Literature DB >> 17482460

Synthesis and antifungal activities of new fluconazole analogues with azaheterocycle moiety.

Nicolas Lebouvier1, Fabrice Pagniez, Muriel Duflos, Patrice Le Pape, Young Min Na, Guillaume Le Baut, Marc Le Borgne.   

Abstract

A series of fluconazole analogues 5-20 incorporating azaindole and indole moieties were prepared using oxirane intermediates synthesized under microwave irradiation. All of the compounds were evaluated in vitro against two clinically important fungi, Candida albicans and Aspergillus fumigatus. Four derivatives 6, 13, 14 and 18 exerted high antifungal activity against C. albicans with MIC(80) values 3- to 28-fold lower than that of fluconazole.

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Year:  2007        PMID： 17482460     DOI： 10.1016/j.bmcl.2007.04.038

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


  8 in total

1.  In vitro synergistic activity of diketopiperazines alone and in combination with amphotericin B or clotrimazole against Candida albicans.

Authors:  S Nishanth Kumar; Bala Nambisan; C Mohandas; A Sundaresan
Journal:  Folia Microbiol (Praha)       Date:  2013-02-28       Impact factor: 2.099

2.  In vitro investigation of antifungal activity of allicin alone and in combination with azoles against Candida species.

Authors:  Alireza Khodavandi; Fahimeh Alizadeh; Farzad Aala; Zamberi Sekawi; Pei Pei Chong
Journal:  Mycopathologia       Date:  2009-11-19       Impact factor: 2.574

3.  Crystal structure of 2-[2-(2,5-di-chloro-benz-yloxy)-2-(furan-2-yl)eth-yl]-2H-indazole.

Authors:  Özden Özel Güven; Gökhan Türk; Philip D F Adler; Simon J Coles; Tuncer Hökelek
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2016-09-05

4.  Design, Synthesis, and Biological Activity of New Triazole and Nitro-Triazole Derivatives as Antifungal Agents.

Authors:  Hossein Sadeghpour; Soghra Khabnadideh; Kamiar Zomorodian; Keyvan Pakshir; Khadijeh Hoseinpour; Nabiollah Javid; Ehsan Faghih-Mirzaei; Zahra Rezaei
Journal:  Molecules       Date:  2017-07-10       Impact factor: 4.411

5.  2-(2H-Indazol-2-yl)-1-phenyl-ethanone.

Authors:  Ozden Ozel Güven; Gökhan Türk; Philip D F Adler; Simon J Coles; Tuncer Hökelek
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-01-04

6.  2-[2-(2,6-Di-chloro-benz-yloxy)-2-phenyl-eth-yl]-2H-indazole.

Authors:  Ozden Ozel Güven; Gökhan Türk; Philip D F Adler; Simon J Coles; Tuncer Hökelek
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2014-03-08

7.  Biological exploration of a novel 1,2,4-triazole-indole hybrid molecule as antifungal agent.

Authors:  Fabrice Pagniez; Nicolas Lebouvier; Young Min Na; Isabelle Ourliac-Garnier; Carine Picot; Marc Le Borgne; Patrice Le Pape
Journal:  J Enzyme Inhib Med Chem       Date:  2020-12       Impact factor: 5.051

8.  Synthesis, Optimization, Antifungal Activity, Selectivity, and CYP51 Binding of New 2-Aryl-3-azolyl-1-indolyl-propan-2-ols.

Authors:  Nicolas Lebouvier; Fabrice Pagniez; Young Min Na; Da Shi; Patricia Pinson; Mathieu Marchivie; Jean Guillon; Tarek Hakki; Rita Bernhardt; Sook Wah Yee; Claire Simons; Marie-Pierre Lézé; Rolf W Hartmann; Angélique Mularoni; Guillaume Le Baut; Isabelle Krimm; Ruben Abagyan; Patrice Le Pape; Marc Le Borgne
Journal:  Pharmaceuticals (Basel)       Date:  2020-08-08
  8 in total

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