Thirteen aminoalcohols and eight diamines were obtained and tested against Trypanosoma cruzi epimastigotes strains MG, JEM and CL-B5 clone. Some of them were equal or more potent (1.0-6.6 times) than the reference compound nifurtimox. From them, three aminoalcohols and two diamines were selected for amastigotes assays. Compound 5 was as potent as the reference drug nifurtimox against amastigote...

We investigated the antiplasmodial properties of crude extracts from Carica papaya leaves to trace the activity through bioassay-guided fractionation. The greatest antiplasmodial activity was observed in the ethyl acetate crude extract. C. papaya showed a high selectivity for P. falciparum against CHO cells with a selectivity index of 249.25 and 185.37 in the chloroquine-sensitive D10 and chlor...

The object-relational database management system (ORDBMS) offers many potential benefits for scientific, multimedia and financial applications. However, work remains in the integration of domain-specific class libraries into ORDBMS query processing. A major problem is that the standard mechanisms for query selectivity estimation, taken from relational database systems, rely on properties specif...

Fishing impacts on marine food webs are predicted by simulations of a size spectrum community model. In this model, predation is determined by predator and prey size and abundance, and drives predator growth and prey mortality. Fishing amplifies temporal oscillations in the biomass flow. Oscillations appear at lower fishing intensity and have wider amplitude when fishing is selective (removes a...

This study designed and synthesized a series of new graveoline analogs on the basis of the structural characteristics of acetylcholinesterase (AChE) dual-site inhibitors. The activity of these analogs was also evaluated. Results showed that the synthesized graveoline analogs displayed stronger inhibitory activity against AChE and higher selectivity than butyrylcholine esterase (BuChE) (Selectiv...

Diffraction of plane waves on dielectric gratings with planar plasmonic inserts is studied with the emphasis put on the anomalous selectivity of diffraction orders. It is shown that some formally propagating orders can be suppressed within a wide frequency range. The effect of suppression is more general than the isolation effect observed earlier in zero-permittivity and (near-)zero-index slabs...

The ability to control encoding and retrieval processing strategically is critical for the efficient use of memory. We examined the ability of younger and older adults to selectively remember words on the basis of their arbitrary point values by using a technique developed by Watkins and Bloom (1999). In the first three experiments, younger subjects recalled more words than did older subjects, ...

Several aliphatic and aromatic lactones and two dimers were synthesized using the sequence: allylation - esterification - metathesis. These compounds were active in vitro against intracellular amastigotes of Leishmania panamensis. The structure-activity relationship showed the importance of the aliphatic side chain to enhance the biological activity and to obtain lower cytotoxicity. It was also...

The high throughput screening of a library of over 87,000 drug-like compounds against the African sleeping sickness parasite resulted in the discovery of hits with a wide range of molecular diversity. We report here the medicinal chemistry development of one such hit, a tetrahydroisoquinoline disulfonamide, with the synthesis and testing of 26 derivatives against the trypanosome subspecies. Act...