Literature DB >> 12760896

Prodrugs of cephalosporin RWJ-333441 (MC-04,546) with improved aqueous solubility.

Scott J Hecker1, Trevor Calkins, Mary E Price, Keith Huie, Sharon Chen, Tomasz W Glinka, Michael N Dudley.   

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.

Entities:  

Mesh：

Substances：

Year:  2003        PMID： 12760896      PMCID： PMC155843          DOI： 10.1128/AAC.47.6.2043-2046.2003

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.191


  6 in total

Review 1.  The chemistry and biological profile of trovafloxacin.

Authors:  K E Brighty; T D Gootz
Journal:  J Antimicrob Chemother       Date:  1997-06       Impact factor: 5.790

2.  In vitro activities of RWJ-54428 (MC-02,479) against multiresistant gram-positive bacteria.

Authors:  S Chamberland; J Blais; M Hoang; C Dinh; D Cotter; E Bond; C Gannon; C Park; F Malouin; M N Dudley
Journal:  Antimicrob Agents Chemother       Date:  2001-05       Impact factor: 5.191

3.  Discovery of RWJ-54428 (MC-02,479), a new cephalosporin active against resistant gram-positive bacteria.

Authors:  S J Hecker; T W Glinka; A Cho; Z J Zhang; M E Price; S Chamberland; D Griffith; V J Lee
Journal:  J Antibiot (Tokyo)       Date:  2000-11       Impact factor: 2.649

4.  In vitro and in vivo properties of Ro 63-9141, a novel broad-spectrum cephalosporin with activity against methicillin-resistant staphylococci.

Authors:  P Hebeisen; I Heinze-Krauss; P Angehrn; P Hohl; M G Page; R L Then
Journal:  Antimicrob Agents Chemother       Date:  2001-03       Impact factor: 5.191

5.  Relationships between structure, antibacterial activity, serum stability, pharmacokinetics and efficacy in 3-(heteroarylthio)cephems. Discovery of RWJ-333441 (MC-04,546).

Authors:  Tomasz Glinka; Keith Huie; Aesop Cho; Maria Ludwikow; Johanne Blais; David Griffith; Scott Hecker; Michael Dudley
Journal:  Bioorg Med Chem       Date:  2003-02-20       Impact factor: 3.641

6.  Investigation of (Oxodioxolenyl)methyl carbamates as nonchiral bioreversible prodrug moieties for chiral amines.

Authors:  J Alexander; D S Bindra; J D Glass; M A Holahan; M L Renyer; G S Rork; G R Sitko; M T Stranieri; R F Stupienski; H Veerapanane; J J Cook
Journal:  J Med Chem       Date:  1996-01-19       Impact factor: 7.446
  6 in total
  2 in total

1.  Benzotriazole-Mediated Synthesis and Antibacterial Activity of Novel N-Acylcephalexins.

Authors:  Khalid A Agha; Nader E Abo-Dya; Tarek S Ibrahim; Eatedal H Abdel-Aal; Wael A Hegazy
Journal:  Sci Pharm       Date:  2016-04-13

Review 2.  Prodrugs for amines.

Authors:  Ana L Simplício; John M Clancy; John F Gilmer
Journal:  Molecules       Date:  2008-03-03       Impact factor: 4.411
  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.