Bioorganic & Medicinal Chemistry 2011-11-15

Thiosemicarbazones derived from 1-indanones as new anti-Trypanosoma cruzi agents.

María E Caputto, Lucas E Fabian, Diego Benítez, Alicia Merlino, Natalia Ríos, Hugo Cerecetto, Graciela Y Moltrasio, Albertina G Moglioni, Mercedes González, Liliana M Finkielsztein

Index: Bioorg. Med. Chem. 19(22) , 6818-26, (2011)

Full Text: HTML

Abstract

In the present work, we synthesized a series of thiosemicarbazones derived from 1-indanones with good anti-Trypanosoma cruzi activity. Most of them displayed remarkable trypanosomicidal activity. All the compounds showed nonspecific cytotoxicity on human erythrocytes. The ability of the new compounds to inhibit cruzipain, the major cysteine protease of T. cruzi, was also explored. Thiosemicarbazones 12 and 24 inhibited this enzyme at the dose assayed. This interaction was also studied in terms of molecular docking.Copyright © 2011 Elsevier Ltd. All rights reserved.