1 research outputs found
New thiazolidine-2,4-dione derivatives combined with organometallic ferrocene: Synthesis, structure and antiparasitic activity
Favourable physicochemical properties of an organometallic ferrocene and antiplasmodial potency of compounds containing the thiazolidineā2,4ādione framework (TZDā4) prompted us to explore compounds containing both the thiazolidineā2,4ādione core and the ferrocenyl unit with the primary aim of identifying compounds with promising antiprotozoal activities. Thus, a new series of rationally designed ferroceneābased thiazolidineā2,4ādione derivatives, containing a selection of secondary cyclic amines, was synthesised and fully characterised using standard spectroscopic techniques. The resulting compounds were screened for their antiplasmodial and antitrypanosomal activities against both the chloroquineāresistant (Dd2) strain of Plasmodium falciparum and the Nagana Trypanosoma brucei brucei 427. The general trend that emerged indicated that the target compounds were more selective towards T. b. brucei compared to the P. falciparum parasite. Moreover, the analogues bearing methylpiperazine (8a) and piperidine (8b) rings were more active against T. b. brucei compared to hit compound TZDā4. Except compound 8b, which appeared promising, none of the synthesised compounds showed better activity than TZDā4 against the P. falciparum parasite. All the synthesised compounds were nonātoxic and often showed >90% viability of the HeLa cell line screened