PMID: 8982793Oct 1, 1996Paper

Antifilarial and trypanocidal properties of phenothiazines and related polycyclics as new lead structures

International Journal for Parasitology
P M LoiseauJ M Vierfond

Abstract

New phenothiazine derivatives and 4 related lead structures have been studied for their antifilarial and trypanocidal properties. Regarding phenothiazine derivatives, the nitrile group at the 3 position on the phenothiazine ring had a strong in vitro antifilarial effect against Molinema dessetae infective larvae. Among the 4 new lead structures, compound 4 or naphtho(2',3': 4,5) thiazolo(3,2-a)benzimidazole-7,12-dione was the most antifilarial, with IC50 of 8 microM at day 8. These results justify further studies in vivo. A slight effect was observed against the trypanosomes maintained in vitro since minimum inhibitory concentrations of active compounds were 50 microM after a 24-h incubation period. Nevertheless, no trypanocidal activity was observed in vivo after a 100 mg kg-1 treatment and the compound 3 or dibenzo(b,f)(1,4)thiazine-11-amine was lethal at this dose. These new lead structures have now to be optimised using pharmaco-modulations.

References

Dec 1, 1970·Experimental Parasitology·S M Lanham, D G Godfrey
Nov 1, 1983·Molecular and Biochemical Parasitology·T Seebeck, P Gehr
Oct 1, 1953·Experimental Parasitology·P D HARWOOD
Dec 1, 1954·The Journal of Pharmacy and Pharmacology·R B GRIFFITHS

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Citations

Apr 8, 2014·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Manitriniaina RajemiarimirahoFrançoise Benoit-Vical
Mar 24, 2011·Future Medicinal Chemistry·Prashant Kumar SinghShailja Misra-Bhattacharya
Jul 18, 2014·PLoS Neglected Tropical Diseases·Joseph D PlanerFrederick S Buckner

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