Structure-activity relationship study on the 6-membered heteroaromatic ring system of diphenylpyrazine-type prostacyclin receptor agonists.

Structure-activity relationship study on the 6-membered heteroaromatic ring system of diphenylpyrazine-type prostacyclin receptor agonists. Research Abstract Details 

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Structure-activity relationship study on the 6-membered heteroaromatic ring system of diphenylpyrazine-type prostacyclin receptor agonists. Abstract Text:

Tetsuo Asaki,Taisuke Hamamoto,Yukiteru Sugiyama,Keiichi Kuwano,Kenji Kuwabara,Tomoko Niwa,Tetsuo Asaki,Taisuke Hamamoto,Yukiteru Sugiyama,Keiichi Kuwano,Kenji Kuwabara,Tomoko Niwa,

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.

Structure-activity relationship study on the 6-membered heteroaromatic ring system of diphenylpyrazine-type prostacyclin receptor agonists. Publishing Authors By Initials

T Asaki,T Hamamoto,Y Sugiyama,K Kuwano,K Kuwabara,T Niwa,T Asaki,T Hamamoto,Y Sugiyama,K Kuwano,K Kuwabara,T Niwa,

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Structure-activity relationship study on the 6-membered heteroaromatic ring system of diphenylpyrazine-type prostacyclin receptor agonists. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 17

Page Numbers: 6588-92

Journal Abbreviation: Bioorg. Med. Chem. Lett.

ISSN: 0960-894X

DAY: 22

MONTH: 09

YEAR: 2007

Structure-activity relationship study on the 6-membered heteroaromatic ring system of diphenylpyrazine-type prostacyclin receptor agonists. Information

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LANGUAGE: eng

NlmUniqueID: 9107377

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Grant and Affiliation Information for Structure-activity relationship study on the 6-membered heteroaromatic ring system of diphenylpyrazine-type prostacyclin receptor agonists.

AFFILIATION: Discovery Research Laboratories, Nippon Shinyaku Co., Ltd, 14, Nishinosho-Monguchi-Cho, Kisshoin, Minami-ku, Kyoto 601-8550, Japan.

Country: England

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MEDLINETA: Bioorg Med Chem Lett

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