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In silico ADMET prediction, evaluation of cytotoxicity in mouse splenocytes and preliminary evaluation of in vitro antimalarial activity of 4-(4-chlorophenyl) thiazole compounds
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Orientador(es)
Resumo(s)
In this work, an in silico study and evaluation of the cytotoxicity of 4-(4-chlorophenyl)thiazole compounds against mouse splenocytes and the chloroquinesensitive Plasmodium falciparum 3D7 strain are reported. The in silico results showed that the compounds have important pharmacokinetic properties for compounds with potential drug candidates. Regarding cytotoxicity assays against splenocytes, the compounds have low cytotoxicity. In addition, they were able to promote activation of these cells by increasing nitric oxide production without promoting cell death. Finally, they were able to promote cell proliferation. Regarding the in vitro anti-P. falciparum activity assays, it was observed that the compounds were able to inhibit the parasite’s growth, presenting IC50 values ranging from 0.79 to greater than 10 µM. These results are promising when compared to chloroquine. Therefore, this study showed that 4-(4-chlorophenyl)thiazole compounds are promising candidates for antimalarials.
Descrição
Funding Information: This study was funded by the Brazilian agencies Fundação de Amparo à Pesquisa do Estado de Pernambuco-FACEPE (Process APQ-0498-4.03/19) and researcher fixation grant-FACEPE (Process BFP-0038-04.03/21). Thanks to MR4, who provided us with the P. falciparum MRA-1029 strain provided by Andrew Talman, Robert Sinden that we used in the trials. The work was partially supported by the FCT project reference CIRCNA/BRB/0281/2019_AMAZING and GHTM-UID/Multi/04413/2013. Funding Information: This study was funded by the Brazilian agencies Fundação de Amparo à Pesquisa do Estado de Pernambuco - FACEPE (Process APQ-0498-4.03/19) and researcher fixation grant -FACEPE (Process BFP -0038-04.03/21). Thanks to MR4, who provided us with the P. falciparum MRA-1029 strain provided by Andrew Talman, Robert Sinden that we used in the trials. The work was partially supported by the FCT project reference CIRCNA/BRB/0281/2019_AMAZING and GHTM-UID/Multi/04413/2013. Publisher Copyright: © 2023, Academia Brasileira de Ciencias. All rights reserved.
Palavras-chave
ADMET antimalarial activity mammalian cell cytotoxicity thiazoles RM Therapeutics. Pharmacology QR Microbiology Infectious Diseases Parasitology Drug Discovery Pharmacology, Toxicology and Pharmaceutics(all) SDG 3 - Good Health and Well-being SDG 9 - Industry, Innovation, and Infrastructure