Document Detail


PF1022A and related cyclodepsipeptides - a novel class of anthelmintics.
MedLine Citation:
PMID:  12052189     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Parasitic nematodes are a major cause of morbidity and mortality in man and also cause widespread loss of food production by infection of livestock. A milestone in the chemotherapy of nematode infections, especially in animals, was the discovery of the avermectins and milbemycins during the 1970s. Since the discovery of these highly active macrolides, reports of potent new classes of anthelmintics have been scarce. One of the most outstanding recently reported anthelmintics is the cyclooctadepsipeptide PF1022A, the most active member of a novel class of anthelmintic agents. During the past years several total syntheses of PF1022A and manifold structure-activity relationships have been established. Additionally, the biosynthesis of PF1022A has been elucidated and intensive investigations into the mode of action of this novel anthelmintic are underway. Comprehensive studies including cyclodepsipeptides with smaller ring-sizes, such as the enniatins, proved the PF1022 family and related cyclodepsipeptides to be the most promising follow-up candidates for the avermectins and milbemycins, which suffer from increasing nematode resistance.
Authors:
Jurgen Scherkenbeck; Peter Jeschke; Achim Harder
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Publication Detail:
Type:  Journal Article; Review    
Journal Detail:
Title:  Current topics in medicinal chemistry     Volume:  2     ISSN:  1568-0266     ISO Abbreviation:  Curr Top Med Chem     Publication Date:  2002 Jul 
Date Detail:
Created Date:  2002-06-07     Completed Date:  2003-08-08     Revised Date:  2005-11-16    
Medline Journal Info:
Nlm Unique ID:  101119673     Medline TA:  Curr Top Med Chem     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  759-77     Citation Subset:  IM    
Affiliation:
Bayer AG, Leverkusen, Germany. juergen.scherkenbeck.js@bayer-ag.de
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MeSH Terms
Descriptor/Qualifier:
Animals
Anthelmintics / chemistry,  therapeutic use*
Depsipeptides*
Humans
Molecular Structure
Nematode Infections / drug therapy*,  prevention & control,  veterinary
Peptides, Cyclic / biosynthesis,  chemistry,  therapeutic use*
Structure-Activity Relationship
Chemical
Reg. No./Substance:
0/Anthelmintics; 0/Depsipeptides; 0/Peptides, Cyclic; 133413-70-4/PF 1022A

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


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