A series of novel carbamo(dithioperoxo)thioate derivatives have been prepared in excellent yield using a significantly fast, one-pot three component reaction and experimented for their potential as anti-filarial agents against model filarial nematode Setaria cervi. Among 23 compounds (4a-w) evaluated for the anti filarial activities, five compounds (4a, 4b, 4c, 4d and 4h) have shown promising anti-proliferative effects on the juvenile stage microfilariae (mf) as well as in adults in a time and dose dependent manner. Compound 4a was found most active against oocytes, mf and adult nematods as well as non-cytotoxic to the normal cells. It has been established that the anti-filarial activity of the compounds were observed due to the involvement of reactive oxygen species (ROS) and apoptosis. Several biochemical and microscopic experiments have been carried out to establish the fact that both intrinsic and extrinsic pathways of apoptosis contribute to the compound 4a mediated death phenomenon of the filarial nematodes. (C) 2017 Elsevier Masson SAS. All rights reserved.
Electrochemical synthesis of carbamo(dithioperoxo)thioates through the dehydrogenation coupling of thiols and amines and the insertion of CS<sub>2</sub>
simple dehydrogenation coupling of thiols and amines and the insertion of CS2 under mild reaction conditions and in the absence of oxidizing reagents. This environmentally friendly electrosynthesis method has a broad substrate scope and can produce a series of bioactive compounds. This strategy is further employed in an electrochemical continuous flow reactor for the preparation of some antifilarial activity