3238-75-3Relevant articles and documents
Chaotropic-anion-induced supramolecular self-assembly of ionic polymeric micelles
Li, Yang,Wang, Yiguang,Huang, Gang,Ma, Xinpeng,Zhou, Kejin,Gao, Jinming
, p. 8074 - 8078 (2014)
Traditional micelle self-assembly is driven by the association of hydrophobic segments of amphiphilic molecules forming distinctive core-shell nanostructures in water. Here we report a surprising chaotropic-anion-induced micellization of cationic ammonium-containing block copolymers. The resulting micelle nanoparticle consists of a large number of ion pairs (≈60 000) in each hydrophobic core. Unlike chaotropic anions (e.g. ClO4 -), kosmotropic anions (e.g. SO42-) were not able to induce micelle formation. A positive cooperativity was observed during micellization, for which only a three-fold increase in ClO4 - concentration was necessary for micelle formation, similar to our previously reported ultra-pH-responsive behavior. This unique ion-pair-containing micelle provides a useful model system to study the complex interplay of noncovalent interactions (e.g. electrostatic, van der Waals, and hydrophobic forces) during micelle self-assembly.
Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials
Dodean, Rozalia A.,Kancharla, Papireddy,Li, Yuexin,Melendez, Victor,Read, Lisa,Bane, Charles E.,Vesely, Brian,Kreishman-Deitrick, Mara,Black, Chad,Li, Qigui,Sciotti, Richard J.,Olmeda, Raul,Luong, Thu-Lan,Gaona, Heather,Potter, Brittney,Sousa, Jason,Marcsisin, Sean,Caridha, Diana,Xie, Lisa,Vuong, Chau,Zeng, Qiang,Zhang, Jing,Zhang, Ping,Lin, Hsiuling,Butler, Kirk,Roncal, Norma,Gaynor-Ohnstad, Lacy,Leed, Susan E.,Nolan, Christina,Huezo, Stephanie J.,Rasmussen, Stephanie A.,Stephens, Melissa T.,Tan, John C.,Cooper, Roland A.,Smilkstein, Martin J.,Pou, Sovitj,Winter, Rolf W.,Riscoe, Michael K.,Kelly, Jane X.
, p. 3475 - 3502 (2019/03/29)
Malaria remains one of the deadliest diseases in the world today. Novel chemoprophylactic and chemotherapeutic antimalarials are needed to support the renewed eradication agenda. We have discovered a novel antimalarial acridone chemotype with dual-stage activity against both liver-stage and blood-stage malaria. Several lead compounds generated from structural optimization of a large library of novel acridones exhibit efficacy in the following systems: (1) picomolar inhibition of in vitro Plasmodium falciparum blood-stage growth against multidrug-resistant parasites; (2) curative efficacy after oral administration in an erythrocytic Plasmodium yoelii murine malaria model; (3) prevention of in vitro Plasmodium berghei sporozoite-induced development in human hepatocytes; and (4) protection of in vivo P. berghei sporozoite-induced infection in mice. This study offers the first account of liver-stage antimalarial activity in an acridone chemotype. Details of the design, chemistry, structure-activity relationships, safety, metabolic/pharmacokinetic studies, and mechanistic investigation are presented herein.
LIBRARY OF PH RESPONSIVE POLYMERS AND NANOPROBES THEREOF
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Page/Page column 59; 60, (2016/01/16)
The present disclosure relates to polymers which contain a hydrophobic and hydrophilic segment which is sensitive to pH. In some aspects, the polymers form a micelle which is sensitive to pH and results in a change in fluorescence based upon the particular pH. In some aspects, the disclosure also provides methods of using the polymers for the imaging of cellular or extracellular environment or delivering a drug.
