Synthesis and larvicidal activities of compounds based on coumarin and dibenzothiophene/carbazole

摘要

Based on a rationally conceived pharmacophore model to build a dual-target mosquito larvicide, a family of coumarin-dibenzothiophene or -carbazole hybrids with various substituents on phenyl were synthesized in moderate yields. Larvicidal activity of hybrid molecules were evaluated against fourth instar larvae of Aedes aegypti. Most of the synthesized hybrids displayed moderate to high activity and the activities of coumarin-linked carbazole hybrids were better than those of dibenzothiophene hybrids. The structure-activity relationships revealed that coumarin, dibenzothiophene and carbazole were the key pharmacophore and carbazole derivatives consisting of an electron-withdrawing group in the coumarin-carbazole hybrid molecular structure possess better activity than their corresponding parent compound.