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Communication | Special issue | Vol 101, No. 1, 2020, pp.116-125
Published online, 19th July, 2019
DOI: 10.3987/COM-19-S(F)18
Rapid Exploration of Novel Anthelmintic Agents from Alkyne-Bearing Avermectin Derivatives via Click Chemistry

Tomoyasu Hirose, Akari Ikeda, Ayumi Tsutsui, Satoshi Ōmura, and Toshiaki Sunazuka*

*The Kitasato Institute for Life Sciences and Graduate School of Infection Control Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641


We applied copper-catalyzed 1,4-disubstituted-1,2,3-triazole formation, a major connective reaction in “Click Chemistry”, to synthesize novel avermectin derivatives. Among the synthetic triazole-containing avermectins, the 4-hydroxybutyltriazole derivative (3a) was found to demonstrate notable antinematodal activity against ivermectin-resistant Trichinella spiralis in vitro. Furthermore, a new compound (3a) also exhibited strong antinematode properties against ivermectin-resistant Haemonchus contortus in sheep following oral administration.