177714-34-0Relevant articles and documents
Synthesis, Structural Characterization, and Biological Evaluation of Some Hydrazone Compounds as Potential Antioxidant Agents
??nar, Ercan,?akmak, Re?it,Eyup, Basaran,Ha?imi, Nesrin
, p. 143 - 152 (2022/03/17)
Abstract: Antioxidants are sufficiently stable molecules that neutralize free radicals by electron transfer and thereby reduce their damaging capacity. Hydrazones, which are frequently used in the discovery studies of new antioxidant agents, are bioactive compounds with very significant utilization areas because of their various biological and clinical applications. In this study, in vitro antioxidant activities of the previously synthesized hydrazone compounds against various free radicals were examined, one by one. It was determined that among the synthesized compounds (II–VIII), especially the compound (II) had a significant effect (IC50 = 4.4 ± 0.04 μg/mL for DPPH, IC50 = 1.8 ± 0.07 μg/mL for ABTS and A0.5 = 2.2 ± 0.02 μg/mL for CUPRAC) on the prevention of free radical-induced oxidative stress, as better results were obtained than the standard substance. All synthesized compounds showed good antioxidant effects compared to BHA in the CUPRAC method. The obtained results demonstrate that most of the synthesized molecules are promising antioxidant agents.
Aromatic acyl hydrazone derivative and application thereof as NA inhibitor
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Paragraph 0039; 0047-0049; 0258; 0263-0265, (2020/12/30)
The invention relates to an aromatic acyl hydrazone derivative as shown in a structural formula I, pharmaceutically acceptable salt and a pharmaceutical composition thereof, and application of the aromatic acyl hydrazone derivative and the pharmaceutically acceptable salt and the pharmaceutical composition in preparation of an influenza virus neuraminidase inhibitor, wherein R is one of trifluoromethyl, nitryl, 3-methyl-4-nitryl, 3-hydroxyl-4-nitryl, 3-nitryl-4-hydroxyl, hydroxyl, dihydroxyl, dinitryl, 3-methoxy-4-hydroxyl or trihydroxyl; Y is selected from hydroxyl, dihydroxyl, 2-hydroxyl-3-methoxy, 2-hydroxyl-4-methoxy,2-hydroxyl-5-methoxy,2-hydroxyl-6-methoxy,3-hydroxyl-2-methoxy,3-hydroxyl-4-methoxy,3-hydroxyl-5-methoxy,3-hydroxyl-6-methoxy,4-hydroxyl-2-methoxy,4-hydroxyl-3-methoxy,4-hydroxyl-3,5-dimethoxy, trihydroxyl, 4-hydroxyl-3-ethoxy, or 4-hydroxyl-3,5-dimethoxy; w is selected from CH or N; and z is selected from CH or N.
Synthesis and assessment of novel anti-chlamydial benzylidene acylhydrazides derivatives
Bao, Xiaofeng,Xue, Ying,Xia, Chao,Lu, Yin,Yang, Ningjing,Zhao, Yu
, p. 31 - 36 (2018/02/14)
Background: Chlamydiae, characterized by a unique biphasic life cycle, are a group of Gram-negative obligate intracellular bacterial pathogens responsible for diseases in a range of hosts including humans. Benzylidene acylhydrazide CF0001 could inhibit chlamydiae independent of iron starvation and T3SS inhibition. This finding promoted us to design and synthesize more benzylidene acylhydrazides to find novel anti-chlamydial agents. Methods: The carboxylic acids 1a-1d were coupled with Boc-hydrazide inpresence of EDCI and DMAP to obtain the intermediate 2a-2d in 60-62% yields. N-Boc deprotections were performed to obtain hydrazide hydrochloride salt 3a-3d. Nextly, the hydrazides were subjected to condensation with aldehydes to obtain benzylidene acylhydrazides 4a-4g in 30-52% yields in two steps. Results: Compound 4d exhibited best inhibitory effect on the formation and growth of chlamydial inclusions. The IC50 value of compound 4d for infectious progenies was 3.55 M, better than 7.30 M of CF0001. Conclusion: To find novel anti-chlamydial agents, we have designed and synthesized benzylidene acylhydrazides 4a-4g. Compounds 4a, 4d, 4g showed inhibitory activity on C. muridarum with the IC50 values from 3.55-12 M. The 3,5-dibromo-4-hydroxyl substitutes on ring B are critical to keep their anti-chlamydial activity. Compound 4d inhibited C. muridarum in a dose-dependent manner without apparent cytotoxicity.
Antimicrobial evaluation of 4-methylsulfanyl benzylidene/3-hydroxy benzylidene hydrazides and QSAR studies
Kumar, Davinder,Narang, Rakesh,Judge, Vikramjeet,Kumar, Devinder,Narasimhan, Balasubramanian
, p. 382 - 394 (2012/08/27)
A series of 4-methylsulfanyl benzylidene/3-hydroxy benzylidene hydrazides (1-20) was synthesized and tested for in vitro antimicrobial activity against S. aureus, B. subtilis, E. coli, C. albicans and A. niger. The results of antimicrobial studies indicated that 3-phenylacrylic acid-(3-hydroxybenzylidene) -hydrazide, 16, was the most effective as it showed both bactericidal and fungicidal properties and other compounds possessed bacteriostatic/fungistatic activity. The multi-target QSAR model demonstrated that the topological parameter, Balaban topological index (J) is effective in describing the antimicrobial activity of synthesized substituted hydrazides. Springer Science+Business Media, LLC 2010.
