弱碱双环-1,2,4-三氧杂环戊烷：高效抗疟臭氧化物。
Weak base dispiro-1,2,4-trioxolanes: potent antimalarial ozonides.
作者信息
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
机构信息
College of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, NE, USA.
出版信息
Bioorg Med Chem Lett. 2007 Mar 1;17(5):1260-5. doi: 10.1016/j.bmcl.2006.12.007. Epub 2006 Dec 15.
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.
合成了30种弱碱1,2,4-二螺三氧杂环戊烷（二级臭氧化物）。氨基酰胺三氧杂环戊烷在抗疟和生物制药特性方面具有最佳组合。胍基、氨氧基和氨基酸三氧杂环戊烷的抗疟活性较差。亲脂性三氧杂环戊烷在代谢上比极性更强的同类物更不稳定。
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