Discovery of FK453, a novel non-xanthine adenosine A1 receptor antagonist
Autor: | Youichi Shiokawa, Takafumi Mitsunaga, Atsushi Akahane, Keizo Yoshida, Takahiro Kusunoki, Takao Terai, Hirohito Katayama, Yasuhiro Kita |
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Rok vydání: | 1996 |
Předmět: |
Stereochemistry
medicine.medical_treatment Organic Chemistry Clinical Biochemistry Antagonist Pharmaceutical Science Pharmacology Xanthine Biochemistry Adenosine receptor chemistry.chemical_compound Adenosine A1 receptor chemistry Drug Discovery medicine Molecular Medicine Diuretic Molecular Biology |
Zdroj: | Bioorganic & Medicinal Chemistry Letters. 6:2059-2062 |
ISSN: | 0960-894X |
DOI: | 10.1016/0960-894x(96)00368-x |
Popis: | Novel 2-phenylpyrazolo[1,5-a]pyridine-3-acryloylamides were synthesized and evaluated for diuretic activities. FK453 (1d), the most potent compound in this series, was found to be a potent and selective adenosine A1 receptor antagonist, whereas 1e, the (S)-enantiomer of FK453, was a weak and non-selective adenosine antagonist. |
Databáze: | OpenAIRE |
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