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  • Title: Synthesis of some N-substituted indole derivatives and their biological activities.
    Author: el-Diwani H, Nakkady SS, Hishmat OH, el-Shabrawy OA, Mahmoud SS.
    Journal: Pharmazie; 1992 Mar; 47(3):178-81. PubMed ID: 1615022.
    Abstract:
    Acylation of 2,3-diphenyl-5-methoxy-indole using ethyl chloroformate or chloroacetyl chloride in dimethylformamide and sodium hydride yielded the N-substituted derivatives 1 and 2, respectively. While Friedel-Crafts acylation using chloroacetyl chloride afforded di-4,6-chloroacetyl derivative 3, the reaction of the N-chloroacetyl derivative 2 with amines, hydrazines, urea, semicarbazide hydrochloride, thiophenol, benzimidazole-2-thiol, thiosemicarbazide, 2-mercaptoethanol and thioglycolic acid was studied. Several of the compounds were tested for their effect on arterial blood pressure, antiinflammatory and ulcerogenic activities.
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