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

Continuing with our efforts to identify new active compounds against malaria and leishmaniasis, fourteen 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 Colombi...

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Authors: Barea, C. (Carlos)|||/items/4f4c9d7c-4235-491b-9444-7a90d51c223d, Pabon, A. (Adriana)|||/items/49b4dd33-b935-4fa8-bfc7-8bb9e2a92b49, Castillo, D. (Denis)|||/items/da7db44a-be7c-4086-8577-76d1c575032b, Zimic, M. (Mirko)|||/items/d2142c18-4e12-4c11-910b-bef72d385f87, Quiliano, M. (Miguel)|||/items/444a2441-d79f-422b-8714-437e2a763195, Galiano, S. (Silvia)|||/items/10b9d373-6e6e-46e4-bfae-e7b241dad5fd, Pérez-Silanes, S. (Silvia)|||/items/e5734c65-2dd8-4fdd-a74a-fc7526136c45, Monge, A. (Antonio)|||/items/804a350e-c7ff-4318-9742-cdc3432eb2a8, Deharo, E. (Eric)|||/items/48bf3a09-fa0f-4898-8f39-dce9f0fcdef9, Aldana, I. (Ignacio)|||/items/2a317afc-d6ab-4970-8bac-41d9715f5618
Format: article
Publication Date:2011
Country:España
Institution:Universidad de Navarra
Repository:Dadun. Depósito Académico Digital de la Universidad de Navarra
Language:English
OAI Identifier:oai:dadun.unav.edu:10171/23742
Online Access:https://hdl.handle.net/10171/23742
Access Level:Open access
Keyword:Quinoxaline
N-oxides
Malaria
Leishmaniasis
Description
Summary:Continuing with our efforts to identify new active compounds against malaria and leishmaniasis, fourteen 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

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