| 4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists. | |
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MedLine Citation:
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PMID: 16919453 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Structure-activity relationships of a 4-aminoquinoline MCH1R antagonist lead series were explored by synthesis of analogs with modifications at the 2-, 4-, and 6-positions of the original HTS hit. Improvements to the original screening lead included lipophilic groups at the 2-position and biphenyl, cyclohexyl phenyl, and hydrocinnamyl carboxamides at the 6-position. Modifications of the 4-amino group were not well tolerated. |
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Authors:
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Jinlong Jiang; Peter Lin; Myle Hoang; Lehua Chang; Carina Tan; Scott Feighner; Oksana C Palyha; Donna L Hreniuk; Jie Pan; Andreas W Sailer; Nancy R Morin; Douglas J MacNeil; Andrew D Howard; Lex H T Van der Ploeg; Mark T Goulet; Robert J DeVita |
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Publication Detail:
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Type: In Vitro; Journal Article Date: 2006-08-17 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: 16 ISSN: 0960-894X ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2006 Oct |
Date Detail:
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Created Date: 2006-09-11 Completed Date: 2006-12-04 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: 5275-9 Citation Subset: IM |
Affiliation:
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Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065-0900, USA. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Aminoquinolines
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chemical synthesis,
chemistry,
pharmacology* Binding, Competitive Cell Line Drug Evaluation, Preclinical Humans Molecular Structure Receptors, Somatostatin / antagonists & inhibitors* Stereoisomerism Structure-Activity Relationship |
| Chemical | |
Reg. No./Substance:
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0/Aminoquinolines; 0/MCHR1 protein, human; 0/Receptors, Somatostatin; 578-68-7/4-aminoquinoline |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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