19881-18-6Relevant articles and documents
Synthesis of new 4[4-(4-nitrophenoxy)phenyl]-5-substituted-2H-1,2,4-triazole-3-thiones and their evaluation as anthelmintics
Namratha,Bilehal, Dinesh,Shyamkumar,Gaonkar, Santosh L.
, p. 1885 - 1897 (2016)
A library of novel 4-[4-(4-nitrophenoxy)phenyl]-5-substituted-2H-1,2,4-triazole-3-thiones containing different substituents at the 5-position is synthesized. The mechanochemical treatment is followed to synthesize target compounds 8 (a-p), and the yields are compared by both the grinding method and the conventional method. The structure of the intermediate, isothiocyanato-4-(4-nitrophenoxy)benzene 6, is analyzed by single crystal X-ray studies. The title compounds are characterized by spectral and elemental analyses and further evaluated for their efficacy as anthelmintics in vitro. Compounds 8c, 8j, 8k, 8l, and 8m exhibit significant anthelmintic activity.
Design, synthesis and bioactivities of phenithionate analogues or derivatives for anti-schistosomiasis
Zhou, Shiyang,Huang, Gangliang
, p. 328 - 336 (2018/03/08)
A novel series of phenithionate analogues or derivatives were designed and synthesized using phenithionate as the lead compound, and their bioactivities were studied. Their structures were confirmed by 1H NMR, 13C NMR, HR-ESI-MS, and elemental analysis, respectively. The results of in vitro inhibitory activity measurement proved that compounds 5a, 5c, 5g, 5i, 5m and 5o had a better inhibitory effect on larva and imago schistosoma. Among them, the inhibitory activity of compound 5i for larva schistosoma was IC50 = 5.21 ± 0.04 μg mL-1, and for imago schistosoma it was IC50 = 6.35 ± 0.08 μg mL-1. Moreover, the experimental results of in vivo anti-schistosomiasis activity measurement showed that they had good anti-schistosomiasis activity. Therefore, these compounds had better drugability.
Novel synthesis of anthelmintic drug 4-isothiocyanato-4′- nitrodiphenyl ether and its analogs
Chaskar,Bandgar,Modhave,Patil,Yewale
experimental part, p. 992 - 1001 (2009/09/08)
An efficient, mild, chemoselective, and convenient protocol for synthesis of isothiocyanate derivatives. This protocol was applied successfully in the novel synthesis of anthelmintic drug 4-isothiocyanato-4′-nitrodiphenyl ether and its analogs. Copyright Taylor & Francis Group, LLC.
