Chemotherapy of Filariasis - On the Search of New Agents Effective on the Reproductive System of Female Adult Worms [1]

The design and synthesis o f a series o f alkyl 5(6)-substituted benzimidazole-2-carbamates (1-13), 7-chloro-4-(4-substituted phenyl)aminoquinolines (14-16), l,2-dimethyl-3-methoxycarbonyl-4,5-disubstituted pyrroles (17—19) and some compounds belonging to the class pimelonitrile (20), dihydroquinoline (21), pyridine (22), pyridoquinoline (23) and tetrahydropyrimidine (24) have been carried out as possible antifilarial agents. All these compounds have been evaluated for their activity against male and female adult worms o f Litomosoides carinii in cotton rats. The effect o f these compounds was also observed on the reproductive system (condition o f developing microfilariae and their release from uterus) o f adult female worms. In this study, three types o f compounds were discovered: (a) those which showed activity on both the male and female adult worms and also had sterilizing effects on surviving adult females (1 -3 , 6 -9 , 13, 19), (b) those which only sterilized the adult females (14-16 , 21, 24), and (c) those which had no effect on female reproduction but killed only adult worms (4, 5, 11, 12, 17,18, 20, 22, 23). This tends to open up a new avenue in the chemotherapy o f filariasis and the future scope o f work on chemosterilization o f adult females has been discussed.