Science and Technology Production
Article
Authorship
Vladimir V. Kouznetsov
;
Leonor Y. Vargas
;
SORTINO, MAXIMILIANO ANDRES
;
Yelkaira Vázquez
;
Mahabir Gupta
;
Ricardo D. Enriz
;
Susana A. Zacchino
Date
2008
Publishing House and Editing Place
Elsevier
Magazine
BIOORGANIC & MEDICINAL CHEMISTRY.,
vol. 16
(pp. 794-809)
Elsevier
Summary
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SIGEVA
Diverse N-substituted anilines bearing hetaryl fragments were easily prepared from corresponding aldimines derived fromcommercially available aromatic aldehydes and anilines. 2-Furyl substituted anilines showed very good antifungal activities againstdermatophytes, particularly against Trichophyton rubrum (MIC = 3.12–6.25 lg/mL). In addition, all active compounds, 45–47, 73,and 74, were tested for cytotoxic activities against breast (MCF-7), lung (H-460), and central nervous system (...
Diverse N-substituted anilines bearing hetaryl fragments were easily prepared from corresponding aldimines derived fromcommercially available aromatic aldehydes and anilines. 2-Furyl substituted anilines showed very good antifungal activities againstdermatophytes, particularly against Trichophyton rubrum (MIC = 3.12–6.25 lg/mL). In addition, all active compounds, 45–47, 73,and 74, were tested for cytotoxic activities against breast (MCF-7), lung (H-460), and central nervous system (SF-268) human cancercell lines with the NCI-anticancer-drug screen. The activity of amines described in this paper, along with the low toxicity of most ofthem, shows promise for the future development of non-toxic new antimycotic agents.
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Key Words
N-substituted aniline derivatives;Antifungal and cytotoxic properties;Synthesis;N-Aryl-N-[1-(heteroyl)but-3-enyl]amines;N-(Hetarylmethyl)anilines;SAR