RT Journal Article
T1 Synthesis, antibacterial and antifungal activities of naphthoquinone derivatives: a structure-activity relationship study
A1 Sanchez-Calvo, Juan M.
A1 Barbero, Gara R.
A1 Guerrero-Vasquez, Guillermo
A1 Duran, Alexandra G.
A1 Macias, Mariola
A1 Rodriguez-Iglesias, Manuel A.
A1 Molinillo, Jose M. G.
A1 Macias, Francisco A.
K1 Naphthoquinone
K1 Antifungal
K1 Antibacterial
K1 Minimum inhibitory concentration
K1 Structure-activity relationship
K1 Biological evaluation
K1 1,4-naphthoquinone derivatives
K1 Potent antifungal
K1 Agents
K1 Naphthopurpurin
K1 Naphthazarins
K1 Inhibition
K1 Anticancer
K1 Quinones
K1 Juglone
AB The synthesis of 1,4-naphthoquinone derivatives is of great interest since these compounds exhibit strong activity as antimalarial, antibacterial, antifungal and anticancer agents. A series of 50 naphthoquinone derivatives was synthesized and evaluated for antibacterial and antifungal activity against Escherichia coli, Pseudomonas aeruginosa, Enterococcus faecalis, Staphylococcus aureus, Candida krusei, Candida parapsilosis and Cryptococcus neoformans using the broth microdilution method. The Candida species were the most susceptible microorganisms. Halogen derivatives of 1,4-naphthoquinone presented strong activity, e.g., 2-bromo-5-hydroxy-1,4-naphthoquinone, which exhibited inhibition at an MIC of 16 A mu g/mL in S. aureus, and 2-chloro-5,8-dihydroxy-1,4-naphthoquinone, with an MIC of 2 A mu g/mL in C. krusei. These compounds showed higher activity against fungi, but the antibacterial activities were very low. The study of structure-activity relationships is very important in the search for new antimicrobial drugs due to the limited therapeutic arsenal.
PB Springer birkhauser
SN 1054-2523
YR 2016
FD 2016-06-01
LK http://hdl.handle.net/10668/18620
UL http://hdl.handle.net/10668/18620
LA en
DS RISalud
RD Apr 9, 2025