| Hazard Information | Back Directory | [Description]
BRD7539B is a Dihydroorotate dehydrogenase (DHODH) inhibitor . RD7539 had shown to target PfDHODH (IC50 = 0.033 μM) selectively over human (Hs) DHODH (IC50 > 50 μM). BRD7539 was reported to have potent activity against both multidrug-resistant asexual blood-stage (P. falciparum, Dd2_x000D_
strain, EC50 = 0.010 μM) and liver-stage (P. berghei, EC50 =0.015 μM) parasites but no activity against sexual blood-stage (P. falciparum, stages IV?V, EC50 > 20 μM) parasites. BRD7539 is an azetidine carbonitrile with three contiguous stereocenters (2S,3S,4S), and stereochemistry-based structure?_x000D_
activity relationships (SSARs) showed that only two of eight possible stereoisomers are active. | [Uses]
BRD7539 is a PfDHODH inhibitor (IC50 = 0.033 μM). BRD7539 has potent activity against both multidrug-resistant asexual blood-stage (P. falciparum, Dd2 strain, EC50 = 0.010 μM) and liver-stage (P. berghei, EC50 = 0.015 μM) parasites[1]. | [References]
[1] Maetani M, et al. Discovery of Antimalarial Azetidine-2-carbonitriles That Inhibit P. falciparum Dihydroorotate Dehydrogenase. ACS Med Chem Lett. 2017 Feb 27;8(4):438-442. DOI:10.1021/acsmedchemlett.7b00030 |
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