Asset Details
Do you wish to reserve the book?
Antiplasmodial, Trypanocidal, and Genotoxicity IIn Vitro/I Assessment of New Hybrid α,α-Difluorophenylacetamide-statin Derivatives
Hey, we have placed the reservation for you!
By the way, why not check out events that you can attend while you pick your title.
Oops! Something went wrong.
Looks like we were not able to place the reservation. Kindly try again later.
Are you sure you want to remove the book from the shelf?
Antiplasmodial, Trypanocidal, and Genotoxicity IIn Vitro/I Assessment of New Hybrid α,α-Difluorophenylacetamide-statin Derivatives
Do you wish to request the book?
Antiplasmodial, Trypanocidal, and Genotoxicity IIn Vitro/I Assessment of New Hybrid α,α-Difluorophenylacetamide-statin Derivatives
Please be aware that the book you have requested cannot be checked out. If you would like to checkout this book, you can reserve another copy
We have requested the book for you!
Your request is successful and it will be processed during the Library working hours. Please check the status of your request in My Requests.
Oops! Something went wrong.
Looks like we were not able to place your request. Kindly try again later.
Journal Article
Antiplasmodial, Trypanocidal, and Genotoxicity IIn Vitro/I Assessment of New Hybrid α,α-Difluorophenylacetamide-statin Derivatives
2023
Overview
Background: Statins present a plethora of pleiotropic effects including anti-inflammatory and antimicrobial responses. A,α-difluorophenylacetamides, analogs of diclofenac, are potent pre-clinical anti-inflammatory non-steroidal drugs. Molecular hybridization based on the combination of pharmacophoric moieties has emerged as a strategy for the development of new candidates aiming to obtain multitarget ligands. Methods: Considering the anti-inflammatory activity of phenylacetamides and the potential microbicidal action of statins against obligate intracellular parasites, the objective of this work was to synthesize eight new hybrid compounds of α,α-difluorophenylacetamides with the moiety of statins and assess their phenotypic activity against in vitro models of Plasmodium falciparum and Trypanosoma cruzi infection besides exploring their genotoxicity safety profile. Results: None of the sodium salt compounds presented antiparasitic activity and two acetated compounds displayed mild anti-P. falciparum effect. Against T. cruzi, the acetate halogenated hybrids showed moderate effect against both parasite forms relevant for human infection. Despite the considerable trypanosomicidal activity, the brominated compound revealed a genotoxic profile impairing future in vivo testing. Conclusions: However, the chlorinated derivative was the most promising compound with chemical and biological profitable characteristics, without presenting genotoxicity in vitro, being eligible for further in vivo experiments.
Publisher
MDPI AG
Subject
