Synthesis and biological evaluation of N 1,N 2-bis-[4-(t-amino)-2-butynyl]phthalamides as oxotremorine and acetylcholine antagonists
A series of N 1,N 2-bis-[4-(t-amino)-2-butynyl] phthalamides have been synthesized and investigated for the blocking of the motor effect of oxotremorine in intact mice and for their antagonistic activity towards acetylcholine on isol
Synthesis and biological evaluation of N-(4-t-amino-2-butynyloxy) and N-(4-t-amino-2-butynyl) phthalimides
A series of N-(4-t-amino-2-butynyloxy) and N-(4-t-amino-2-butynyl) phthalimides have been prepared through the Mannich reaction from N-(propargyloxy) phthalimide or N-propargylphthalimide with formaldehyde and various cyclic amines. These compounds have been investigated for blockade of oxotremorine in intact mice, and for their antagonistic activity towards acetylcholine on isolated guinea pig ileal preparations. None of the oxyphthalimido derivatives show oxotremorine antagonistic activity, but all have an acetylcholine antagonistic activity. The phthalimido compounds, on the other hand, have both oxotremorine and acetylcholine antagonistic activity.
Eldeen,Shubber,Musa,et al.
p. 85 - 88
(2007/10/02)
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