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.

01 Feb 2001·Current opinion in investigational drugs (London, England : 2000)

RWJ-333441 Microcide/RW Johnson.

Review

Author: 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].

01 Dec 2000·Expert opinion on investigational drugs

40th Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC)

Author: Dougherty, Thomas ; Ho, Hsu-Tso ; Ryan, Brenda ; Wu, Ping ; Barrett, John F ; Frosco, Mary-Beth

The 40th ICAAC Meeting provided one of the widest varieties of new antibacterial and antifungal agents in years, with a range of improved "classical" agents (β-lactams, carbapenems), novel quinolone agents and totally new ideas for novel therapeutic intervention.Among the compounds reported were potent anti-MRSA carbapenems, novel des-fluoroquinolones (BMS 284756/T-3811), non-fluorinated quinolones, quinolone-related antibacterials, novel cephalosporins (cefditoren, RWJ-54428, MC 04546), ketolides (telithromycin, ABT-773), novel streptogramins and novel β-lactamase inhibitors, bacterial and fungal efflux pump inhibitors and novel antifungals (azasordarins, echinocandins, azoles).

100 Deals associated with RWJ-333441

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Indication	Highest Phase	Country/Location	Organization	Date
MRSA - Methicillin resistant Staphylococcus aureus infection	Preclinical	United States	Essential Therapeutics, Inc.	05 Mar 2003
Bacterial Infections	Discovery	United States	Johnson & Johnson Pharmaceutical Research & Development LLC	-

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