives of the C-3 primary amino group were prepared and evaluated for solubility, cleavage in serum in vitro, and conversion to RWJ-333441 in vivo. Improved solubility at physiologic pH values and release of RWJ-333441 in vitro and in vivo were observed for several prodrugs, including the aspartate derivative RWJ-333442.
2001-02-01·Current opinion in investigational drugs (London, England : 2000)
RWJ-333441 Microcide/RW Johnson.
Review
作者: Jiraskova, N
Microcide and RW Johnson Pharmaceutical Research Institute are investigating a novel cephalosporin prodrug RWJ-333442 for the potential treatment of bacterial infections. RWJ-333442 is the prodrug of RWJ-333441; it has an improved solubility profile and studies are in progress in human serum, rats and rhesus macaques [382578], [382862], [383594].