2. Academic Validation
  3. Synthesis and antifungal evaluation of phenol-derived bis(indolyl)methanes combined with FLC against Candida albicans

Synthesis and antifungal evaluation of phenol-derived bis(indolyl)methanes combined with FLC against Candida albicans

  • Bioorg Med Chem Lett. 2022 Feb 15;58:128525. doi: 10.1016/j.bmcl.2022.128525.
Yuan Jiang 1,  Liuqing Su 1,  Yichuan Liao 1,  Yunhong Shen 1,  Hui Gao 1,  Yi Zhang 1,  Ruirui Wang 2,  Zewei Mao 3
Affiliations

Affiliations

  • 1 School of Chinese Materia Medica, Yunnan University of Chinese Medicine, Kunming 650500, PR China.
  • 2 School of Chinese Materia Medica, Yunnan University of Chinese Medicine, Kunming 650500, PR China. Electronic address: [email protected].
  • 3 School of Chinese Materia Medica, Yunnan University of Chinese Medicine, Kunming 650500, PR China. Electronic address: [email protected].
PMID: 34998904 DOI: 10.1016/j.bmcl.2022.128525
Abstract

With the widespread use of azole antifungals in the clinic, the drug resistance has been emerging continuously. In this work, we focus on boron trifluoride etherate catalyzed condensation of indole and salicylaldehydes to form bis(indolyl)methanes (BIMs) in high yields, and in vitro Antifungal activity against Candida albicans were evaluated. The results showed that most phenol-derived BIMs combined with fluconazole (FLC) exhibited good Antifungal activity against sensitive and drug-resistant C. albicans. Further mechanism study demonstrated that BI-10 combined with FLC could inhibit hyphal growth, result in ROS accumulation, and decrease mitochondrial membrane potential (MMP) as well as altering membrane permeability.

Keywords

Antifungal activity; BF(3)•Et(2)O catalyzed synthesis; Bis(indolyl)methanes; Mechanistic studies.

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Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-145873
    Antifungal Agent