RESUMEN
cis- and trans-(Cl,Cl)-[RuII(FT)Cl2(NO)](PF6) complexes show efficient NO photodelivery upon two-photon excitation in the NIR region. Moreover, cytotoxicity and phototoxicity studies provide evidence that these complexes are promising candidates as photoactivatable molecular tools for resection of malignancies.
Asunto(s)
Antineoplásicos/química , Rayos Infrarrojos , Óxido Nítrico/metabolismo , FototerapiaRESUMEN
A series of GEQ analogues bearing pyrrolidinone or pyrrolidine cores were synthesized and evaluated against InhA, essential target for Mycobacterium tuberculosis (M.tb) survival. The compounds were also evaluated against M.tb H37Rv growth. Interestingly, some of the compounds, not efficient as InhA inhibitors, are active against M.tb with MICs up to 1.4 µM. In particular, compound 4b was screened with different M.tb mutated strains in order to identify the cellular target, but without success, suggesting a new possible mode of action.
Asunto(s)
Proteínas Bacterianas/antagonistas & inhibidores , Diseño de Fármacos , Mycobacterium tuberculosis/efectos de los fármacos , Oxidorreductasas/antagonistas & inhibidores , Pirrolidinas/química , Pirrolidinas/farmacología , Pirrolidinonas/química , Pirrolidinonas/farmacología , Antituberculosos/química , Antituberculosos/metabolismo , Antituberculosos/farmacología , Proteínas Bacterianas/química , Proteínas Bacterianas/metabolismo , Evaluación Preclínica de Medicamentos , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/metabolismo , Inhibidores Enzimáticos/farmacología , Escherichia coli/efectos de los fármacos , Proteínas de Transporte de Membrana/metabolismo , Pruebas de Sensibilidad Microbiana , Simulación del Acoplamiento Molecular , Mycobacterium tuberculosis/metabolismo , Oxidorreductasas/química , Oxidorreductasas/metabolismo , Conformación Proteica , Pirrolidinas/metabolismo , Pirrolidinonas/metabolismo , Relación Estructura-ActividadRESUMEN
Hitherto unknown AuâAl interactions have been evidenced upon coordination of the geminal phosphorus-aluminum Lewis pair Mes2 PC(=CHPh)AltBu2 (Mes=2,4,6-trimethylphenyl). Four different gold(I) complexes featuring alkyl (Me), aryl (Ph, C6F5), and alkynyl (C≡CPh) co-ligands have been prepared. X-ray diffraction analyses show that PâAuâAl bridging coordination induces noticeable bending of the ligand (the PCAl bond angle shrinks by 13°). This new type of transition metalâLewis acid interaction has been analyzed by DFT calculations.
Asunto(s)
Aluminio/química , Oro/química , Complejos de Coordinación/química , Cristalografía por Rayos X , Ácidos de Lewis/química , Conformación Molecular , Fósforo/química , Elementos de Transición/químicaRESUMEN
Coordination of Mes2PC(=CHPh)AltBu2 to metal chlorides has been studied. Bridging PâM-ClâAl coordinations were observed with Rh and Pd fragments, while chloride abstraction systematically occurred with gold. The resulting zwitterionic complexes have been fully characterized and analyzed by DFT calculations.
Asunto(s)
Aluminio/química , Complejos de Coordinación/química , Oro/química , Interacciones Hidrofóbicas e Hidrofílicas , Fósforo/química , Ligandos , Modelos Moleculares , Conformación MolecularRESUMEN
The copper complex of a polydentate non-symmetrical Schiff base ligand [LCu]2, prepared by template synthesis, has been reacted with the series of lanthanide ions. This complex used as a ligand possesses two functions (phenol and oxime) able to coordinate the Ln ions and, according to the Ln ion, three types of complexes are obtained. From La to Eu, trinuclear [(LCu)2Ln(NO3)3] complexes with a double phenoxo-oximato bridge were isolated. From Gd to Ho, the complexes [(LCu)2Ln(NO3)3(H2O)] are still trinuclear, with a supplementary water molecule linked to the Ln ion but the Cu(II) and Ln(III) ions are only bridged by the oximato (N-O) pair, the phenoxo oxygen atom being hydrogen-bridged to the Ln-coordinated water molecule. Then, with heavier Ln ions, dinuclear [(LCu)Ln(NO3)3(H2O)2] complexes are characterized. The magnetic study demonstrates that the oximato bridge is responsible for the antiferromagnetic character of the Cu-Gd interaction, with JCuGd = -0.63 cm(-1) in [(LCu)2Gd(NO3)3(H2O)], in contrast to the ferromagnetic Cu-Gd interaction induced by the single oxygen atom phenoxo bridge.
RESUMEN
Three new spermidine alkaloids and two known compounds were isolated from the leaves of Androya decaryi. Their structures were elucidated on the basis of their spectroscopic data (NMR and mass spectrometry), by X-Ray diffraction and by comparison with literature values. Evaluation of the in vitro antiplamosdial properties of the isolated compounds revealed they did not possess any significant activity.