2. Academic Validation
  3. Dispiropyrrolidine tethered piperidone heterocyclic hybrids with broad-spectrum antifungal activity against Candida albicans and Cryptococcus neoformans

Dispiropyrrolidine tethered piperidone heterocyclic hybrids with broad-spectrum antifungal activity against Candida albicans and Cryptococcus neoformans

  • Bioorg Chem. 2020 Jul;100:103865. doi: 10.1016/j.bioorg.2020.103865.
Sarah Lawson 1,  Natarajan Arumugam 2,  Abdulrahman I Almansour 3,  Raju Suresh Kumar 3,  Shankar Thangamani 4
Affiliations

Affiliations

  • 1 Arizona College of Osteopathic Medicine, Midwestern University, 19555 N. 59th Ave., Glendale, AZ 85308, USA.
  • 2 Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia. Electronic address: anatarajan@ksu.edu.sa.
  • 3 Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.
  • 4 Department of Pathology and Population Medicine, College of Veterinary Medicine, Midwestern University, 19555 N. 59th Ave., Glendale, AZ 85308, USA. Electronic address: sthang@midwestern.edu.
PMID: 32361055 DOI: 10.1016/j.bioorg.2020.103865
Abstract

Invasive Fungal infections along with rising incidence of resistance to Antifungal drugs pose increasing threat to immunocompromised individuals, including Cancer patients. In this study, we examined the Antifungal activity of dispiropyrrolidine tethered piperidone heterocyclic hybrids. Results indicate that compounds 5a and 6i have demonstrated a potent Antifungal effect on multiple Fungal strains, including Candida albicans, without exhibiting cytotoxicity to mammalian cells. Furthermore, these two compounds exhibited significant inhibition on Candida albicans hyphae and biofilm development that surpasses the FDA-approved Antifungal drug currently used for treatment. Taken together, our results suggest that 5a and 6i are promising candidates for development into new Antifungal drugs.

Keywords

Antifungal agent; Dispiropyrrolidine; Domino multicomponent reaction; Ionic liquids; Toxicity.

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