Design, synthesis, and in vitro antiprotozoal, antimycobacterial activities of N-{2-[(7-chloroquinolin-4-yl)amino]ethyl}ureas

Synthesis of nitro(benzo)thiazole acetamides and in vitro antiprotozoal effect against amitochondriate parasites Giardia intestinalis and Trichomonas vaginalis

“…In vitro susceptibility assays were performed using methods previously described. 5,17,19 All the screened compounds showed strong giardicidal bioactivity. It is interesting to note that 5-nitrothiazole series (compounds 1-4) were more potent than 6-nitrobenzothiazole analogues (compounds 5-8), being all more active than the drugs of choice.…”

“…In vitro susceptibility assays were performed as previously described. 5,17,19 Briefly: 4 Â 10 4 trophozoites of G. lamblia or T. vaginalis were incubated for 48 h at 37°C with increasing concentrations of synthesized compounds, Nitazoxanide, Metronidazole and starting reagents (0.001, 0.01, 0.1, 1, and 10 lM). As the negative control, trophozoites were incubated in culture medium with DMSO used in the experiments.…”

Anti- Plasmodium falciparum activity of quinoline–sulfonamide hybrids

“…The compounds N 1 -(7-chloroquinolin-4-yl)alkyldiamine (17-19) were synthesized with 85-90% yield by the nucleophilic substitution reaction between of 4,7-dichloroquinoline (16) (1.0 mmol) with the corresponding diamines (1.0 mmol) 19 . The addition-elimination reaction between the appropriate sulfonyl chloride (1.2 mmol) and the N 1 -(7-chloroquinolin-4-yl)alkyldiamines (17-19) (1.0 mmol) was performed in MeOH and TEA (1.0 mmol) at 25 °C, to obtain N-(2-((7-chloroquinolin-4-yl)amino)alkyl)benzenesulfonamides (1-15) with 50-77% yield 20 .…”

Chloroquine treatment against naturally occuring Giardia duodenalis infection in dogs

“…Furthermore, chloroquine was shown to be more effective than metronidazole on G. duodenalis trophozoites (26). Although the mechanism of action of chloroquine is not entirely understood, as the latter compound's efficacy was attributed to a reduced ability of Giardia trophozoite in vitro for attaching to surfaces.…”