Lowering of 5-nitroimidazole's mutagenicity: Towards optimal antiparasitic pharmacophore

Hydrogenosome Metabolism Is the Key Target for Antiparasitic Activity of Resveratrol against Trichomonas vaginalis

“…Some studies have analyzed the in vitro antitrichomonal activity of some natural extracts from medicinal plants, which displayed good antitrichomonal activity, with IC 50 s ranging between 5.6 and 8.0 g/ml (39)(40)(41)(42)(43). These values are similar to those obtained for RESV in this study but much higher than those obtained for MDZ, the antiprotozoal drug used as a positive control, which in the present study yielded a slightly higher value than in other studies (44).…”

Synthesis of Novel Highly Functionalized 4-Thiazolidinone Derivatives from 4-Phenyl-3-thiosemicarbazones

“…It is reported that thiazolidinones exhibit antibacterial [9], antifungal [10], anticonvulsant [11], antitubercular [12], anti-inflammatory [13], antihistaminic [14,15], cardiovascular [16] and anti-HIV [17] activities. As part of our research program on new bioactive compounds [18][19][20][21][22], we report herein an efficient synthesis of some new highly functionalized thiazolidinones derived from 4-phenyl-3-thiosemicarbazones.…”

Synthetic Nitroimidazoles: Biological Activities and Mutagenicity Relationships

“…They have shown that the replacement of the methyl group at the 2-position by a lactam group could double the mutagenicity of metronidazole [50]. In this study, the methyl group at the 2-position combined with the arylsulfonylmethyl group at the 4-position lowered the MP TA100 of dimetridazole, metronidazole and secnidazole series [47]. A good correlation was demonstrated between the antiprotozoal activity and the mutagenicity for these molecules which reflects their ability to damage DNA through covalent binding and induction of DNA breaks [51].…”

“…The antiparasitic activity of nitroimidazoles 10 bearing an arylsulfonylmethyl group was assessed against T. vaginalis, and the in vitro cytotoxicity was evaluated on human monocytes and the mutagenicity was determined by the Salmonella mutagenicity assay (Figure 1) [47]. Molecules, bearing an additional methyl group on the 2-position, showed a lower mutagenicity than metronidazole.…”