“…Kumar et al (2011b) synthesized and evaluated antimicrobial assays, as well as performed QSAR studies of twenty 3-ethoxy-4-hydroxybenzylidene/4-nitrobenzylidene hydrazides. Seven of the new compounds ( 14 – 20 ) showed the antibacterial activity higher than that of ciprofloxacin against S. aureus , B. subtilis , and E. coli (Fig.…”
Section: Introductionmentioning
confidence: 99%
“…Seven of the new compounds ( 14 – 20 ) showed the antibacterial activity higher than that of ciprofloxacin against S. aureus , B. subtilis , and E. coli (Fig. 7) (Kumar et al 2011b). Fig.…”
Hydrazide–hydrazone derivatives are present in many bioactive molecules and display a wide variety of biological activities, such as antibacterial, antitubercular, antifungal, anticancer, anti-inflammatory, anticonvulsant, antiviral, and antiprotozoal action. Therefore, many medicinal chemists synthesize various hydrazide–hydrazones and evaluate them for biological activities. Among biological properties of this class of compounds, antimicrobial activity is the most frequently encountered in scientific literature. This paper is focused on the overview of the literature findings of the last six years (2010–2016) covering the research on antimicrobial activity of hydrazide–hydrazone derivatives. This review may also serve as a useful guide for the development of new hydrazide–hydrazones as potential antimicrobial agents.
“…Kumar et al (2011b) synthesized and evaluated antimicrobial assays, as well as performed QSAR studies of twenty 3-ethoxy-4-hydroxybenzylidene/4-nitrobenzylidene hydrazides. Seven of the new compounds ( 14 – 20 ) showed the antibacterial activity higher than that of ciprofloxacin against S. aureus , B. subtilis , and E. coli (Fig.…”
Section: Introductionmentioning
confidence: 99%
“…Seven of the new compounds ( 14 – 20 ) showed the antibacterial activity higher than that of ciprofloxacin against S. aureus , B. subtilis , and E. coli (Fig. 7) (Kumar et al 2011b). Fig.…”
Hydrazide–hydrazone derivatives are present in many bioactive molecules and display a wide variety of biological activities, such as antibacterial, antitubercular, antifungal, anticancer, anti-inflammatory, anticonvulsant, antiviral, and antiprotozoal action. Therefore, many medicinal chemists synthesize various hydrazide–hydrazones and evaluate them for biological activities. Among biological properties of this class of compounds, antimicrobial activity is the most frequently encountered in scientific literature. This paper is focused on the overview of the literature findings of the last six years (2010–2016) covering the research on antimicrobial activity of hydrazide–hydrazone derivatives. This review may also serve as a useful guide for the development of new hydrazide–hydrazones as potential antimicrobial agents.
“…It is worth to add that beside antibacterial activity (Küçükgüzel et al, 2002, Küçükgüzel et al, 2003, Özkay et al, 2010, Deep et al, 2010, Rasras et al, 2010, Kumar et al, 2011, Rutkauskas et al, 2013, Pieczonka et al, 2013, Cukurovali and Yilmaz, 2014, Satyanarayana et al, 2014, Morjan et al, 2014, Rambabu et al, 2015), hydrazide-hydrazone derivatives have attracted much attention thanks to their usability as intermediates in organic synthesis (Rollas and Kűçűkgűzel, 2007, Bala et al, 2013) and they display a wide spectrum of such interesting biological properties as antifungal (Loncle et al, 2004, Backes et al, 2014), antitubercular (Koçyiğit-Kaymakçıoğlu et al, 2006, Koçyiğit-Kaymakçıoğlu et al, 2009, Pavan et al, 2010, Velezheva et al, 2016), antiviral (Şenkardes et al, 2016), anticancer (Kumar et al, 2012, Çıkla et al, 2013, Wardakhan et al, 2013, Nasr et al, 2014, Küçükgüzel et al, 2015, He et al, 2016, Mukherjee et al, 2016), anti-inflammatory (Moldovan et al, 2011) and analgesic activity (Mohareb et al, 2010).…”
In this research we synthesized and tested for antimicrobial activity 21 nitrofurazone analogues. The compounds we obtained were identified on the basis ofH NMR and C NMR spectroscopy. The screening of antimicrobial properties of synthesized compounds revealed a wide spectrum of antimicrobial activity. Compounds ,, -, and - showed very high bactericidal effect towards spp. ATTC and spp. ATTC (MIC = 0.002-7.81 µg/ml and MBC = 0.002-31.25 µg/ml). The levels of activity of several compounds were far better than those of nitrofurantoin, ciprofloxacin or cefuroxime.
“…Ligand-based molecular design and QSAR approaches are promising fields with several applications in drug development, which use a battery of novel molecular descriptors and different classification algorithms for in silico virtual drug screening studies [5,6]. In the present research, we use and compare a set of different machine learning (ML) techniques using the 2D atom-based quadratic indices as attributes with the objective to perform the QSAR modeling of two datasets.…”
The atom-based quadratic indices are used in this work together with some machine learning techniques that includes: support vector machine, artificial neural network, random forest and k-nearest neighbor. This methodology is used for the development of two quantitative structure-activity relationship (QSAR) studies for the prediction of proteasome inhibition. A first set consisting of active and non-active classes was predicted with model performances above 85% and 80% in training and validation series, respectively. These results provided new approaches on proteasome inhibitor identification encouraged by virtual screenings procedures. .
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