Literature DB >> 27914798

Antimycobacterial activity of novel hydrazide-hydrazone derivatives with 2H-chromene and coumarin scaffold.

Violina T Angelova1, Violeta Valcheva2, Nikolay G Vassilev3, Rosen Buyukliev4, Georgi Momekov5, Ivan Dimitrov4, Luciano Saso6, Mirjana Djukic7, Boris Shivachev8.   

Abstract

This study reports the synthesis of new 2H-chromene or coumarin based acylhydrazones, which were evaluated for their in vitro antimycobacterial activity against reference strain Mycobacterium tuberculosis H37Rv and compared to the first-line antituberculosis drugs, isoniazid (INH) and ethambutol (EMB). The most active compounds 7m (MIC 0.13μM), 7o (MIC 0.15μM) and 7k (MIC 0.17μM) demonstrated antimycobacterial activity at submicromolar concentration level and remarkably minimal associated cytotoxicity in the human embryonic kidney cell line HEK-293T. Structure-activity relationship for this class of compounds has been established.
Copyright © 2016 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  2H-Chromene; Antitmycobacterial activity; Coumarin; Cytotoxicity; Hydrazide-hydrazone

Mesh：

Substances：

Year:  2016        PMID： 27914798     DOI： 10.1016/j.bmcl.2016.11.071

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


  3 in total

1.  Development of New Antimycobacterial Sulfonyl Hydrazones and 4-Methyl-1,2,3-thiadiazole-Based Hydrazone Derivatives.

Authors:  Violina T Angelova; Tania Pencheva; Nikolay Vassilev; Elena K-Yovkova; Rositsa Mihaylova; Boris Petrov; Violeta Valcheva
Journal:  Antibiotics (Basel)       Date:  2022-04-22

2.  Crystal structures and Hirshfeld surface analyses of (E)-N'-benzyl-idene-2-oxo-2H-chromene-3-carbo-hydrazide and the disordered hemi-DMSO solvate of (E)-2-oxo-N'-(3,4,5-trimeth-oxybenzyl-idene)-2H-chromene-3-carbohydrazide: lattice energy and inter-molecular inter-action energy calculations for the former.

Authors:  Ligia R Gomes; John Nicolson Low; James L Wardell; Camiola Capelini; Vitoria R F Câmara; Edson F da Silva; Samir A Carvalho
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2019-09-03

3.  A Coumarin-Based Analogue of Thiacetazone as Dual Covalent Inhibitor and Potential Fluorescent Label of HadA in Mycobacterium tuberculosis.

Authors:  Asma Farjallah; Laurent R Chiarelli; Martin Forbak; Giulia Degiacomi; Mathieu Danel; Fernanda Goncalves; Chantal Carayon; Cendrine Seguin; Marco Fumagalli; Monika Záhorszká; Elodie Vega; Souhir Abid; Anna Grzegorzewicz; Mary Jackson; Antonio Peixoto; Jana Korduláková; Maria Rosalia Pasca; Christian Lherbet; Stefan Chassaing
Journal:  ACS Infect Dis       Date:  2021-02-22       Impact factor: 5.084
  3 in total

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