4.2 Article

Design, Synthesis, and Evaluation of Novel L-Pyroglutamic Acid Derivatives as Potent Antifungal Agents

Journal

CHEMISTRY OF NATURAL COMPOUNDS
Volume 57, Issue 6, Pages 1081-1085

Publisher

SPRINGER
DOI: 10.1007/s10600-021-03553-1

Keywords

L-pyroglutamic acid; Phytophthora infestans; antifungal activity; structure-activity relationship

Funding

  1. National Natural Science Foundation of China [21977083]

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A series of novel L-pyroglutamate derivatives containing 1,2,3-triazole ring substructures were synthesized and evaluated for their antifungal activity against Phytophthora infestans. Compounds with phenyl or benzyl substituents at the meta-position of the triazole ring exhibited potent antifungal activity. Some of the L-pyroglutamic acid derivatives showed promising antifungal activity against Phytophthora infestans.
A series of novel L-pyroglutamate containing 1,2,3-triazole ring substructures was synthesized and characterized by adopting an appropriate synthetic scheme. The effect of different substituents on the triazole ring at the ortho-, meta- and para-positions of the benzene ring was evaluated for the inhibition of zoospore release activity against Phytophthora infestans. Among the triazole analogs of L-pyroglutamate, compounds with a phenyl or benzyl group on the triazole ring at the meta-position of the benzene ring showed potent antifungal activity. Results indicated that some of the L-pyroglutamic acid derivatives possessed antifungal activity against Phytophthora infestans.

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