TITLE:
Synthesis and Trypanocidal Evaluation of Some Novel 2-(Substituted Benzylidene)-5, 7-Dibromo-6-Hydroxy-1-Benzofuran-3(2H)-Ones
AUTHORS:
K. L. Ameta, Nitu S. Rathore, Biresh Kumar, Edith S. Malaga M, Manuela Verastegui P, Robert H. Gilman, B. L. Verma
KEYWORDS:
Chalcones; Aurones; Trypanosoma cruzi; Chagas Disease; Inhibition
JOURNAL NAME:
International Journal of Organic Chemistry,
Vol.2 No.3A,
November
29,
2012
ABSTRACT: Substituted 2-benzylidene-1-benzofuran-3-ones are commonly known as aurones. This class of bioactive heterocycles belongs to flavonoid family. The article intends to put forth the rational design and synthesis of a new series of aurones using 3’,5’-dibromo-2’,4’-dihydroxychalcones and copper bromide in presence of DMF-water mixture (8:2, v/v) for the first time. Preliminary bioassay shows that most of compounds have good trypanocidal activity against Trypanosoma cruzi at 10 μg/mL. Few compounds are equally potent to the standard drugs Benznidazole and Nifurtimox. The structures of the newly synthesized products 2a-n were established by elemental analysis, FTIR, 1H NMR, 13C NMR and mass spectroscopic studies.