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Dispiropyrrolidine tethered piperidone heterocyclic hybrids with broad-spectrum antifungal activity against Candida albicans and Cryptococcus neoformans.
Lawson, Sarah; Arumugam, Natarajan; Almansour, Abdulrahman I; Suresh Kumar, Raju; Thangamani, Shankar.
Afiliação
  • Lawson S; Arizona College of Osteopathic Medicine, Midwestern University, 19555 N. 59th Ave., Glendale, AZ 85308, USA.
  • Arumugam N; Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia. Electronic address: anatarajan@ksu.edu.sa.
  • Almansour AI; Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.
  • Suresh Kumar R; Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.
  • Thangamani S; 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.
Bioorg Chem ; 100: 103865, 2020 07.
Article em En | MEDLINE | ID: mdl-32361055
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.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piperidonas / Candida albicans / Cryptococcus neoformans / Antifúngicos Limite: Humans Idioma: En Revista: Bioorg Chem Ano de publicação: 2020 Tipo de documento: Article País de afiliação: Estados Unidos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piperidonas / Candida albicans / Cryptococcus neoformans / Antifúngicos Limite: Humans Idioma: En Revista: Bioorg Chem Ano de publicação: 2020 Tipo de documento: Article País de afiliação: Estados Unidos