TY - JOUR
T1 - Synthesis and in vitro evaluation of new ethyl and methyl quinoxaline-7-carboxylate 1,4-di-N-oxide against Entamoeba histolytica
AU - Duque-Montaño, Blanca Estela
AU - Gómez-Caro, Lilia Citlalli
AU - Sanchez-Sanchez, Mario
AU - Monge, Antonio
AU - Hernández-Baltazar, Efrén
AU - Rivera, Gildardo
AU - Torres-Angeles, Oscar
N1 - Funding Information:
Blanca Estela Duque Montaño is the recipient of a scholarship (No. 208856 ) from CONACyT México . The authors are thankful to Dra. Mireya de la Garza for her donation of the Entamoeba histolytica strain HM1:IMSS. We wish to express our gratitude to CONACYT (CB-2010-01, clave 0157358) and the Instituto Politecnico Nacional (SIP-IPN, Mexico) for their financial support. Gildardo Rivera holds a scholarship from the Comision de Operacion y Fomento de Actividades Academicas (COFAA-IPN). All participants declare no conflict of interest.
PY - 2013/8/1
Y1 - 2013/8/1
N2 - In our search for new antiamoebic agents, a new series of ethyl and methyl quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives have been synthesized using the Beirut reaction. All compounds were characterized by spectroscopic techniques and elemental analysis. Antiamoebic activity was evaluated in vitro against Entamoeba histolytica strain HM1:IMSS by the microdilution method, and the structure-activity relationship was analyzed. We found that eleven quinoxaline derivatives showed greater activity than metronidazole and nitazoxanide with IC50 values in the range 1.99-0.35 μM. Compounds T-001 and T-016 shows IC50 values of 1.41 and 1.47 μM, respectively, with a value of selectivity index >60.
AB - In our search for new antiamoebic agents, a new series of ethyl and methyl quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives have been synthesized using the Beirut reaction. All compounds were characterized by spectroscopic techniques and elemental analysis. Antiamoebic activity was evaluated in vitro against Entamoeba histolytica strain HM1:IMSS by the microdilution method, and the structure-activity relationship was analyzed. We found that eleven quinoxaline derivatives showed greater activity than metronidazole and nitazoxanide with IC50 values in the range 1.99-0.35 μM. Compounds T-001 and T-016 shows IC50 values of 1.41 and 1.47 μM, respectively, with a value of selectivity index >60.
KW - Antiamoebic activity
KW - Antiparasitic agents
KW - Cytotoxicity
KW - Quinoxaline 1,4-di-N-oxide
UR - http://www.scopus.com/inward/record.url?scp=84879685294&partnerID=8YFLogxK
U2 - 10.1016/j.bmc.2013.05.036
DO - 10.1016/j.bmc.2013.05.036
M3 - Artículo
SN - 0968-0896
VL - 21
SP - 4550
EP - 4558
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
IS - 15
ER -