RT Journal Article
T1 Study of a selected series of 3- and 4-Arylcoumarins as antifungal agents against Dermatophytic Fungi: T. rubrum and T. mentagrophytes
A1 López Cisneros, Carmen Lucía
A1 Cazar Ramírez, María Elena
A1 Bailón Moscoso, Natalia
A1 Guardado Yordi, Estela
A1 Borges, Fernanda
A1 Uriarte Villares, Eugenio
A1 Matos, Maria João
K1 Antifungalagents
K1 Arylcoumarins
K1 Heterocycles
K1 Synthesis
AB The main etiological agents in dermatophytosis of human skin and nails are Trichophyton, in particular Trichophyton rubrum (T. rubrum) and Trichophyton mentagrophytes (T. mentagrophytes). A new series of twenty-three 3- and 4-arylcoumarins was synthesized and the antifungal activities against clinical isolates of T. rubrum and T. mentagrophytes were evaluated. Sixteen out of twenty-three molecules exhibited antifungal activity against one or both fungi strains. In some cases, the activity against T. rubrum has been comparable to fluconazole, one of the standards, being 8-methoxy-3-(4’-nitrophenyl)coumarin (16) the best compound within this series (minimum inhibitory concentration, MIC=6.25 μg/mL). The preliminary structure-activity relationship study showed that the antifungal activity depends on the position and nature of the substitution patterns. The cytotoxicity of eleven compounds on D-384 (astrocytoma), A-549 (lung cancer) and RKO (colorectal cancer) cell lines was also performed. With the aim of deeply understand the potential of these molecules as hits to develop new drugs, the theoretical absorption, distribution, metabolism and excretion (ADME) properties of the active compounds were calculated
PB Wiley
YR 2021
FD 2021
LK http://hdl.handle.net/10347/29064
UL http://hdl.handle.net/10347/29064
LA eng
NO ChemistrySelect2021,6, 9981–998. https://doi.org/10.1002/slct.202103099
NO MJM thanks Xunta de Galicia (Galician Plan of Research, Innovation and Growth 2011–2015, Plan I2 C, Grants ED481B 2014/086-0 and ED481B 2018/007), Ministerio de Ciencia e Innovación (PID2020-116076RJ−I00/AEI/10.13039/501100011033) and Fundação para a Ciência e Tecnologia (FCT, CEECIND/02423/2018 and UIDB/00081/2020)
DS Minerva
RD 24 abr 2026