Literature DB >> 19765866

Synthesis and antimycobacterial activity of N'-[(E)-(monosubstituted-benzylidene)]-2-pyrazinecarbohydrazide derivatives.

Fátima M F Vergara1, Camilo H da S Lima, Maria das Graças M de O Henriques, André L P Candéa, Maria C S Lourenço, Marcelle de L Ferreira, Carlos R Kaiser, Marcus V N de Souza.   

Abstract

The present article describes a series of twenty-six N'-[(E)-(monosubstituted-benzylidene)]-2-pyrazinecarbohydrazide (4-29), which were synthesized and evaluated for their cell viabilities in non infected and infected macrophages with Mycobacterium bovis Bacillus Calmette-Guerin (BCG). Afterwards, the non-cytotoxic compounds (4, 6, 8, 15, 21, 23, 24, 27 and 28) were assessed against Mycobacterium tuberculosis ATCC 27294 using the micro plate Alamar Blue assay (MABA) and the activity expressed as the minimum inhibitory concentration (MIC) in microg/mL. The compounds 6, 23, 27 and 28 exhibited a significant activity (50-100 microg/mL) when compared with first line drugs such as pyrazinamide and were not cytotoxic in their respective MIC values.

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Year:  2009        PMID: 19765866     DOI: 10.1016/j.ejmech.2009.08.009

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  7 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.  Biological evaluation of isoniazid derivatives as an anticancer class.

Authors:  Felipe A R Rodrigues; Augusto C A Oliveira; Bruno C Cavalcanti; Claudia Pessoa; Alessandra C Pinheiro; Marcus V N de Souza
Journal:  Sci Pharm       Date:  2013-09-22

3.  A Target-Based Whole Cell Screen Approach To Identify Potential Inhibitors of Mycobacterium tuberculosis Signal Peptidase.

Authors:  Shilah A Bonnett; Juliane Ollinger; Susantha Chandrasekera; Stephanie Florio; Theresa O'Malley; Megan Files; Jo-Ann Jee; James Ahn; Allen Casey; Yulia Ovechkina; David Roberts; Aaron Korkegian; Tanya Parish
Journal:  ACS Infect Dis       Date:  2016-09-19       Impact factor: 5.084

4.  Anti-Mycobacterial Evaluation of 7-Chloro-4-Aminoquinolines and Hologram Quantitative Structure-Activity Relationship (HQSAR) Modeling of Amino-Imino Tautomers.

Authors:  Marcelle L F Bispo; Camilo H S Lima; Laura N F Cardoso; André L P Candéa; Flávio A F M Bezerra; Maria C S Lourenço; Maria G M O Henriques; Ricardo B Alencastro; Carlos R Kaiser; Marcus V N Souza; Magaly G Albuquerque
Journal:  Pharmaceuticals (Basel)       Date:  2017-06-09

5.  Facile Synthesis of 5-Aryl-N-(pyrazin-2-yl)thiophene-2-carboxamides via Suzuki Cross-Coupling Reactions, Their Electronic and Nonlinear Optical Properties through DFT Calculations.

Authors:  Gulraiz Ahmad; Nasir Rasool; Adeel Mubarik; Ameer Fawad Zahoor; Muhammad Ali Hashmi; Muhammad Zubair; Muhammad Bilal; Mohamed Hussien; Muhammad Saeed Akhtar; Sajjad Haider
Journal:  Molecules       Date:  2021-12-02       Impact factor: 4.411

6.  Seeking potent anti-tubercular agents: design and synthesis of substituted-N-(6-(4-(pyrazine-2-carbonyl)piperazine/homopiperazine-1-yl)pyridin-3-yl)benzamide derivatives as anti-tubercular agents.

Authors:  Singireddi Srinivasarao; Adinarayana Nandikolla; Amaroju Suresh; Kevin Van Calster; Linda De Voogt; Davie Cappoen; Balaram Ghosh; Himanshu Aggarwal; Sankaranarayanan Murugesan; Kondapalli Venkata Gowri Chandra Sekhar
Journal:  RSC Adv       Date:  2020-03-25       Impact factor: 3.361

7.  A class of hydrazones are active against non-replicating Mycobacterium tuberculosis.

Authors:  Shilah A Bonnett; Devon Dennison; Megan Files; Anumita Bajpai; Tanya Parish
Journal:  PLoS One       Date:  2018-10-17       Impact factor: 3.240

  7 in total

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