Synthesis and HIV-1 Integrase Inhibition of Novel Bis- or Tetra-Coumarin Analogues

design, synthesis, and acetylcholinesterase inhibitory activity of novel coumarin analogues

Design, synthesis, and acetylcholinesterase inhibitory activity of novel coumarin analogues.

Three series (series A-C) of coumarin analogues with phenylpiperazine functions as substitution were designed and synthesized for studying their potential for treating Alzheimer's (AD) disease. Their anticholinesterase activities were assayed according to Ellmann's method against freshly prepared acetylcholinesterase (AChE) from Electrophorus electricus using donepezil as the reference compound...

Chicoric acid analogues as HIV-1 integrase inhibitors.

The present study was undertaken to examine structural features of L-chicoric acid (3) which are important for potency against purified HIV-1 integrase and for reported cytoprotective effects in cell-based systems. Through a progressive series of analogues, it was shown that enantiomeric D-chicoric acid (4) retains inhibitory potency against purified integrase equal to its L-counterpart and fur...

Novel HIV integrase inhibitors with anti-HIV activity: insights into integrase inhibition from docking studies.

The mechanism of integrase is generally accepted to be dependant on the presence of two divalent metal ions in the active site. However, the only available crystal structures of HIV-1 integrase contain either one or no metal ions, hampering structure-based design studies of integrase inhibitors. For this reason, a two-metal ion model of integrase was constructed. This model was used for computa...

novel coumarin analogues: as new acetylcholinesterase inhibitors