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ACS Infect Dis ; 5(6): 917-931, 2019 06 14.
Artículo en Inglés | MEDLINE | ID: mdl-30832472

RESUMEN

Mosquito-borne arboviral diseases such as Zika, dengue fever, and chikungunya are transmitted to humans by infected adult female Aedes aegypti mosquitoes and affect a large portion of the world's population. The Kir1 channel in Ae. aegypti ( AeKir1) is an important ion channel in the functioning of mosquito Malpighian (renal) tubules and one that can be manipulated in order to disrupt excretory functions in mosquitoes. We have previously reported the discovery of various scaffolds that are active against the AeKir1 channel. Herein we report the synthesis and biological characterization of a new 2-nitro-5-(4-(phenylsulfonyl) piperazin-1-yl)- N-(pyridin-4-ylmethyl)anilines scaffold as inhibitors of AeKir1. This new scaffold is more potent in vitro compared to the previously reported scaffolds, and the molecules kill mosquito larvae.


Asunto(s)
Aedes/efectos de los fármacos , Compuestos de Anilina/síntesis química , Compuestos de Anilina/farmacología , Proteínas de Insectos/antagonistas & inhibidores , Piperazinas/síntesis química , Piperazinas/farmacología , Canales de Potasio de Rectificación Interna/antagonistas & inhibidores , Animales , Femenino , Ensayos Analíticos de Alto Rendimiento , Larva/efectos de los fármacos , Sulfonamidas/química
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