88368-69-8Relevant academic research and scientific papers
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, antiviral activity, and molecular docking study of trans-ferulic acid derivatives containing acylhydrazone moiety
Wang, Zhenzhen,Xie, Dandan,Gan, Xiuhai,Zeng, Song,Zhang, Awei,Yin, Limin,Song, Baoan,Jin, Linhong,Hu, Deyu
, p. 4096 - 4100 (2017/08/23)
In this study, we report the synthesis and antiviral activity of trans-ferulic acid derivatives containing acylhydrazone moiety. Biological tests demonstrated that most target compounds showed potent antiviral activity against tobacco mosaic virus (TMV). Compound D4 showed remarkable inactivating activity with EC50 value of 36.59 μg/mL, which was obviously superior to ribavirin (126.05 μg/mL). Molecular docking results revealed that compound D4 exhibited the optimal combining capacity with five hydrogen bonds to different amino-acid residues of TMV coat protein (TMV-CP). Docking results were consistent with the inactivating activity of target compounds against TMV.
Synthesis of piplartine analogs and preliminary findings on structure–antimicrobial activity relationship
Fregnan, Antonio Maciel,Brancaglion, Guilherme Andrade,Galv?o, Alexandre Francisco Cerqueira,D’Sousa Costa, Cinara Oliveira,Moreira, Diogo Rodrigo Magalh?es,Soares, Milena Botelho Pereira,Bezerra, Daniel Pereira,Silva, Naiara Chaves,de Souza Morais, Stella Maria,Oliver, Josidel Concei??o,Dias, Amanda Latercia Tranches,Coelho, Luiz Felipe Leomil,Carvalho, Diogo Teixeira,Dias, Danielle Ferreira,de Souza, Thiago Belarmino
, p. 603 - 614 (2017/02/15)
In this work it is described the synthesis, characterization and antimicrobial and toxicity evaluation of a series of analogs of piplartine, a piperamide found in Piper sp. The compounds structures were confirmed by infrared spectroscopy, 1H, 13C nuclear magnetic resonance, high resolution mass spectroscopy and were evaluated against strains of Candida spp., Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. Derivative 24 was almost four-fold more potent (IC50: 48.83 μM) and five-fold less toxic (SI > 3) than piplartine (IC50: 189.2 μM; SI: 0.21) against Candida krusei, as well as two-fold more potent than fluconazole (IC50: 104.48 μM). This compound was also active against Candida tropicalis at 97.67 μM. Benzoyl derivative 17 was three-fold more potent (IC50: 85.2 μM) and more than five-fold less toxic (CC50: 231.71 μM) than piplartine (IC50: 315.33 μM and CC50: 41.14 μM) against Staphylococcus aureus. Given these findings, we have found analogs of piplartine which can be assumed as prototypes for the optimization and the development of new antimicrobial (compounds 24 and 17) agents.
NEW GUANIDINE DERIVATIVES IN CINNAMIC SERIES
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Paragraph 0119-0125; 0164; 0165; 0166; 0167; 0168, (2013/07/05)
The invention relates to novel guanidine derivatives in the cinnamic series of general formula (I): The invention also relates to the process for preparing said guanidine derivatives and also to synthetic intermediates. Finally, the invention relates to t
Design and synthesis of new (E)-cinnamic N-acylhydrazones as potent antitrypanosomal agents
Carvalho, Samir A.,Feitosa, Larisse O.,Soares, Marcio,Costa, Thadeu E.M.M.,Henriques, Maria G.,Salomao, Kelly,De Castro, Solange L.,Kaiser, Marcel,Brun, Reto,Wardell, James L.,Wardell, Solange M.S.V.,Trossini, Gustavo H.G.,Andricopulo, Adriano D.,Da Silva, Edson F.,Fraga, Carlos A.M.
experimental part, p. 512 - 521 (2012/09/07)
We report herein the synthesis and trypanocidal profile of new (E)-cinnamic N-acylhydrazones (NAHs) designed by exploiting molecular hybridization between the potent cruzain inhibitors (E)-1-(benzo[d][1,3]dioxol-5-yl)-3-(4-bromophenyl) prop-2-en-1-one and (E)-3-hydroxy-N'-((2-hydroxynaphthalen-1-yl)methylene)-7- methoxy-2-naphthohydrazide. These derivatives were evaluated against both amastigote and trypomastigote forms of Trypanosoma cruzi and lead us to identify two compounds that were approximately two times more active than the reference drug, benznidazole, and with good cytotoxic index. Although designed as cruzain inhibitors, the weak potency displayed by the best cinnamyl NAH derivatives indicated that another mechanism of action was likely responsible for their trypanocide action.
