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    
Abstract/OtherAbstract:
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.
Authors:
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    
Affiliation:
College of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, NE, USA.
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MeSH Terms
Descriptor/Qualifier:
Antimalarials / chemical synthesis,  chemistry,  pharmacology*
Heterocyclic Compounds / chemical synthesis,  chemistry,  pharmacology*
Molecular Conformation
Parasitic Sensitivity Tests
Spiro Compounds / chemical synthesis,  chemistry,  pharmacology*
Stereoisomerism
Structure-Activity Relationship
Chemical
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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