148904-02-3Relevant articles and documents
Exploiting Miraculous Atmospheric CO2 Fixation in the Design of Dysprosium Single-Molecule Magnets
Tian, Haiquan,Zhao, Lang,Tang, Jinkui
, p. 1173 - 1181 (2018)
A system of CO32--bridged polynuclear dysprosium complexes has been complemented with the emergence of a key component, namely, [Dy6(μ4-CO3)3(μ3-OH2)(spch)6
N-acylhydrazones confer inhibitory efficacy against New Delhi metallo-β-lactamase-1
Gao, Han,Li, Jia-Qi,Kang, Peng-Wei,Chigan, Jia-Zhu,Wang, Huan,Liu, Lu,Xu, Yin-Sui,Zhai, Le,Yang, Ke-Wu
, (2021/07/07)
The expression of β-lactamases, especially metallo-β-lactamases (MβLs) in bacteria is one of the main causes of drug resistance. In this work, an effective N-acylhydrazone scaffold as MβL inhibitor was constructed and characterized. The biological activity assays indicated that the synthesized N-acylhydrazones 1–11 preferentially inhibited MβL NDM-1, and 1 was found to be the most effective inhibitor with an IC50 of 1.2 μM. Analysis of IC50 data revealed a structure–activity relationship, which is that the pyridine and hydroxylbenzene substituents at 2-position improved inhibition of the compounds on NDM-1. ITC and enzyme kinetics assays suggested that it reversibly and competitively inhibited NDM-1 (Ki = 0.29 ± 0.05 μM). The synthesized N-acylhydrazones showed synergistic antibacterial activities with meropenem, reduced 4–16-fold MIC of meropenem on NDM-1- producing E. coli BL21 (DE3), while 1 restored 4-fold activity of meropenem on K. pneumonia expressing NDM-1 (NDM-K. pneumoniae). The mice experiments suggested that 1 combined meropenem to fight against NDM-K. pneumoniae infection in the spleen and liver. Cytotoxicity assays showed that 1 and 2 have low cytotoxicity. This study offered a new framework for the development of NDM-1 inhibitors.
Synthesis and pharmacological evaluation of pyrazine N-acylhydrazone derivatives designed as novel analgesic and anti-inflammatory drug candidates
Silva, Yolanda Karla Cupertino Da,Augusto, Cristina Villarinho,Barbosa, Maria Leticia De Castro,Melo, Gabriela Muniz De Albuquerque,Queiroz, Aline Cavalcanti De,Dias, Thays De Lima Matos Freire,Junior, Walfrido Bispo,Barreiro, Eliezer J.,Lima, Lidia Moreira,Alexandre-Moreira, Magna Suzana
experimental part, p. 5007 - 5015 (2010/09/05)
In this paper, we report the synthesis and pharmacological evaluation of pyrazine N-acylhydrazone (NAH) derivatives (2a-s) designed as novel analgesic and anti-inflammatory drug candidates. This series was planned by molecular simplification of prototype
Synthesis and antimycobacterial activity of N′-[(E)-(monosubstituted-benzylidene)]-2-pyrazinecarbohydrazide derivatives
Vergara, Fatima M.F.,Lima, Camilo H. da S.,Henriques, Maria das Gracas M. de O.,Candea, Andre L.P.,Lourenco, Maria C.S.,Ferreira, Marcelle de L.,Kaiser, Carlos R.,de Souza, Marcus V.N.
experimental part, p. 4954 - 4959 (2010/02/27)
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 μg/mL. The compounds 6, 23, 27 and 28 exhibited a significant activity (50-100 μg/mL) when compared with first line drugs such as pyrazinamide and were not cytotoxic in their respective MIC values.
