Antimalarial activity of N-alkyl amine, carboxamide, sulfonamide, and urea derivatives of a dispiro-1,2,4-trioxolane piperidine |
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Authors: | Padmanilayam Maniyan Scorneaux Bernard Dong Yuxiang Chollet Jacques Matile Hugues Charman Susan A Creek Darren J Charman William N Tomas Josefina Santo Scheurer Christian Wittlin Sergio Brun Reto Vennerstrom Jonathan L |
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Institution: | College of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, NE, USA. |
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Abstract: | With an aim to identify a dispiro-1,2,4-trioxolane with high oral activity and good physicochemical properties, 27 derivatives of an achiral piperidine trioxolane were synthesized; most were potent antimalarial peroxides with IC(50)s ranging from 0.20 to 7.0 ng/mL. The oral efficacies of two of these were superior to artesunate and comparable to artemether. The attractive chemical simplicity of these compounds is balanced only by an apparent metabolic susceptibility. |
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