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% Inhibition of CYP450 isoforms 1A2/2C9/2D6/3A4 at 10 μM was 2/10/28/-14.
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Although the corresponding compound of 6l with a secondary amine (NH) linkage (instead of the tertiary amine linkage in 6l) was not prepared and evaluated, compounds with this side chain (dimethylaminoethylamine-) were synthesized in closely related series and were discovered to have much reduced ROCK potency.
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note
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In vivo pharmacokinetic data were obtained in rats from three determinations with standard deviation ≤20%.
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