112887-29-3Relevant academic research and scientific papers
Synthesis and gastroprokinetic activity of 2-Almino-N-[(4-benzyl-2-morpholinyl)methyl]benzamide derivatives
Kato,Morie,Ohno,Yoshida,Yoshida,Naruto
, p. 582 - 587 (2007/10/02)
2-Alkoxy-4-amino-N-[(4-benzyl-2-morpholinyl)methyl]-5-chlorobenzamides had been identified as the interesting members of a series of selective and potent gastroprokinetic agents. A new series of 2-amino- and 2-(substituted amino)-N-[(4-benzyl-2-morpholinyl)methyl]benzamides (13-35) has been synthesized and these compounds were examined to determine whether they have advantages over the 2-morpholinyl benzamides 1 with a 2-alkoxy group. The gastroprokinetic activity was generally reduced, but several compounds showed relatively:potent activity, comparable to that of the standard agent, metoclopramide. N-[(4-Benzyl-2-morpholinyl)methyl]-4-chloro-2-[(4- chlorobenzoyl)amino]benzamide (32) showed the most potent activity in this series.
Substituted benzamide derivatives, for enhancing gastrointestinal motility
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, (2008/06/13)
Compounds of the formula: STR1 wherein R is hydrogen, alkoxycarbonyl, benzyloxycarbonyl, heteroarylalkyl, phenylalkenyl, or --T--(Y)p --R6 (wherein T is single bond or alkylene, Y is oxygen, sulfur or carbonyl, R6 is phenyl, substituted phenyl, naphthyl, or diphenylmethyl, and p is 0 or 1, provided that when T is single bond, p is 0); R1 is halogen, hydroxy, alkoxy, cycloalkyloxy, alkenyloxy, alkynyloxy, alkoxy interrupted by oxygen or carbonyl, alkylthio, amino, monosubstituted amino, or a substituted alkoxy; R2 is hydrogen; R3 is hydrogen, halogen, amino, alkylamino, dialkylamino, alkanoylamino, or nitro; R4 is hydrogen, halogen, nitro, sulfamoyl, alkylsulfamoyl, or dialkylsulfamoyl; or any two adjacent groups of the R1, R2, R3 and R4 may combine to form alkylenedioxy, and the remaining two groups are each hydrogen; R5 is hydrogen or alkyl; X is alkylene; m and n are each 1 or 2; provided that at least one of the groups R2, R3 and R4 is other than hydrogen, and acid addition salts, quaternary ammonium salts and N-oxide derivatives thereof, processes for preparation thereof, and pharmaceutical composition containing the same. Said compounds, salts and N-oxide derivatives thereof show excellent gastrointestinal motility enhancing activity.
