Title compds. [I; R1 = H, alkyl, halo, N3, alkylthio, PhS, PhCH2S, alkoxyalkyloxy, amino; R2-R4 = H, alkyl, (substituted) aryl; R5, R6 = H,, OH, amino, alkoxy, (substituted) aryloxy, PhCH2O, amino, halo, CF3, OCF3, NO2, alkyl, carboxy, carbalkoxy, carbamoyl, alkylcarbamoyl; R5R6 = methylenedioxy, carbonyldioxy, carbonyldiamino; X = OH, (substituted) alkoxy, amino, heterocyclyl], were prepd. Thus, (E,E)-5-(5,6-dichloro-1H-indol-2-yl)-2-methyl-2,4-pentadienoic acid (prepn. given) and 3-diethylamino-1-propylamine, HOBT, and DCC were refluxed in MeCN/THF to give 36.4% (E,E)-5-(5,6-dichloro-1H-indol-2-yl)-N-[3-(diethylamino)propyl]-2-methyl-2,4-pentadienamide. The latter inhibited chicken osteoclast bafilomycin-sensitive ATPase with IC50 = 1.2 μM.
Preparation of 5-(indol-2-yl)-2,4-pentadienoates as inhibitors of bone resorption / C. Farina, S. Gagliardi, E. Consolandi, G. Nadler, P. Seneci.
Preparation of 5-(indol-2-yl)-2,4-pentadienoates as inhibitors of bone resorption.
P. SeneciUltimo
1998
Abstract
Title compds. [I; R1 = H, alkyl, halo, N3, alkylthio, PhS, PhCH2S, alkoxyalkyloxy, amino; R2-R4 = H, alkyl, (substituted) aryl; R5, R6 = H,, OH, amino, alkoxy, (substituted) aryloxy, PhCH2O, amino, halo, CF3, OCF3, NO2, alkyl, carboxy, carbalkoxy, carbamoyl, alkylcarbamoyl; R5R6 = methylenedioxy, carbonyldioxy, carbonyldiamino; X = OH, (substituted) alkoxy, amino, heterocyclyl], were prepd. Thus, (E,E)-5-(5,6-dichloro-1H-indol-2-yl)-2-methyl-2,4-pentadienoic acid (prepn. given) and 3-diethylamino-1-propylamine, HOBT, and DCC were refluxed in MeCN/THF to give 36.4% (E,E)-5-(5,6-dichloro-1H-indol-2-yl)-N-[3-(diethylamino)propyl]-2-methyl-2,4-pentadienamide. The latter inhibited chicken osteoclast bafilomycin-sensitive ATPase with IC50 = 1.2 μM.
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