Literature DB >> 24900319

Preparation, gram-negative antibacterial activity, and hydrolytic stability of novel siderophore-conjugated monocarbam diols.

Mark E Flanagan1, Steven J Brickner2, Manjinder Lall1, Jeffrey Casavant1, Laura Deschenes1, Steven M Finegan1, David M George1, Karl Granskog1, Joel R Hardink1, Michael D Huband1, Thuy Hoang1, Lucinda Lamb1, Andrea Marra3, Mark Mitton-Fry1, John P Mueller1, Lisa M Mullins1, Mark C Noe1, John P O'Donnell1, David Pattavina1, Joseph B Penzien1, Brandon P Schuff1, Jianmin Sun1, David A Whipple4, Jennifer Young1, Thomas D Gootz5.   

Abstract

A novel series of monocarbam compounds exhibiting promising antibacterial activity against multidrug resistant Gram-negative microorganisms is reported, along with the synthesis of one such molecule MC-1 (1). Also reported are structure-activity relationships associated with the in vitro and in vivo efficacy of 1 and related analogues in addition to the hydrolytic stability of such compounds and possible implications thereof.

Entities:  

Keywords:  MC-1; Monocarbam; antibiotic; monobactam; siderophore-conjugate; β-lactam

Year:  2011        PMID: 24900319      PMCID: PMC4018130          DOI: 10.1021/ml200012f

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN: 1948-5875            Impact factor:   4.345


  23 in total

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6.  In vitro properties of BAL30072, a novel siderophore sulfactam with activity against multiresistant gram-negative bacilli.

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Journal:  Antimicrob Agents Chemother       Date:  2010-03-22       Impact factor: 5.191

7.  The efficiency of C-4 substituents in activating the beta-lactam scaffold towards serine proteases and hydroxide ion.

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5.  Clinically relevant Gram-negative resistance mechanisms have no effect on the efficacy of MC-1, a novel siderophore-conjugated monocarbam.

Authors:  Craig J McPherson; Lisa M Aschenbrenner; Brian M Lacey; Kelly C Fahnoe; Margaret M Lemmon; Steven M Finegan; Baswanth Tadakamalla; John P O'Donnell; John P Mueller; Andrew P Tomaras
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Review 6.  Antibiotic Hybrids: the Next Generation of Agents and Adjuvants against Gram-Negative Pathogens?

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Review 7.  Exploiting bacterial iron acquisition: siderophore conjugates.

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8.  Synthesis, spectral and extended spectrum beta-lactamase studies of transition metal tetraaza macrocyclic complexes.

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