| N-heterocyclic derived M1 positive allosteric modulators. | |
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MedLine Citation:
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PMID: 20097564 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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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:
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Type: Journal Article Date: 2010-01-11 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: 20 ISSN: 1464-3405 ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2010 Feb |
Date Detail:
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Created Date: 2010-02-15 Completed Date: 2010-06-02 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: England |
Other Details:
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Languages: eng Pagination: 1334-7 Citation Subset: IM |
Copyright Information:
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Copyright 2010 Elsevier Ltd. All rights reserved. |
Affiliation:
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Department of Medicinal Chemistry, Merck Research Laboratories, Sumneytown Pike, PO Box 4, West Point, PA 19486, USA. scott_d_kuduk@merck.com |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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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:
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0/Carboxylic Acids; 0/Heterocyclic Compounds; 0/Pyrazoles; 0/Quinolines |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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