Synthesis and biological evaluation of 4-oxycoumarin derivatives as a new class of antifilarial agents.
Basic Information
ID: ALA3414470
Journal: Eur J Med Chem
Title: Synthesis and biological evaluation of 4-oxycoumarin derivatives as a new class of antifilarial agents.
Authors: Misra S, Singh LK, Priyanka, Gupta J, Misra-Bhattacharya S, Katiyar D.
Abstract: A series of 4-oxycoumarin derivatives was synthesized, characterized and evaluated in vitro and in vivo for antifilarial activity against the human lymphatic filarial parasite, Brugia malayi. A majority of the compounds studied showed potent in vitro activity with low IC50 values in the micro molar (μM) range (0.014-1.73 and 0.0056-0.43) against adult worms and microfilariae, respectively. Compounds 8 and 9 were identified to be the most promising antifilarial candidate molecules exhibiting activity in the nanomolar (nM) range. The IC50 values for compound 8 were 14 nM and 5.6 nM while for compound 9 were 94 nM and 13 nM, respectively, for adult worm and microfilaria. These two compounds also displayed promising adulticidal activity (74.9 ± 4.8% and 69.4 ± 2.8%, respectively) in the primary rodent (jird) screen. This study also serves as a starting point for investigating structure-activity relationship with different amino substituents.
CiteXplore: 25768703
DOI: 10.1016/j.ejmech.2015.02.043
Patent ID: ┄