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Antimicrobial Agents and Chemotherapy, June 2003, p. 2043-2046, Vol. 47, No. 6
0066-4804/03/$08.00+0     DOI: 10.1128/AAC.47.6.2043-2046.2003
Copyright © 2003, American Society for Microbiology. All Rights Reserved.

Prodrugs of Cephalosporin RWJ-333441 (MC-04,546) with Improved Aqueous Solubility

Scott J. Hecker,* Trevor Calkins, Mary E. Price, Keith Huie, Sharon Chen, Tomasz W. Glinka, and Michael N. Dudley

Microcide Pharmaceuticals, Inc., Mountain View, California

Received 21 October 2002/ Returned for modification 26 January 2003/ Accepted 5 March 2003

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.

* Corresponding author. Present address: 16387 Englewood Ave., Los Gatos, CA 95032. Phone: (408) 356-4421. E-mail: scottjhecker{at}attbi.com.

Antimicrobial Agents and Chemotherapy, June 2003, p. 2043-2046, Vol. 47, No. 6
0066-4804/03/$08.00+0     DOI: 10.1128/AAC.47.6.2043-2046.2003
Copyright © 2003, American Society for Microbiology. All Rights Reserved.





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