THERAPEUTIC POTENTIAL OF NOVEL HETEROCYCLIC THIAZOLIDINE COMPOUNDS AGAINST HUMAN LYMPHATIC FILARIAL PARASITE: AN IN VITRO STUDY
AbstractObjective: Following World Health Organization tropical disease research mandate, there is definitive need for search of new lead molecules for development of drug against human lymphatic filariasis. Thiazolidineone derivatives has shown versatile therapeutic potential. The present study has been undertaken to explore the possible antifilarial effect of such synthetic compounds against filarial parasite, Brugia malayi. Methods: A series of 12 thiazolidineone derivatives, following synthesis and characterization, were screened for antifilarial potential in vitro against microfilarial stage of Brugia malayi; those showed significant effect were tested against adult parasites also. The pharmacological response in terms of loss of parasitic motility was assessed under microscope. Further dose dependent response and potential lethality onto host cells for such effective drugs were carried out. Result: Out of the tested compounds, four such compounds showed significant activity and those were tested against the adult worms; one of these compounds showed marked effect. The corresponding IC50 and LD50 values were deduced for each of these four effective compounds. Most of them showed a good therapeutic index. Conclusion: Since the standard drug Diethyl Carbamazine Citrate is largely dependent on the host innate immune response and also not effective as microfilaricidal, hence the observed result with that thiazolidineone compounds have definitive potential for being considered as important therapeutic lead molecules against both microfilarial as well as the adult stage of the parasite
Article Information
15
1480-92
445
1148
English
IJPSR
A. Mandvikar, S.V. Hande , P. Yeole , K. Goswami * and M. V. R. Reddy
Department of Biochemistry, Mahatma Gandhi Institute of Medical Sciences, Sevagram, Maharashtra, India
goswamikln@gmail.com
07 October, 2015
23 November, 2015
12 January, 2016
10.13040/IJPSR.0975-8232.7(4).1480-92
01 April, 2016