Weak base dispiro-1,2,4-trioxolanes: potent antimalarial ozonides |
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| Authors: | Tang Yuanqing Dong Yuxiang Wittlin Sergio Charman Susan A Chollet Jacques Chiu Francis C K Charman William N Matile Hugues Urwyler Heinrich Dorn Arnulf Bajpai Saroj Wang Xiaofang Padmanilayam Maniyan Karle Jean M 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: | Thirty weak base 1,2,4-dispiro trioxolanes (secondary ozonides) were synthesized. Amino amide trioxolanes had the best combination of antimalarial and biopharmaceutical properties. Guanidine, aminoxy, and amino acid trioxolanes had poor antimalarial activity. Lipophilic trioxolanes were less stable metabolically than their more polar counterparts. |
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