Certain benzoyl chloride phenylhydrazones have been found to be active against insects and mites, and they have also been found to be effective, broad-spectrum anthelmintics for suppressing parasitic worms in animals, particularly sheep. The benzoyl ring and the phenylhydrazone ring can be substituted with a halogen atom, a nitro group, or an alkyl group of from 1 to 6 carbon atoms, inclusive. A new class of pentahalobenzoyl chloride phenylhydrazones is described, particularly pentafluorobenzoyl chloride phenylhydrazones. The compounds are prepared by reacting a benzoic acid phenylhydrazide with phosphorus pentachloride to obtain a benzoyl chloride (dichlorophosphinyl)phenylhydrazone that is reacted with phenol to produce the desired benzoyl chloride phenylhydrazones. Certain of the compounds can be prepared by direct chlorination of a benzaldehyde phenylhydrazone. Methods of using the new compounds and new anthelmintic formulations are described. The new compound p-toluoyl chloride phenylhydrazone is effective against worms at rates at least as low as 100 mg./kg. of body weight in sheep.
Synthesis and biological activity of anthelmintic thiadiazoles using an AF-2 receptor binding assay
作者:Byung H Lee、Fred E Dutton、Michael F Clothier、Jerry W Bowman、John P Davis、Sandra S Johnson、Eileen M Thomas、Marjorie R Zantello、Erich W Zinser、James C McGuire、David P Thompson、Timothy G Geary
DOI:10.1016/s0960-894x(99)00267-x
日期:1999.6
suum), we prepared two series of analogs. Only the series containing the thiadiazole ring had potencies comparable to that of compound 1. Analog 50 exhibited an apparent potency in the AF-2 binding assay 300 times that of compound 1.
Certain benzoyl chloride phenylhydrazones have been found to be active against insects and mites. The benzoyl ring and the phenylhydrazone ring can be substituted with a halogen atom, a nitro group, or an alkyl group of from 1 to 6 carbon atoms, inclusive. A new class of pentahalobenzoyl chloride phenylhydrazones is described, particularly pentafluorobenzoyl chloride phenylhydrazones. A further new class of alkylbenzoyl chloride phenylhydrazones, particularly p-toluoyl chloride phenylhydrazones are also described. The compounds are prepared by reacting a benzoic acid phenylhydrazide with phosphorus pentachloride to obtain a benzoyl chloride (dichlorophosphinyl)phenylhydrazone that is reacted with phenol to produce the desired benzoyl chloride phenylhydrazones. Certain of the compounds can be prepared by direct chlorination of a benzaldehyde phenylhydrazone. Methods of use and compositions are described.
Synthesis and Characterization of New 3<sup>″</sup>,5<sup>″</sup>-DIARYL-3<sup>″</sup><i>H</i>-Dispiropyran/Thiopyran[4,2′-Chroman-3′,2<sup>″</sup>-[1,3,4-Thiadiazol]-4′-One Derivatives and Related Compounds as Anticancer and Antiviral Agents
作者:Mohamed I. Hegab、Eman. M. H. Morsy、Ahmed E. Abd El-Megeid、Mamdouh M. Ali、W. M. El-Senousy、Hala E. M. Tolan、Farouk A. Gad、Farouk M. E. Abdel-Megeid
DOI:10.1080/10426507.2015.1032410
日期:2015.11.2
inhibiting of human tyrosine kinase showed that most of the tested compounds possess antiproliferative activity as potent to moderate growth inhibitory activity, especially compounds 3b, 5a, 5c, 5e, 5g, and 5k. Also, the prepared compounds were tested against rotavirus Wa strain and adenovirus type 7 and the results showed that two compounds (5e,n) were active.