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The extensive pharmacological applications of the pyrazole-based compounds stimulated us to synthesize the highly functionalized, pyrazolylmalonyl diisothiocyanate derivative (2)via treating 2-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)malonyl dichloride (1) with ammonium thiocyanate in acetonitrile at room temperature. The diisothiocyanate derivative 2 was subsequently conducted with a double molar ratio of different nitrogen nucleophiles like 4-acetylaniline, 2-aminobenzoic acid, 6-aminothiouracil, 2-aminothiadiazole derivative, hydrazine, phenylhydrazine, thiophene-2-carbohydrazide, 2-hydroxybenzohydrazide, 2-cyanoacetohydrazide, thiourea, thiosemicarbazide, 2-aminoaniline, and thiocarbohydrazide, aiming to construct some valuable heterocyclic systems. The synthesized compounds were screened for their insecticidal activity against healthy late third instar larvae P. interpunctella and Nilaparvata lugens and the results showed that pyrimidinethione, thiadiazolotriazine, and tetrazinethione derivatives exhibited the highest insecticidal potency that are supported by DFT stimulation and their molecular docking. [ABSTRACT FROM AUTHOR]

A new series of various N-(1-(2-chlorobenzo[h]quinolin-3-yl)-1-substituted-vin-2-yl)benzamide derivatives was designed and synthesized based on the 2-chlorobenzo[h]quinoline core as potential antioxidant and insecticidal agents. In vitro antioxidant activities of these compounds were evaluated and compared with commercial antioxidant (ascorbic acid). The results showed good antioxidant activities of these compounds. In addition, in vitro insecticidal activities revealed that most of these compounds exhibited high insecticidal activity against cotton leafworm compared with chlorpyrifos. Some compounds in these series were better than the commercial insecticidal, chlorpyrifos. [ABSTRACT FROM AUTHOR]

It was well known that hydrazine–hydrazone derivatives have an important role in different synthetic and medicinal fields. Therefore, the hydrazide–hydrazone derivative 3 was treated with electrophilic reagents achieving some quinoline-based heterocyclic systems such as chromene and pyridine derivatives and screened for their rodenticidal activity. The potent compounds were subjected to density functional theory studies. Seven compounds were tested for hemorrhoidal activity. Compounds 5, 6, and 7 were more effective against rodents than the other synthesized compounds, which were controlled by the most potent active second-generation products, such as chlorophacinone, brodifacoum, and warfarin. This could be attributed to their existence in more tautomeric structures. As a result, they could be used as rodenticides. [ABSTRACT FROM AUTHOR]

The broad spectrum of biological activity of pyrazole derivatives coupled with our interest in the chemistry of nitrogen heterocycles led us to synthesize a bis-benzoxazinone derivative bearing a pyrazole scaffold and utilize it as a key material for the construction of some bisimidazole, bistriazole, and bisbenzimidazole derivatives obtained by reactions with some mono- and bidentate nitrogen nucleophiles. The density functional theory studies of the synthesized compounds were calculated. The synthesized compounds were screened for their in vitro antitumor activity against two human tumor cell lines; HepG2 and MCF-7. Some compounds displayed satisfactory activities. [ABSTRACT FROM AUTHOR]