Cytotoxic, larvicidal, nematicidal, and antifeedant activities of piperidin-connected 2-thioxoimidazolidin-4-one derivatives.
Journal:
Saudi journal of biological sciences
Published Date:
Dec 24, 2017
Abstract
The objective of this study was to investigate brine shrimp cytotoxicity, larvicidal, nematicidal, and antifeedant activities of novel piperidin-connected 2-thioxo-imidazolidin-4-one derivatives. The activities of target compounds were compared with some naturally occurring (-)-pinidinol, hydantocidin, and positive controls. Target compounds were synthesized via cyclocondensation method. The compounds were synthesized and then characterized by infrared spectroscopy, H NMR, C NMR, mass spectral, and elemental analyses. Brine shrimp cytotoxicity assay was investigated using freshly hatched, free-swimming nauplii of . Larvicidal screening was performed against urban mosquito larvae (). Nematicidal activity was evaluated using nematodes of . Regarding antifeedant activity, marine-acclimated fingerlings were used. Compounds (piperidin-connected 2-thioxoimidazolidin-4-one) were found to be lethal to the second instar larvae of mosquito, which produced LD values of 1.37, 6.66, 6.51 μg/mL, compared to compounds (-) pinidinol and hyantocidin LD values of 18.28 and 22.11 μg/mL respectively. Compound was found to kill 100% of fish fingerlings within 6 h at 20 µg/mL, with LD values of 1.54, 1.79, 1.52 µg/mL, compared to compounds (-) pinidinol and hyantocidin with LD values of 10.21 and 21.05 μg/mL respectively. Compound with LD value of 1.57 μg/mL demonstrated high nematicidal activity compared to compound , , (-) Pinidinol and Hyantocidin LD values of 6.45, 2.42, 14.25, 26.30 μg/mL respectively. Therefore, the 2-thioxoimidazolidin-4-one with piperidin ring showed high potential cytotoxic, larvicidal, nematicidal, and antifeedent activities.
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