Synthesis and antimalarial activity of new nanocopolymer β-lactams and molecular docking study of their monomers
摘要:
This report describes the preparation of some new beta-lactam nanocopolymers. These nanoparticles are synthesized in water by emulsion polymerization of an acrylate beta-lactam pre-dissolved in a mixture of co-monomers in the presence of sodium dodecyl sulfate as a surfactant and potassium persulfate as a radical initiator. Dynamic light scattering analysis and electron microscopy images of these emulsions show that the nanoparticles are approximately 30-70 nm in diameter. These compounds have been evaluated for their antimalarial activities against chloroquine-resistant Plasmodium faliparum K1 strain demonstrating IC50 varying from 14 to 50 A mu M. The interactions between these beta-lactam nanocopolymers and the P. falciparum single-stranded DNA-binding proteins have been studied by molecular docking calculations.
Schiff bases derived from p-aminobenzyl alcohol as trigger groups for pH-dependent prodrug activation
摘要:
A number of novel acid-sensitive Schiff bases derived horn p-aminobenzyl alcohol and various benzaldehyde derivatives were synthesized and were subsequently shown to trigger benzyl elimination reactions The kinetics of acid-catalyzed hydiolysis at pH 50 as well as stability at pH 74 were studied using fluorogenic model compounds Two fluoro-substituted Schiff bases showed efficient hydrolysis at pH 5 0 combined with a long-term stability at pH 74 and are considered suitable candidates for the development of anticancer prodrugs (c) 2010 Elsevier Ltd All lights reserved