Discovery of FR166124, a novel water-soluble pyrazolo[1,5-a]pyridine adenosine A1 receptor antagonist

DOI: 10.1016/S0960-894X(99)00304-2

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 1979 - 1984 (1999)

Update date:2022-08-04

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Authors:

Kuroda, Satoru

Akahane, Atsushi

Itani, Hiromichi

Nishimura, Shintaro

Durkin, Kieran

Kinoshita, Takayoshi

Tenda, Yoshiyuki

Sakane, Kazuo

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Article abstract of DOI:10.1016/S0960-894X(99)00304-2

Novel 3-(2-cycloalkyl and cycloalkenyl-3-oxo-2,3-dihydropyridazin-6- yl)-2-phenylpyrazolo[1,5-a]pyridines were synthesized and evaluated for their adenosine A₁ receptor binding activities. In this series, FR166124 (3) was found to be the most potent and selective adenosine A₁ receptor antagonist, and the double bond of the cyclohexenyl acetic acid group was essential for selectivity of A₁ receptor binding. Furthermore, the solubility in water of the sodium salt of FR166124 was high.

Full text of DOI:10.1016/S0960-894X(99)00304-2

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