Antifungal, cytotoxic and SAR studies of a series of N-alkyl, N-aryl and N-alkylphenyl-1, 4-pyrrolediones and related compounds

…, F Garibotto, V Cechinel Filho, M Gupta, R Enriz…

Index: Sortino; Garibotto; Cechinel Filho; Gupta; Enriz; Zacchino Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 9 p. 2823 - 2834

Full Text: HTML

Citation Number: 26

Abstract

Abstract The synthesis, in vitro evaluation and SAR studies of 67 maleimides and derivatives acting as antifungal agents are reported. A detailed SAR study supported by theoretical calculations led us to determine that: an intact maleimido ring appears to be necessary for a strong antifungal activity, dissimilarly affected by the substituents in positions 2 and 3. The best activities were shown by 2, 3-nonsubstituted followed by 2, 3 dichloro-and 2-methyl- ...