Literature DB >> 25736994

Synthesis of novel pleuromutilin derivatives. Part 1: preliminary studies of antituberculosis activity.

Ying-Jie Dong1, Zi-Hui Meng1, Yan-Qing Mi1, Chun Zhang1, Zhi-Hao Cui1, Peng Wang1, Zhi-Bin Xu2.   

Abstract

The worldwide threat from tuberculosis (TB) has resulted in great demand for new drugs, particularly those that can treat multidrug-resistant TB. We synthesized novel pleuromutilin derivatives with N-benzylamine side chain substituted at the C14 position and evaluated their activity in vitro against a virulent strain of Mycobacterium tuberculosis (H37Rv). The primary assay results showed that five compounds inhibited the H37Rv at 20μM, with a MIC of one of the analogues as low as 7.2μM.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Antitubercular activity; N-Benzylamine side chain; Pleuromutilin derivatives

Mesh:

Substances:

Year:  2015        PMID: 25736994     DOI: 10.1016/j.bmcl.2015.02.023

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


  5 in total

1.  Heterologous expression reveals the biosynthesis of the antibiotic pleuromutilin and generates bioactive semi-synthetic derivatives.

Authors:  Fabrizio Alberti; Khairunisa Khairudin; Edith Rodriguez Venegas; Jonathan A Davies; Patrick M Hayes; Christine L Willis; Andy M Bailey; Gary D Foster
Journal:  Nat Commun       Date:  2017-11-28       Impact factor: 14.919

2.  Insights into the Classical Genetics of Clitopilus passeckerianus - the Pleuromutilin Producing Mushroom.

Authors:  Kate M J de Mattos-Shipley; Gary D Foster; Andy M Bailey
Journal:  Front Microbiol       Date:  2017-06-09       Impact factor: 5.640

3.  An antimycobacterial pleuromutilin analogue effective against dormant bacilli.

Authors:  Maddie R Lemieux; Shajila Siricilla; Katsuhiko Mitachi; Shakiba Eslamimehr; Yuehong Wang; Dong Yang; Jeffrey D Pressly; Ying Kong; Frank Park; Scott G Franzblau; Michio Kurosu
Journal:  Bioorg Med Chem       Date:  2018-08-18       Impact factor: 3.641

4.  Identification and manipulation of the pleuromutilin gene cluster from Clitopilus passeckerianus for increased rapid antibiotic production.

Authors:  Andy M Bailey; Fabrizio Alberti; Sreedhar Kilaru; Catherine M Collins; Kate de Mattos-Shipley; Amanda J Hartley; Patrick Hayes; Alison Griffin; Colin M Lazarus; Russell J Cox; Christine L Willis; Karen O'Dwyer; David W Spence; Gary D Foster
Journal:  Sci Rep       Date:  2016-05-04       Impact factor: 4.379

Review 5.  Diterpenes Specially Produced by Fungi: Structures, Biological Activities, and Biosynthesis (2010-2020).

Authors:  Fa-Lei Zhang; Tao Feng
Journal:  J Fungi (Basel)       Date:  2022-02-28
  5 in total

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