Document Detail

Effect of functional group polarity on the antimalarial activity of spiro and dispiro-1,2,4-trioxolanes.
MedLine Citation:
PMID:  16759871     Owner:  NLM     Status:  MEDLINE    
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 LogP/LogD) lead compounds with good physicochemical properties. More lipophilic trioxolanes tended to have better oral activities than their more polar counterparts. Trioxolanes with a wide range of neutral and basic, but not acidic, functional groups had good antimalarial profiles.
Yuxiang Dong; Yuanqing Tang; Jacques Chollet; Hugues Matile; Sergio Wittlin; Susan A Charman; William N Charman; Josefina Santo Tomas; Christian Scheurer; Christopher Snyder; Bernard Scorneaux; Saroj Bajpai; Scott A Alexander; Xiaofang Wang; Maniyan Padmanilayam; Srinivasa R Cheruku; Reto Brun; Jonathan L Vennerstrom
Publication Detail:
Type:  In Vitro; Journal Article; Research Support, Non-U.S. Gov't     Date:  2006-06-08
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  14     ISSN:  0968-0896     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2006 Sep 
Date Detail:
Created Date:  2006-08-21     Completed Date:  2006-11-07     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  6368-82     Citation Subset:  IM    
College of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, NE, USA.
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MeSH Terms
Antimalarials / chemical synthesis,  chemistry,  pharmacology*
Heterocyclic Compounds / chemical synthesis,  chemistry,  pharmacology*
Molecular Conformation
Parasitic Sensitivity Tests
Spiro Compounds / chemical synthesis,  chemistry,  pharmacology*
Structure-Activity Relationship
Reg. No./Substance:
0/1,2,4-trioxane; 0/Antimalarials; 0/Heterocyclic Compounds; 0/Spiro Compounds

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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