This study explored a series of resorcinol derivatives originally identified as heat shock protein 90 inhibitors for activity against protozoan parasites. The repurposing of this series revealed that some of these compounds are active against chloroquine-sensitive Plasmodium falciparum (3D7) and Trypanosoma brucei brucei strains with IC50 values below 10 μM without obvious cytotoxic effects against human cervix adenocarcinoma (HeLa) cells at 25 μM.

Herein a series of novel thiosemicarbazones (TSCs) derived from 2-oxoquinoline scaffold is reported, and the target compounds have been successfully synthesized and characterized using standard spectroscopic techniques. The in vitro biological activities of synthesized molecules were evaluated against Plasmodium falciparum malaria parasites (strain 3D7), Trypanosoma brucei brucei parasites (strain 427) and HeLa cells. All the compounds displayed modest or no activity at a concentration of 20 μΜ and percentage viability of >50 % was often observed. Except for compound 9o, none of the final compounds exhibited cytotoxic effects against HeLa cells at 20 μΜ.

Sleeping sickness (trypanosomiasis) is a neglected tropical disease that affects mostly the poorest communities in sub-Saharan Africa. Toxic side effects associated with the use of current anti-trypanosomal drugs, which in some cases kill faster than the disease itself, necessitate the search for new drugs with better safety margins. To this effect, a small library bearing different substituents at position -1, -3, and -6 of the quinolone nucleus were synthesized and evaluated in vitro against HeLa cell lines and Trypanosoma brucei brucei for cytotoxicity and trypanocidal potentials, respectively. While most of these compounds showed no cytotoxic effect, they exhibited moderate to weak anti-trypanosomal activities. The SAR studies of this series provide new information worth considering in future exploration of the quinolone scaffold in search of more potent and safe trypanocidal agents.

Água residual proveniente de uma indústria de tabuleiro de fibra dura caracterizada por ter um elevado conteúdo orgânico (15-30 g/L DQO) foi estudada utilizando um sistema arejado seqüêncial de forma a definir uma estratégia de start up. A concentração de DQO na entrada do sistema variou na faixa de 0,5-25 g/L e o tempo de residência hidráulico foi mantido em 5 dias. O sistema seqüêncial proposto reduziu DBO, DQO, SST e fenol sobre 90% quando a concentração de DQO na entrada foi menor a 25 g/L.

Wastewater from a hardboard mill characterized by a high organic content (15-30 g/L COD) was studied in a bench scale sequential aerated system in order to define a start up strategy. Inlet COD concentration varied from 0.5 to 25 g/L and the hydraulic retention time was maintained at 5 days. The sequential system proposed could reduce BOD, COD, TSS and phenol over 90% except when the inlet COD concentration was lower than 25 g/L.