Effect of functional group polarity on the antimalarial activity of spiro and dispiro-1,2,4-trioxolanes

Based on the structures of several lipophilic trioxolane antimalarial prototypes, we set out to determine which functional groups were associated with good antimalarial profiles and identify more polar (lower Log P/Log D) lead compounds with good physicochemical properties. More lipophilic trioxolan...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2006-09, Vol.14 (18), p.6368-6382
Hauptverfasser:	Dong, Yuxiang, Tang, Yuanqing, Chollet, Jacques, Matile, Hugues, Wittlin, Sergio, Charman, Susan A., Charman, William N., Tomas, Josefina Santo, Scheurer, Christian, Snyder, Christopher, Scorneaux, Bernard, Bajpai, Saroj, Alexander, Scott A., Wang, Xiaofang, Padmanilayam, Maniyan, Cheruku, Srinivasa R., Brun, Reto, Vennerstrom, Jonathan L.
Format:	Artikel
Sprache:	eng
Schlagworte:	1,2,4-Trioxolane Antibiotics. Antiinfectious agents. Antiparasitic agents Antimalarial Antimalarials - chemical synthesis Antimalarials - chemistry Antimalarials - pharmacology Antiparasitic agents Artemisinin Biological and medical sciences Heterocyclic Compounds - chemical synthesis Heterocyclic Compounds - chemistry Heterocyclic Compounds - pharmacology In Vitro Techniques Medical sciences Molecular Conformation Parasitic Sensitivity Tests Pharmacology. Drug treatments Secondary ozonide Spiro Compounds - chemical synthesis Spiro Compounds - chemistry Spiro Compounds - pharmacology Stereoisomerism Structure-Activity Relationship
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