Document Detail


Efficient synthesis of the first betulonic acid-acetylene hybrids and their hepatoprotective and anti-inflammatory activity.
MedLine Citation:
PMID:  19524443     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The Sonogashira reaction can be applied for the preparation of acetylenic derivatives of betulonic acid where the triterpenoid moiety can serve as either the halo- or the acetylenic component. This reaction opened access to the first derivatives of betulonic acid containing either the arylethynyl (C[triple bond]C-Ar(Het) or the ethynyl (C[triple bond]CH) moieties. From the fundamental perspective, this work illustrates the possibility of selective Pd-catalyzed cross-coupling at terminal acetylenes in the presence of a terminal alkene. Hepatoprotective and anti-inflammatory properties of selected acetylenic derivatives of betulonic acid were investigated using the CCl4-induced hepatitis and carrageenan-induced edema models, respectively.
Authors:
Sergey F Vasilevsky; Anastasiya I Govdi; El'vira E Shults; Makhmut M Shakirov; Irina V Sorokina; Tatyana G Tolstikova; Dmitry S Baev; Genrikh A Tolstikov; Igor V Alabugin
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.     Date:  2009-05-29
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  17     ISSN:  1464-3391     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2009 Jul 
Date Detail:
Created Date:  2009-07-15     Completed Date:  2009-10-08     Revised Date:  2009-11-19    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  5164-9     Citation Subset:  IM    
Affiliation:
Institute of Chemical Kinetics and Combustion, Siberian Branch of the Russian Academy of Sciences, 3 Institutskaya str., 630090 Novosibirsk, Russian Federation. vasilev@kinetics.nsc.ru
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MeSH Terms
Descriptor/Qualifier:
Acetylene / chemical synthesis,  chemistry*,  therapeutic use*
Animals
Anti-Inflammatory Agents / chemical synthesis,  chemistry*,  therapeutic use*
Drug-Induced Liver Injury / drug therapy*
Edema / chemically induced,  drug therapy
Enzymes / blood
Inflammation / chemically induced,  drug therapy
Male
Mice
Oleanolic Acid / analogs & derivatives*,  chemical synthesis,  chemistry,  therapeutic use
Chemical
Reg. No./Substance:
0/Anti-Inflammatory Agents; 0/Enzymes; 0/betulonic acid; 508-02-1/Oleanolic Acid; 74-86-2/Acetylene

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


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