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Synthesis of new S-substituted derivatives of 5-[3- (1H-indol-3-yl) propyl]-1,3,4-oxadiazol-2-ylhydrosulfide as suitable antibacterial and anticancer agents with moderate cytotoxicity

Nazir, M.; Abbasi, M.A.; Aziz-Ur-Rehman, -; Siddiqui, S.Z.; Ali Shah, S.A.; Shahid, M.; Fatima, H.; Iftikhar, S.; Zaib Saleem, R.S.

Pakistan Journal of Pharmaceutical Sciences 32(6): 2585-2597

2019

ISSN/ISBN: 1011-601X
PMID: 31969290
Document Number: 698714
In the study presented here, the nucleophilic substitution reaction of 5-[3-(1H-indol-3-yl)propyl]-1,3,4-oxadiazol-2-ylhydrosulfide was carried out with different alkyl/aralkyl halides (5a-r) to form its different S-substituted derivatives (6a-r), as depicted in scheme 1. The structural confirmation of all the synthesized compounds was done by IR, 1H-NMR, 13C-NMR and CHN analysis data. Bacterial biofilm inhibitory activity of all the synthesized compounds was carried out against Bacillus subtilis and Escherichia coli. The anticancer activity of these molecules was ascertained using anti-proliferation (SRB) assay on HCT 116 Colon Cancer Cell lines while the cytotoxicity of these molecules was profiled for their haemolytic potential. From this investigation it was rational that most of the compounds exhibited suitable antibacterial and anticancer potential along with a temperate cytotoxicity.

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