Other bioactive products U 1300Naphthoquinoidal [1,2,3]-Triazole, a New Structural Moiety Active Against Trypanosoma cruzi. -Triazole derivatives (IV) of nor-β-lapachone are synthesized and tested against the infective bloodstream trypomastigote form of Trypanosoma cruzi. All derivatives are more active than the original quinones. The apolar phenyl-substituted triazole (IVe) is the most active compound. -(DA SILVA, E. N. J.; MENNA-BARRETO, R. F. S.; PINTO, M. D. C. F. R.; SILVA, R. S. F.; TEIXEIRA, D. V.; DE SOUZA, M. C. B. V.; DE SIMONE, C. A.; DE CASTRO*, S. L.; FERREIRA, V. F.; PINTO, A. V.; Eur.

The method represents the first catalytic, directed method for ortho‐functionalizations of simple naphthoquinones.

Imidazoles from Nitroallylic Acetates and -Bromonitroalkenes with Amidines: Synthesis and Trypanocidal Activity Studies. -Cascade reactions of amidines (II) with title compounds (I) and (IV) afford 2,4,5-trisubstituted and 2,4-disubstituted imidazoles (III), (V), and (VI), respectively. Some of the obtained compounds exhibit trypanocidal activity similar or even higher [cf. (IIIa)] than the standard benznidazole. -(GOPI, E.; KUMAR, T.; MENNA-BARRETO, R. F. S.; VALENCA, W. O.; DA SILVA*, E. N. J.; NAMBOOTHIRI, I. N. N.; Org. Biomol. Chem. 13 (2015) 38, 9862-9871, http://dx.

Activity. -Compound (IIId) shows better and compounds (IIIe) and (IIIf) show similar activity against Trypanosoma cruzi compared with the reference benznidazole. All other compounds are less active or even inactive. -(KUMAR, T.; VERMA, D.; MENNA-BARRETO, R. F. S.; VALENCA, W. O.; DA SILVA*, E. N. J.; NAMBOOTHIRI, I. N. N.; Org.

VI) are formed in high yields with good to excellent, dia-and enantioselectivities. The transformation, which involves an S N2 ' -intramolecular oxa-Michael addition sequence, is amenable for scale-up even with low catalyst loadings. Preliminary evaluation of the -lapachone derivatives (III) for trypanocidal activity show no deleterious effects on the parasites. -(NAIR, D. K.; MENNA-BARRETO, R. F. S.; DA SILVA, E. N. J.; MOBIN, S. M.; NAMBOOTHIRI*, I. N. N.; Chem. Commun. (Cambridge) 50 (2014) 53, 6973-6976, http://dx.doi.org/10.1039/c4cc02279c ; Dep. Chem., Indian Inst. Technol. Bombay, Mumbai 400 076, India; Eng.) -M. Paetzel 47-025