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Synthesis, Antifungal Activities and Molecular Docking Studies of Benzoxazole and Benzothiazole Derivatives
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Synthesis, Antifungal Activities and Molecular Docking Studies of Benzoxazole and Benzothiazole Derivatives
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Journal Article
Synthesis, Antifungal Activities and Molecular Docking Studies of Benzoxazole and Benzothiazole Derivatives
2018
Overview
Based on benzoxazole and benzothiazole scaffold as an important pharmacophore, two series of 2-(aryloxymethyl) benzoxazole and benzothiazole derivatives were synthesized and their antifungal effects against eight phytopathogenic fungi were evaluated. Compounds
,
,
, and
exhibited significant antifungal activities against most of the pathogens tested. Especially
,
,
,
,
, and
inhibited the growth of
with IC
of 4.34⁻17.61 μg/mL, which were stronger than that of the positive control, hymexazol (IC
of 38.92 μg/mL).
was the most potent inhibitor (IC
of 4.34 μg/mL) against
, which was about nine times more potent than hymexazol. Most of the test compounds displayed significant antifungal effects against
(IC
of 19.92⁻77.41 μg/mL), among them,
was the best one (IC
of 19.92 μg/mL). The structure-activity relationships (SARs) were compared and analyzed. The result indicates that the electron-drawing ability and position of the substituents have a significant impact on biological activities. Furthermore, docking studies were carried out on the lipid transfer protein sec14p from
, and preliminarily verified the antifungal activities. Taken together, these results provide 2-(phenoxymethyl)benzo[d]oxazole as an encouraging framework that could lead to the development of potent novel antifungal agents.
Publisher
MDPI,MDPI AG
Subject
Antifungal Agents - chemical synthesis
/ Antifungal Agents - chemistry
/ Antifungal Agents - pharmacology
/ Benzothiazoles - chemical synthesis
/ Benzothiazoles - pharmacology
/ Benzoxazoles - chemical synthesis
/ Molecular Docking Simulation
/ Saccharomyces cerevisiae - drug effects
