2 resultados para SALVAGE
em Biblioteca Digital da Produção Intelectual da Universidade de São Paulo (BDPI/USP)
Resumo:
This paper analyzes the changes the ways of organizing memory have undergone since ancient times, turning them into the current artificial memory systems. It aims to draw a parallel between the art of memory (which associates images to specific texts) and the hypertext (which also uses associations, but in a non-linear way). Our methodology consisted of a qualitative approach, involving the collection of texts about the art of memory and hypertext; this enables us to salvage the historical-cultural changes which have modified form and use of the art of memory and allowed the creation of hypertext. It also analyzes the similarities among artificial memory systems created by different cultures in order to prevent loss of knowledge produced by society.
Resumo:
Schistosomiasis is considered the second most important tropical parasitic disease, with severe socioeconomic consequences for millions of people worldwide. Schistosoma monsoni, one of the causative agents of human schistosomiasis, is unable to synthesize purine nucleotides de novo, which makes the enzymes of the purine salvage pathway important targets for antischistosomal drug development. In the present work, we describe the development of a pharmacophore model for ligands of S. mansoni purine nucleoside phosphorylase (SmPNP) as well as a pharmacophore-based virtual screening approach, which resulted in the identification of three thioxothiazolidinones (1-3) with substantial in vitro inhibitory activity against SmPNP. Synthesis, biochemical evaluation, and structure activity relationship investigations led to the successful development of a small set of thioxothiazolidinone derivatives harboring a novel chemical scaffold as new competitive inhibitors of SmPNP at the low-micromolar range. Seven compounds were identified with IC(50) values below 100 mu M. The most potent inhibitors 7, 10, and 17 with 1050 of 2, 18, and 38 mu M, respectively, could represent new potential lead compounds for further development of the therapy of schistosomiasis.