174186-17-5Relevant academic research and scientific papers
Benzofuran derivatives useful as inhibitors of bone resorption
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, (2008/06/13)
This invention relates to a novel heterocyclic compound represented by formula (I), wherein each symbol is as defined in the specification and a pharmaceutically acceptable salt thereof which are the inhibitors of bone resorption and bone metabolism, to p
7-(N-substituted)amino-2,3-polymethylene benzofurane derivatives with tracheal relaxant activity
Vazzana,Sparatore
, p. 637 - 642 (2007/10/03)
A set of twelve 7-(N-substituted)amino-2,3-polymethylenebenzofuranes (1-12) together with three related compounds (13-15) was prepared. Ten selected compounds were tested for tracheal relaxant activity in vitro and two of them (6,7) were also subjected to a broad pharmacological screening. Five compounds (2, 7, 9, 12, 14) at the concentration of 30 μg/ml exhibited high tracheal relaxant activity (73-94% tone reduction) that was superior than that of theophylline at the same concentration. The 7-(N-trifluoromethylsulfonyl)amino-2,3-tetramethylenebenzofurane (9) was highly active till the concentration of 1 μg/ml giving a stronger tracheal relaxation than amrinone at 3 μg/ml. On the other hand the general screening did not show any other major activity. The benzofurane derivatives 1-13 were obtained through obvious steps from the corresponding 7-nitrobenzofuranes, which were prepared by a Fischer indole-like cyclization of O-[(2-nitro)phenyl] ketone oximes. In one case two peculiar side products were isolated.
