Further SAR on the (phenylsulfonyl)piperazine scaffold as inhibitors of the  Aedes aegypti Kir1 (AeKir) channel and larvicides.

Further SAR on the (phenylsulfonyl)piperazine scaffold as inhibitors of the Aedes aegypti Kir1 (AeKir) channel and larvicides. ChemMedChem. 2020 Sep 14;: Authors: Aretz C, Kharade SV, Chronister K, Trigueros RR, Rodriguez EM, Piermarini PM, Denton JS, Hopkins CR Abstract Zika virus (ZIKV), dengue fever (DENV) and chikungunya (CHIKV) are arboviruses that are spread to humans from the bite of an infected adult female  Aedes aegypti  mosquito. As there are no effective vaccines or therapeutics for these diseases, the primary strategy for controlling the spread of these viruses is to prevent the mosquito from biting humans through the use of insecticides. Unfortunately, the commonly used classes of insecticides have seen a significant increase in resistance, thus complicating control efforts. Inhibiting the renal inward rectifier potassium (Kir) channel of the mosquito vector  Aedes aegypti  has been shown to be a promising target for the development of novel mosquitocides. We have shown that Kir1 channels play key roles in mosquito diuresis, hemolymph potassium homeostasis, flight, and reproduction. Previous work from our laboratories identified a novel (phenylsulfonyl)piperazine scaffold as potent  Ae Kir channel inhibitors with activity against both adult and larval mosquitoes. Herein, we report further SAR work around this scaffold and have identified additional compounds with improved  in vitro  potency and mosquito larvae ...
Source: ChemMedChem - Category: Chemistry Authors: Tags: ChemMedChem Source Type: research