Bioorganic & Medicinal Chemistry Letters 2011-08-01

New salicylamide and sulfonamide derivatives of quinoxaline 1,4-di-N-oxide with antileishmanial and antimalarial activities.

Carlos Barea, Adriana Pabón, Denis Castillo, Mirko Zimic, Miguel Quiliano, Silvia Galiano, Silvia Pérez-Silanes, Antonio Monge, Eric Deharo, Ignacio Aldana

Index: Bioorg. Med. Chem. Lett. 21(15) , 4498-502, (2011)

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Abstract

Continuing with our efforts to identify new active compounds against malaria and leishmaniasis, 14 new 3-amino-1,4-di-N-oxide quinoxaline-2-carbonitrile derivatives were synthesized and evaluated for their in vitro antimalarial and antileishmanial activity against Plasmodium falciparum Colombian FCR-3 strain and Leishmania amazonensis strain MHOM/BR/76/LTB-012A. Further computational studies were carried out in order to analyze graphic SAR and ADME properties. The results obtained indicate that compounds with one halogenous group substituted in position 6 and 7 provide an efficient approach for further development of antimalarial and antileishmanial agents. In addition, interesting ADME properties were found.Copyright © 2011 Elsevier Ltd. All rights reserved.