ZHANG Ming-Zhe, HE Mei-Yu. SYNTHESIS OF DIACYLHYDRAZIDES OF 2-INDOLE AND THEIR PHYSIOLOGICAL ACTIVITYJ. Acta Pharmaceutica Sinica, 1984, 19(10): 737-741.
Citation: ZHANG Ming-Zhe, HE Mei-Yu. SYNTHESIS OF DIACYLHYDRAZIDES OF 2-INDOLE AND THEIR PHYSIOLOGICAL ACTIVITYJ. Acta Pharmaceutica Sinica, 1984, 19(10): 737-741.

SYNTHESIS OF DIACYLHYDRAZIDES OF 2-INDOLE AND THEIR PHYSIOLOGICAL ACTIVITY

  • Several diacyl (aroyl) hydrazides of 2-indole were synthesised by the reaction of 2-indolecarboxylic acid hydrazides with acyl (aroyl) chlorides (RCOCl or ArCOC1, R=H, CH3, C2H5, CICH2, CH3(CH2)3, and Ar=4-Br-C6H4-or 3-C5H4N-) in anhydrous DMF or acetonitrile. It was found that when 2-indolecarboxylic acid hydrazide reacted with acetyl or propionyl chloride in acetonitrile, two other compounds were isolated. Their structures were established by 13C NMR spectroscopy.Formyl and acetylhydrazide of 2-indolecarboxylic acid and 2--5-(2-ethyl)-1,3,4oxadiazole-indole were shown to have bacteriostatic activity in vitro on Mycobacterium tuberculosis (Zopf.) Lehmann et Neumann.
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