Weak base dispiro-1,2,4-trioxolanes: Potent antimalarial ozonides

被引：53

作者：

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：

[1] Univ Nebraska, Med Ctr, Coll Pharm, Omaha, NE 68182 USA

[2] Swiss Trop Inst, CH-4002 Basel, Switzerland

[3] Monash Univ, Victorian Coll Pharm, Parkville, Vic 3052, Australia

[4] F Hoffmann La Roche & Co Ltd, CH-4070 Basel, Switzerland

[5] Basilea Pharmaceut Ltd, CH-4058 Basel, Switzerland

[6] Walter Reed Army Med Ctr, Walter Reed Army Inst Res, Div Expt Therapeut, Washington, DC 20307 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 05期

关键词：

1,2,4-trioxolanes; secondary ozonides; antimalarial; peroxide; artemisinin;

D O I：

10.1016/j.bmcl.2006.12.007

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：1260 / 1265

页数：6

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