Bioorganic and Medicinal Chemistry Letters p. 1979 - 1984 (1999)
Update date:2022-08-04
Topics:
Kuroda, Satoru
Akahane, Atsushi
Itani, Hiromichi
Nishimura, Shintaro
Durkin, Kieran
Kinoshita, Takayoshi
Tenda, Yoshiyuki
Sakane, Kazuo
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.
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