Discovery of novel indole and indoline derivatives against Candida albicans as potent antifungal agents.

Bioorg Med Chem Lett

College of Chinese Materia Medica, Yunnan University of Chinese Medicine, Kunming 650500, PR China; Engineering Laboratory for National Health Theory and Product of Yunnan Province, Yunnan University of Chinese Medicine, Kunming 650500, PR China; College of Pharmacy, Dali University, Dali 671000, PR China. Electronic address:

Published: September 2022

With the widespread use of azole antifungals in the clinic, the drug resistance has been emerging continuously. In this work, we have designed and prepared a series of novel indole and indoline derivatives, and in vitro antifungal activity against C. albicans were evaluated. The results showed that title compounds exhibited good antifungal effect on Azole-resistant C. albicans. Further mechanism study demonstrated that S18 could inhibit the biofilm formation and hyphae growth of C. albicans through the Ras-cAMP-PKA signaling pathway.

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Source
http://dx.doi.org/10.1016/j.bmcl.2022.128826DOI Listing

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