| Structure-activity relationship study on the 6-membered heteroaromatic ring system of diphenylpyrazine-type prostacyclin receptor agonists. | |
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MedLine Citation:
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PMID: 17920266 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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A series of prostacyclin receptor agonists was prepared by modifying the central heteroaromatic ring of lead compound 2, and a docking study was performed to investigate their structure-activity relationships by using a homology-modeled structure of the prostacyclin receptor. Compound 2 and its derivatives could be docked to the prostacyclin receptor in two ways depending on the position of the nitrogen atom within the heteroaromatic ring. Furthermore, hydrogen bonding between the nitrogen atom in the heteroaromatic ring and the hydroxyl group of Ser20 or Tyr75 of the receptor appears to be important for the potent expression of biological activity. |
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Authors:
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Tetsuo Asaki; Taisuke Hamamoto; Yukiteru Sugiyama; Keiichi Kuwano; Kenji Kuwabara; Tomoko Niwa |
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Publication Detail:
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Type: Comparative Study; Journal Article Date: 2007-09-22 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: 17 ISSN: 1464-3405 ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2007 Dec |
Date Detail:
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Created Date: 2007-11-06 Completed Date: 2008-03-03 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: 6588-92 Citation Subset: IM |
Affiliation:
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Discovery Research Laboratories, Nippon Shinyaku Co., Ltd, 14, Nishinosho-Monguchi-Cho, Kisshoin, Minami-ku, Kyoto 601-8550, Japan. t.asaki@po.nippon-shinyaku.co.jp |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Heterocyclic Compounds
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chemistry*,
pharmacology* Humans Molecular Structure Platelet Aggregation / drug effects Platelet Aggregation Inhibitors / chemistry, pharmacology Pyrazines / chemistry*, pharmacology* Receptors, Epoprostenol / agonists*, physiology Structure-Activity Relationship |
| Chemical | |
Reg. No./Substance:
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0/Heterocyclic Compounds; 0/Platelet Aggregation Inhibitors; 0/Pyrazines; 0/Receptors, Epoprostenol |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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