In Silico Approach Towards the Prediction of Drug-Likeness; Synthesis and In Vitro Evaluation of Biphenyl Derivatives
2021
Two series of biphenyl derivatives have been synthesized, characterized and
evaluated for various biological activities. One of the products demonstrates
efficient urease inhibition. All compounds synthesized from fast blue B salt and
O-alkylated derivatives display excellent
β-glucuronidase inhibition activity, and one of those is a scavenger of
superoxide anion radical. The products are not active in phosphodiestrase
inhibition bioassay. Most of synthetic biphenyl analogues have demonstrated
significant in vitro antimalarial activity against plasmodium falciparum. All
synthesized compounds exhibit low mortality effect on the tested insects.
Molecular structures of the synthesized compounds have been docked into the
active sites of urease and β-glucuronidase protein, and all active compounds
have demonstrated good interacting pattern. Upon further experimental
validation, these compounds could be used as potential inhibitors against urease
and β-glucuronidase.
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