Three novel cobalt(iii)-triazole complexes with structural and redox properties suitable for hypoxia-activated drug delivery were obtained. A major influence of the ancillary ligands (TPA, py2en, py2enMe2) on the electronic properties and reactivity of their complexes was observed. An [O2]-dependent reduction to cobalt(ii) by ascorbic acid provided evidence of hypoxic selectivity.

No abstract

No abstract

We described the synthesis of a new congener series of 1,2,3-triazolyl-4-oxoquinolines and evaluated their ability to inhibit oseltamivir (OST)-resistant influenza strains. Oxoquinoline derivative 1i was the most potent compound within this series, inhibiting 94% of wild-type (WT) influenza neuraminidase (NA) activity. Compound 1i inhibited influenza virus replication with an EC50 of 0.2μM with less cytotoxicity than OST, and also inhibited different OST-resistant NAs. These results suggest that 1,2,3-triazolyl-4-oxoquinolines represent promising lead molecules for further anti-influenza drug design.

Nucleic acids U 0700Synthesis and anti-HSV-1 Activity of Quinolonic Acyclovir Analogues. -The majority of the acyclonucleosides (VI) and (VII) obtained possess anti-HSV activity. In general, the acids (VII) appear to be more effective inhibitors than their corresponding esters (VI). Compounds (VIIg) and (VId) are the most effective anti-HSV-1 derivatives which provide a 1.5-and 1.3-fold increase, resp., in their antiviral activity in relation to acyclovir. -(D'A. LUCERO, B.; GOMES, C. R. B.; DE P. P. FRUGULHETTI, I. C.; FARO, L. V.; ALVARENGA, L.; DE SOUZA*, M. C. B. V.; DE SOUZA, T. M. L.; FERREIRA, V. F.; Bioorg. Med. Chem. Lett. 16 (2006) 4, 1010-1013; Dep. Quim. Org., Univ. Fed.