3538-69-0Relevant academic research and scientific papers
Synthesis and application of photo-active carboxymethyl cellulose derivatives
Monier,Abdel-Latif,Ji
, p. 137 - 146 (2016)
In this work, the polysaccharide carboxymethyl cellulose (CMC) was first activated via periodate oxidation then modified by insertion of photo-active cinnamic acid hydrazide moieties to finally produce the photo-crosslinkable CMC-CM with various extents of functionalizations. The chemical structures of the manufactured polymeric materials were entirely investigated utilizing FTIR, 1H, 13C NMR, and UV-vis spectra. Upon irradiation in UV light, the progress and kinetics of the cross-linking were detected using UV-vis spectra. Moreover, the crystallinity changes before and after chemical modification and subsequent UV irradiation were examined by XRD spectra. Also, the obtained hydrogels with various cross-linking densities were freeze dried to visualize the morphological changes using SEM. In addition, the rheological experiments indicated the improvement of the hydrogel mechanical properties by increasing both UV irradiation time and degree of cinnamate functionalization. The obtained hydrogel exhibited good swelling, gelation and biodegradation properties, which indicate a promising potential in different biomedical applications.
Ion-exchange resin catalysts in the liquid-phase hydrazinolysis of cinnamic acid
Dzhumadullaeva,Baeshov
, p. 24 - 27 (2017)
The catalytic activity of a synthetic ion-exchange resins has been studied in the reaction of cinnamic acid with hydrazine (aqueous medium, 363 K, 1.0–2.5 h) yielding the corresponding hydrazide. Efficient catalysts for the process are the anion-exchange resins AV-17-8 and AN-31. The modifying effect of the substrate—hydrazine hydrate—on the catalytic properties of the ion-exchange systems has been demonstrated. On the basis of IR spectroscopic studies, a plausible process mechanism was suggested. It involves polymer-bound quaternary ammonium ions of the anion exchanger.
Synthesis, characterization and study of mesomorphic behavior of new bent and linear core compounds containing heterocyclic rings
Al-Dujaili, Ammar H.,Karam, Nisreen H.,Shanshal, Alaa K.
, (2021/08/20)
The article presents the synthesis and liquid crystalline properties of some of new bent and linear core compounds containing a 1,3,4-oxadiazole, piperazine and thiazolidin-4-one rings as a central core. The new synthesized compounds were characterized by elemental analysis and FTIR, 1HNMR and mass spectroscopy). The liquid crystalline properties were studied by polarized optical microscopy and differential scanning calorimetry. All Schiff bases compounds with 1,3,4-oxadiazole and piprzaine ring in central core presented liquid crystalline properties. The liquid crystallinity of compounds containing 1,3,4-oxadiazole and thiazolidin-4-one rings as a central core were found depending on the type of terminal substituents.
ANTIMICROBIAL AGENTS AND COMPOSITIONS AND USES THEREOF
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Paragraph 0256-0257, (2021/04/01)
Described herein are compounds that act as antimicrobial agents, compositions comprising these compounds, and methods of their use in to treating infections caused by Helicobacter pylori (H. pylori) or killing or inhibititing the growth of H. pylori.
Novel fluorozoone-like fluorinion probe based on flavonoids
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Paragraph 0026; 0027, (2020/02/06)
The invention discloses a preparation method of a novel fluorozoone-like visible fluorinion probe which is prepared from flavonoids of a formula I shown in the description and a 3-phenylacrylic acid type derivative. The preparation method comprises the fo
Identification of novel functionalized carbohydrazonamides designed as chagas disease drug candidates
Do Nascimento, Mayara S. S.,Camara, Vitória R. F.,da Costa, Juliana S.,Barbosa, Juliana M. C.,Lins, Alessandra S. M.,Salom?o, Kelly,de Castro, Solange L.,Carvalho, Samir A.,da Silva, Edson F.,Fraga, Carlos A. M.
, p. 774 - 783 (2020/08/19)
Background: Although several research efforts have been made worldwide to discover novel drug candidates for the treatment of Chagas disease, the nitroimidazole drug benznidazol remains the only therapeutic alternative in the control of this disease. However, this drug presents reduced efficacy in the chronic form of the disease and limited safety after long periods of admini-stration, making it necessary to search for new, more potent and safe prototypes. Objective: We described herein the synthesis and the trypanocidalaction of new functionalized carbohydrazonamides (2-10) against trypomastigote forms of Trypanosoma cruzi. Methods: These compounds were designed through the application of molecular hybridization concept between two potent anti-T. cruzi prototypes, the nitroimidazole derivative megazol (1) and the cinnamyl N-acylhydrazone derivative (14) which have been shown to be twice as potent in vitro as benznidazole. Results: The most active compounds were the (Z)-N'-((E)-3-(4-nitrophenyl)-acryloyl)-1-methyl-5-nitro-1H-imidazol-2-carbohydrazonamide (6) (IC50 =9.50 μM) and the (Z)-N'-((E)-3-(4-hydroxyphe-nyl)-acryloyl)-1-methyl-5-nitro-1H-imidazol-2-carbohydrazonamide (8) (IC50 =12.85 μM), which were almost equipotent to benznidazole (IC50 =10.26 μM) used as standard drug. The removal of the amine group attached to the imine subunit in the corresponding N-acylhydrazone derivatives (11-13) resulted in less potent or inactive compounds. The para-hydroxyphenyl derivative (8) presented also a good selectivity index (SI = 32.94) when tested against mammalian cells from Swiss mice. Conclusion: The promising trypanocidal profile of new carbohydrazonamide derivatives (6) and (8) was characterized. These compounds have proved to be a good starting point for the design of more effective trypanocidal drug candidates.
Cinnamoyl-N-Acylhydrazone-Donepezil Hybrids: Synthesis and Evaluation of Novel Multifunctional Ligands Against Neurodegenerative Diseases
Ortiz, Cindy Juliet Cristancho,Damasio, Caio Miranda,Pruccoli, Letizia,Nadur, Nathália Fonseca,de Azevedo, Luciana Luiza,Guedes, Isabella Alvim,Dardenne, Laurent Emmanuel,Kümmerle, Arthur Eugen,Tarozzi, Andrea,Viegas, Claudio
, p. 3003 - 3020 (2020/10/22)
Abstract: A new series of ten multifunctional Cinnamoyl-N-acylhydrazone-donepezil hybrids was synthesized and evaluated as multifunctional ligands against neurodegenerative diseases. The molecular hybridization approach was based on the combination of 1-b
Synthesis and Docking Study of N-(Cinnamoyl)- N′-(substituted)acryloyl Hydrazide Derivatives Containing Pyridinium Moieties as a Novel Class of Filamentous Temperature-Sensitive Protein Z Inhibitors against the Intractable Xanthomonas oryzae pv. oryzae Infections in Rice
Feng, Yu-Mei,Li, Zhong,Liu, Li-Wei,Ma, Hao-Dong,Qi, Pu-Ying,Shao, Wu-Bin,Wang, Pei-Yi,Wang, Yi,Wu, Zhi-Bing,Yang, Song,Zhou, Xiang
, p. 8132 - 8142 (2020/09/02)
Xanthomonas oryzae pv. oryzae (Xoo) is an offensive phytopathogen that can invade a wide range of plant hosts to develop bacterial diseases, including the well-known rice bacterial leaf blight. However, few agrochemicals have been identified to effectively prevent and eliminate Xoo-induced diseases. Thus, designing novel antibacterial compounds on the basis of the potential targets from Xoo may lead to the discovery of highly efficient and innovative anti-Xoo agents. Filamentous temperature-sensitive protein Z (FtsZ), an important functional protein in the progression of cell division, has been widely reported and exploited as a target for creating antibacterial drugs in the field of medicine. Therefore, the fabrication of innovative frameworks targeting XooFtsZ may be an effective method for managing bacterial leaf blight diseases via blocking the binary division and reproduction of Xoo. As such, a series of novel N-(cinnamoyl)-N′-(substituted)acryloyl hydrazide derivatives containing pyridinium moieties were designed, and the anti-Xoo activity was determined. The bioassay results showed that compound A7 had excellent anti-Xoo activity (EC50 = 0.99 mg L-1) in vitro and distinct curative activity (63.2% at 200 mg L-1) in vivo. Further studies revealed that these designed compounds were XooFtsZ inhibitors, validating by the reduced GTPase activity of recombinant XooFtsZ, the nonfilamentous XooFtsZ assembly observed in the TEM images, and the prolonged Xoo cells from the fluorescence patterns. Computational docking studies showed that compound A7 had strong interactions with ASN34, GLN193, and GLN197 residues located in the α helix regions of XooFtsZ. The present study demonstrates the developed FtsZ inhibitors can serve as agents to control Xoo-induced infections.
Synthesis of N′-propylhydrazide analogs of hydroxamic inhibitors of histone deacetylases (HDACs) and evaluation of their impact on activities of HDACs and replication of hepatitis C virus (HCV)
Kozlov, Maxim V.,Konduktorov, Konstantin A.,Shcherbakova, Anastasia S.,Kochetkov, Sergey N.
, p. 2369 - 2374 (2019/06/17)
N′-Propylhydrazide analogs of hydroxamic inhibitors of histone deacetylases (HDACs), including tubastatin A, vorinostat and belinostat, were synthesized. All prepared compounds inhibited HDAC1/2/3, but not HDAC6, except for one hydrazide analog of HDAC4/5/7 inhibitor that was completely inactive. A novel 4-substituted derivative of N′-propylbenzohydrazide with extremely high anti-HCV activity was discovered.
Colorimetric and ratiometric sensors derivated from natural building blocks for fluoride ion detection
Shi, Heng,Zhao, Fengfei,Chen, Xinghan,Yang, Shilong,Xing, Jieni,Chen, Hongjin,Zhang, Rui,Liu, Jian
, (2019/11/03)
Three novel colorimetric and ratiometric probes (SH-1~3) for fluoride ion detection were designed and synthesized from nature small molecules. Obvious yellow-to-orange color change of these probes in the THF was achieved only in presence of F?
