Synthesis and antibacterial activity of a series novel 5,7-diisoprenyloxyflavone derivatives

Abstract

In the present study, a series of novel 5,7-diisoprenyloxyflavone derivatives were designed, synthesized, and evaluated for their antibacterial activity. Most of these compounds displayed significant antibacterial effects against Gram-positive bacteria, especially against strains of multidrug-resistant clinical isolates . Compounds 4c, 4g, 4i, 4j, 4k, 4l, 4n, 4q and 4t showed high levels of antimicrobial activity against Staphylococcus aureus RN4220 with minimum inhibitory concentrations of 4.0-20 μM. Compound 4k showed the most potent activity among these compounds against all multidrug-resistant clinical isolates tested. Unfortunately, none of the compounds were active against Gram-negative bacteria at the doses of 24-164 μM.

Untitled

“…Thus, it is necessary to produce scaffolds to develop new leads for further therapeutic purposes. In fact, the new drug development approach has been carried out with various procedures, such as combining existing drugs [4], use of natural ingredients [5], synthesis of new compounds [6,7], and the development of environmentally friendly synthesis (green chemistry) [8]. The multicomponent reaction (MCR) is an approach to achieve the efficient synthesis.…”