Purpose: To synthesize hybrid benzimidazolyl-chalcone derivatives, evaluate their anthelmintic activity, and establish some structural elements which could lead to induction and enhancement of this activity. Methods: A series of 1-(1H-benzimidazol-2-yl)-3-aryl-2-propen-1-one compounds (6a-z) was synthesized by condensation reaction of 2-acetylbenzimidazole with aryl and heteroaryl aldehyde derivatives. The physicochemical characterization of these benzimidazolyl-chalcones was carried out by nuclear magnetic resonance spectroscopy ( 1 H and 13 C NMR) and mass spectroscopy (MS). All compounds were screened in vitro for their nematicidal activity against Haemonchus contortus in larval development assay. The anthelmintic activities obtained were compared with those of anthelmintic reference drugs (fenbendazole and ivermectin); 1,3-diphenyl-2-propen-1-one also used as reference for chalcone. Results: Compounds 6a, 6g, 6w and 6y showed good nematicidal activity (LC100) at 0.002 and 0.0092 µg/ml. The activity of these four benzimidazolyl-chalcones is nearly equal to that of fenbendazole. It is also interesting to know that these compounds have anti-haemonchus activity which is equal or more efficient than ivermectin. Four other compounds (6d, 6h, 6o and 6t) possess interesting anthelmintic activities at 0.68 and 0.16 µg/ml. Conclusion: Preliminary structure-activity relationship studies revealed that arylpropenone group in position 2 of the benzimidazole ring can be considered as new pharmacophore for nematicidal activity.
Intra articular Coronal fracture of the femoral condyle (Hoffa) is rare-especially that of medial condyle. We report the case of a patient who had a bilateral Hoffa fracture of the medial condyles (type 33 - B3, Orthopaedic Trauma Association) occurred as a result of an accident at work (worker mover). Lesions were treated with the functional and orthopaedic approach. At follow- up of 8-month functional score was excellent with normal flexion, an absence of laxity, an absence of pain and an unlimited market. Through a review of the literature the mechanism, the diagnostic methods and therapeutic will be analysed.
Condensation of substituted aromatic ketones (acetophenone) and substituted aldehydes give unsaturated ketones 14 (chalcones) which react with o-phenylenediamine 7 to afford the corresponding benzodiazepines 15. Treatments of benzodiazepines under basic conditions give benzimidazole derivatives. Structures of all synthesized compounds have been characterized by their NMR and mass spectral data.
The crystal structures of five N-(2,3-dihydroxybenzylidene)amine derivatives, C7H6NO2--R [R = phenyl (1), p-methylphenyl (2), o-chlorophenyl (3), isopropyl (4) and cyclopropyl (5)] are presented and discussed.
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