Synthesis of New Dehydrodieugenol Derivatives via Olefin Cross Metathesis and In Vitro Evaluation of Their Trypanocidal Activity
In: EISSN: 2073-4344 ; Catalysts ; https://hal.science/hal-04193306 ; Catalysts, 2023, 13 (7), pp.1097. ⟨10.3390/catal13071097⟩, 2023
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Zugriff:
International audience ; Ruthenium-catalyzed cross metathesis using biseugenol (1) with electron-deficient olefins methyl (2a) and ethyl (2b) acrylates, acrylic acid (2c), acrylonitrile (2d), and methyl methacrylate (2e) derivatives have been conducted to afford respective derivatives 3a-3e with good yields and excellent conversion rates. Activity of prepared compounds against trypomastigote and amastigote forms of Trypanosoma cruzi and mammalian cytotoxicity have been evaluated. The results obtained indicate that the IC50 values for amastigotes of compounds 3b and 3d are quite similar to those of biseugenol (1), but unlike this compound, they show reduced toxicities with SI values similar to those of the standard drug benznidazol.
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Synthesis of New Dehydrodieugenol Derivatives via Olefin Cross Metathesis and In Vitro Evaluation of Their Trypanocidal Activity
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| Autor/in / Beteiligte Person: | Galhardo, Thalita S. ; Ueno, Anderson K. ; Carvalho, Wagner A. ; Costa-Silva, Thaís A ; Goncalves, Marina M. ; Abiuzi, Mariana B. ; Tempone, Andre G. ; Lago, João Henrique G ; Mandelli, Dalmo ; Fischmeister, Cedric ; Bruneau, Christian ; Universidade Federal do ABC = Federal University of ABC = Université Fédérale de l'ABC Brazil (UFABC) ; Federal University of Sao Paulo (Unifesp) ; Instituto Adolfo Lutz São Paulo, Brazil ; Institut des Sciences Chimiques de Rennes (ISCR) ; Université de Rennes (UR)-Institut National des Sciences Appliquées - Rennes (INSA Rennes) ; Institut National des Sciences Appliquées (INSA)-Institut National des Sciences Appliquées (INSA)-Ecole Nationale Supérieure de Chimie de Rennes (ENSCR)-Institut de Chimie - CNRS Chimie (INC-CNRS)-Centre National de la Recherche Scientifique (CNRS) ; CAPES-COFECUB PHC 884-17, 883/2017 ; Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior-Brasil (CAPES) 001 ; Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq) ; Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP) 2021/02789-7, 2021/04464-8, 2018/07885-1, 2017/50333-7, 2018/10279-6 ; CNPq 312288/2019-0, 422290/2016-5, 404843/2018-2 ; FAPESP 2018/01258-5, 2021/12342-0 ; Sustainable Technologies Unit of UFABC (NuTS) ; 88887.198050/2018-00 |
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| Zeitschrift: | EISSN: 2073-4344 ; Catalysts ; https://hal.science/hal-04193306 ; Catalysts, 2023, 13 (7), pp.1097. ⟨10.3390/catal13071097⟩, 2023 |
| Veröffentlichung: | HAL CCSD, 2023 |
| Medientyp: | academicJournal |
| DOI: | 10.3390/catal13071097 |
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