Document Detail


N-heterocyclic derived M1 positive allosteric modulators.
MedLine Citation:
PMID:  20097564     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Replacement of a phenyl ring with N-linked heterocycles in a series of quinolone carboxylic acid M1 positive allosteric modulators was investigated. In particular, a pyrazole derivative exhibited improvements in potency, free fraction, and CNS exposure.
Authors:
Scott D Kuduk; Christina N Di Marco; Victoria Cofre; Daniel R Pitts; William J Ray; Lei Ma; Marion Wittmann; Lone Veng; Matthew A Seager; Kenneth Koeplinger; Charles D Thompson; George D Hartman; Mark T Bilodeau
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Publication Detail:
Type:  Journal Article     Date:  2010-01-11
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  20     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2010 Feb 
Date Detail:
Created Date:  2010-02-15     Completed Date:  2010-06-02     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  1334-7     Citation Subset:  IM    
Copyright Information:
Copyright 2010 Elsevier Ltd. All rights reserved.
Affiliation:
Department of Medicinal Chemistry, Merck Research Laboratories, Sumneytown Pike, PO Box 4, West Point, PA 19486, USA. scott_d_kuduk@merck.com
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MeSH Terms
Descriptor/Qualifier:
Allosteric Regulation
Animals
CHO Cells
Carboxylic Acids / chemical synthesis*,  chemistry,  pharmacology
Cell Line
Cricetinae
Cricetulus
Heterocyclic Compounds / chemical synthesis*,  chemistry,  pharmacology
Humans
Molecular Structure
Pyrazoles / chemical synthesis*,  chemistry,  pharmacology
Quinolines / chemical synthesis*,  chemistry,  pharmacology
Rats
Structure-Activity Relationship
Chemical
Reg. No./Substance:
0/Carboxylic Acids; 0/Heterocyclic Compounds; 0/Pyrazoles; 0/Quinolines

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