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Title: Synthesis and biological evaluation of l-acetyl-3-(2-acetoxy-3-substituted propyloximino) indol-2(3H)-ones
Authors: Padhy, A K
Sahu, S K
Panda, P K
Kar, D M
Misro, P K
Issue Date: May-2004
Publisher: NISCAIR-CSIR, India
IPC Code: Int.Cl.7 C 07 D 209/04 // A 61 P 31/10, 31/04
Abstract: 1-Acetyl 3-oximino-indol-2 (3H)-one 2 on reaction with epichlorohydrin in acetone gave l-acetyl-3-(2, 3-epoxy propyloximino) indol-2(3H)-one 3, which, on subsequent reaction with piperidine, pyrolidine, dicyclohexyl amine, diphenyl amine gave corresponding Mannich base 4, which on acetylation furnishes 5a-e. All these synthetic compounds 2, 3 and 5a-e are screened for their anti-microbial action, gross behavioral, toxicity, antagonism of tetrabenazine induced ptosis, inhibition of pentobarbitone-induced narcosis and effect on blood presure and respiration rate in suitable experimental models. Test compouds 2, 3 and 5a-e reduce MIC against B. substilis, E. coli, and C. albicans.Further, these compounds inhibit tetrabenazine induced ptosis in mice, of which except compound 2, all shows a ptosis score of 2 at the end of 150 and 210 min. In the test of inhibition of pentobarbitone induced narcosis all compounds except compound 2 possess a significant decrease in sleeping time. All test compounds inhibit the histamine-induced fall in blood pressure except compound 2. Test compounds 5a-e have a negligible skeletal muscle contraction effect when tested on frog's rectus abdominus muscle
Page(s): 971-975
ISSN: 0975-0983(Online); 0376-4699(Print)
Appears in Collections:IJC-B Vol.43B(05) [May 2004]

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