An article Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials WOS:000464768300020 published article about PLASMODIUM-BERGHEI; CATALYZED AMINATION; CYTOCHROME-B; LIVER-STAGE; MALARIA; VIVAX; CHALLENGES; RESISTANT; PROPHYLAXIS; MUTATIONS in [Dodean, Rozalia A.; Kancharla, Papireddy; Li, Yuexin; Winter, Rolf W.; Riscoe, Michael K.; Kelly, Jane X.] Portland State Univ, Dept Chem, Portland, OR 97201 USA; [Dodean, Rozalia A.; Li, Yuexin; Smilkstein, Martin J.; Pou, Sovitj; Winter, Rolf W.; Riscoe, Michael K.; Kelly, Jane X.] Dept Vet Affairs Med Ctr, Portland, OR 97239 USA; [Melendez, Victor; Read, Lisa; Bane, Charles E.; Vesely, Brian; Kreishman-Deitrick, Mara; Black, Chad; Li, Qigui; Sciotti, Richard J.; Olmeda, Raul; Thu-Lan Luong; 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] Walter Reed Army Inst Res, Div Expt Therapeut, Silver Spring, MD 20910 USA; [Huezo, Stephanie J.; Rasmussen, Stephanie A.; Cooper, Roland A.] Dominican Univ Calif, Dept Nat Sci & Math, San Rafael, CA 94901 USA; [Stephens, Melissa T.; Tan, John C.] Univ Notre Dame, Genom Core Facil, Notre Dame, IN 46556 USA; [Tan, John C.] Univ Notre Dame, Eck Inst Global Hlth, Notre Dame, IN 46556 USA in 2019, Cited 53. The Name is 2,4-Dichlorobenzoic acid. Through research, I have a further understanding and discovery of 50-84-0. Recommanded Product: 2,4-Dichlorobenzoic acid
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.
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Chloride – Wikipedia,
,Chlorides – an overview | ScienceDirect Topics