Synthesis and antileishmanial evaluation of 1-aryl-4-(4, 5-dihydro-1H-imidazol-2-yl)-1H-pyrazole derivatives

…, LL Leon, MM Canto-Cavalheiro

Index: Dos Santos, Mauricio S.; Oliveira, Mariana L.V.; Bernardino, Alice M.R.; De Leo, Rosa M.; Amaral, Veronica F.; De Carvalho, Flavia T.; Leon, Leonor L.; Canto-Cavalheiro, Marilene M. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 24 p. 7451 - 7454

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Citation Number: 18

Abstract

A series of 1-aryl-4-(4, 5-dihydro-1H-imidazol-2-yl)-1H-pyrazoles (4a–g) and 5-amino-1-aryl- 4-(4, 5-dihydro-1H-imidazol-2-yl)-1H-pyrazoles (5a–g) were synthesized and evaluated in vitro against three Leishmania species: L. amazonensis, L. braziliensis and L. infantum (L. chagasi syn.). The cytotoxicity was assessed. Among the derivatives examined, six compounds emerged as the most active on promastigotes forms of L. amazonensis with ...