Miscellaneous T. cruzi compounds

Nitroheteroarenes continue to attract research activity. A series of 5-nitro-2-furyl derivatives were evaluated for in vivo efficacy against T cruzi [64] and an improved toxicity profile. Compound 65 showed a good efficacy profile in vivo and better acute toxicity profile when compared to nifurti-mox. A series of 5-nitroindazoles, represented by 66 (IC50 = 7.4 iM), were reported as having activity similar to nifurtimox (IC50 = 3.4 iM) in a growth inhibition assay [65]. 

Renauld, E. A. Worthey, C. Flertz-Fowler, E. Ghedin, C. Peacock, D. C. Bartholomeu, B. J. Haas, A. N. Tran, J. R. Wortman, U. C. Alsmark, S. Angiuoli, A. Anupama, J. Badger, F. Bringaud, E. Cadag, J.M. Carlton, G.C. Cerqueira, T. Creasy, A. L. Delcher, 

Mutabilis, 102 Avenue Gaston Roussel, Romainville F-93230, France 

Annual Reports in Medicinal Chemistry, Volume 45 ISSN 0065-7743, DOI 10.1016/S0065-7743(10)45018-6 

Significant work continues by both the academic groups and the pharmaceutical industry to validate the FASH targets and discover relevant inhibitors. A selection of some efforts to inhibit bacterial fatty acid biosynthesis at various stages is presented in this chapter. 

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