13724-89-5Relevant academic research and scientific papers
Synthesis and Activity Studies on 3-(Carboxyalkylthio)rifamycin S Derivatives
Cellai, Luciano,Martuccio, Concetta,Marzano, Marina,Onori, Alberto Mochi,Mannina, Luisa,et al.
, p. 317 - 324 (2007/10/03)
A series of rifamycin S derivatives carrying at C(3) an aliphatic side-chain of variable length terminating with a carboxyl has been synthesised; in particular, five of these compounds carry a terminal dipeptide.The aim was to prepare potential bifunctional HIV-1 reverse transcriptase inhibitors, able both to bind at the non-nucleoside inhibitors binding site, through the chromophore rings, and to interfere with the catalytic centre, through the side-chain terminal carboxyl.Some of the compounds display an interesting inhibitory power (IC50 45-60 μM).In addition, a few of these derivatives have been also tested as potential antibacterial agents, and showed a good level of activity toward Gram-positive bacteria.
