Literature DB >> 17350259

Quinazolinone fungal efflux pump inhibitors. Part 3: (N-methyl)piperazine variants and pharmacokinetic optimization.

William J Watkins1, Lee Chong, Aesop Cho, Ramona Hilgenkamp, Maria Ludwikow, Negar Garizi, Nadeem Iqbal, John Barnard, Rajeshwar Singh, Deidre Madsen, Karen Lolans, Olga Lomovskaya, Uma Oza, Padmapriya Kumaraswamy, Andrea Blecken, Shuang Bai, David J Loury, David C Griffith, Michael N Dudley.   

Abstract

Further structure-activity relationships of a novel series of fungal efflux pump inhibitors with respect to potentiation of the activity of fluconazole against strains of C. albicans and C. glabrata over-expressing ABC-type efflux pumps are systematically explored. Rat protein binding and pharmacokinetics of selected analogues are reported.

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Year:  2007        PMID: 17350259     DOI: 10.1016/j.bmcl.2007.02.047

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Permeability Barrier of Gram-Negative Cell Envelopes and Approaches To Bypass It.

Authors:  Helen I Zgurskaya; Cesar A Löpez; S Gnanakaran
Journal:  ACS Infect Dis       Date:  2015       Impact factor: 5.084

Review 2.  Microbial efflux pump inhibition: tactics and strategies.

Authors:  George P Tegos; Mark Haynes; J Jacob Strouse; Mohiuddin Md T Khan; Cristian G Bologa; Tudor I Oprea; Larry A Sklar
Journal:  Curr Pharm Des       Date:  2011       Impact factor: 3.116

3.  ABC transporter Cdr1p contributes more than Cdr2p does to fluconazole efflux in fluconazole-resistant Candida albicans clinical isolates.

Authors:  Ann R Holmes; Ya-Hsun Lin; Kyoko Niimi; Erwin Lamping; Mikhail Keniya; Masakazu Niimi; Koichi Tanabe; Brian C Monk; Richard D Cannon
Journal:  Antimicrob Agents Chemother       Date:  2008-08-18       Impact factor: 5.191

  3 in total

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