Chemical and Pharmaceutical Bulletin p. 1486 - 1493 (1992)
Update date:2022-08-04
Topics:
Yamanaka
Suda
Kabasawa
Kawamura
Ogawa
Sawada
Ohhara
Structural modification of the cardiotonic agent, loprinone (E-1020, 1), suggested by data that it has a less positive chronotropic effect than milrinone (15), led us to find novel bradycardic agents that were structurally different from homoveratryl amine derivatives. Alkyl-oxy, -thio, and -amino derivatives at the 2-position of the pyridine ring of 1 produced bradycardic activity without a significant effect on blood pressure and myocardial contractility. Aryloxy analogues also decreased beart rate, and members with an electron-withdrawing group at the ortho position of the phenyl ring showed higher activity. Replacement of the imidazo[1,2-a]pyridine with pyridine resulted in diminished activity. The mechanism of bradycardic activity of these compounds seems to be direct action on the sinus node.
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()Doi:10.1016/S0040-4020(01)88306-X
(1992)
