| 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. |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| 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
Previous Document: Relationship between the lipophilicity of gallic acid n-alquil esters' derivatives and both myeloper...
Next Document: C19-steroids as androgen receptor modulators: design, discovery, and structure-activity relationship...