Synthesis and pharmacological evaluation of childinin E and several derivatives as anti-hyphal formation inhibitors against Candida albicans

[Display omitted] •The first total synthesis of childinin E was achieved from the commercial benzaldehyde.•Five benzophenone derivatives were obtained by using the synthetic route of childinin E.•The antifungal properties of the synthesized compounds against Candida albicans were evaluated by an ant...

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Bibliographic Details
Published in:Tetrahedron letters 2020-12, Vol.61 (49), p.152588, Article 152588
Main Authors: Kamauchi, Hitoshi, Hirata, Momoka, Takao, Koichi, Sugita, Yoshiaki
Format: Article
Language:English
Subjects:
Benzophenone
Candida albicans
Daldinia spp
Hyphal formation
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Summary:[Display omitted] •The first total synthesis of childinin E was achieved from the commercial benzaldehyde.•Five benzophenone derivatives were obtained by using the synthetic route of childinin E.•The antifungal properties of the synthesized compounds against Candida albicans were evaluated by an anti- hyphal formation test.•Anti-hyphal formation activity of benzophenone derivatives was evaluated.•Childnin E and two derivatives exhibited anti-hyphal formation activity. The natural highly substituted benzophenone childinin E (1) was previously isolated from the fungus Daldinia childiae. Here we describe the total synthesis of childinin E and several derivatives using a linear seven-step sequence. The antifungal properties of the synthesized compounds against Candida albicans were evaluated by an anti-hyphal formation test. Childnin E and two derivatives exhibited anti-hyphal formation activity.
ISSN:0040-4039
1873-3581
DOI:10.1016/j.tetlet.2020.152588