Synthesis and Biological Activity of Novel 4-/5-/6-/7-Nitro-N ′-(4-Aryl-1,3-Thiazol-2-yl)1H-Indole-2-Carbohydrazide Derivatives
摘要:
New 4-/5-/6-/7-nitro-N'-(4-aryl-1,3-thiazol-2-yl)-1H-indole-2-carbohydrazides (4a-t) were prepared by treating respective nitroindole thiosemicarbazide with aromatic acylbromides. The newly synthesized compounds were characterized by analytical and spectral data. The compounds were also screened for antifungal and antibacterial activity. Some of the compounds exhibited promising antimicrobial activity.
Synthesis of some new biologically active 1,3,4-oxadiazolyl nitroindoles and a modified Fischer indole synthesis of ethyl nitro indole-2-carboxylates
摘要:
An efficient and modified synthesis of ethyl-4-nitro/5-nitro/6-nitro and 7-nitroindole-2-carboxylates is described. Carbo-hydrazides of corresponding ethyl nitroindole-2-carboxylates underwent smooth one-step transformation to 1,3,4-oxadiazolyl nitroindoles (4a-I) on reaction with aromatic carboxylic acids in the presence of phosphorus oxychloride. An alternate method to synthesize 1,3,4-oxadiazolyl nitroindoles is also described. Among the newly synthesized 1,3,4-oxadiazolyl nitroindoles, a few compounds are studied for anti-inflammatory activity. (c) 2005 Published by Elsevier Ltd.
Novel 8-chloro-6-(2-fluorophenyl)-1-(aryl)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine s (5a-f) were prepared by treating 7-chloro-5-(2-fluorophenyl)-1,3-dihydro-2H-1,4-benzodiazepine-2-thione with various aromatic acid hydrazides. The newly prepared compounds were characterized by spectral analysis. Compounds were tested for anticonvulsant activity. Four of the tested compounds such as 5a, 5d, 5e