Document Detail


Structure-activity relationship study on the 6-membered heteroaromatic ring system of diphenylpyrazine-type prostacyclin receptor agonists.
MedLine Citation:
PMID:  17920266     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Tetsuo Asaki; Taisuke Hamamoto; Yukiteru Sugiyama; Keiichi Kuwano; Kenji Kuwabara; Tomoko Niwa
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Publication Detail:
Type:  Comparative Study; Journal Article     Date:  2007-09-22
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  17     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2007 Dec 
Date Detail:
Created Date:  2007-11-06     Completed Date:  2008-03-03     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  6588-92     Citation Subset:  IM    
Affiliation:
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
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MeSH Terms
Descriptor/Qualifier:
Heterocyclic Compounds / 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:
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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