Synthesis and characterisation of halogenated bis(acylthiourea) derivatives and its antibacterial activities

A total of 12 bis(acylthiourea) derivatives with different pharmacophores have been synthesized via nucleophilic substitution reaction of benzene-1,4-dicarbonyl isothiocyanate intermediate with aromatic amine bearing halogens at the ortho, meta and para positions. The structures of the synthesised c...

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Bibliographic Details
Main Authors: Ainaa Nadiah, Abd Halim, Zainab, Ngaini
Format: Article
Published: Taylor & Francis 2017
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Online Access:http://ir.unimas.my/id/eprint/18505/
Description
Summary:A total of 12 bis(acylthiourea) derivatives with different pharmacophores have been synthesized via nucleophilic substitution reaction of benzene-1,4-dicarbonyl isothiocyanate intermediate with aromatic amine bearing halogens at the ortho, meta and para positions. The structures of the synthesised compounds were confirmed by CHN elemental analysis, FT-IR, ¹H NMR and ¹³C NMR spectroscopies. Antibacterial studies of the compounds via the Kirby Bauer disc diffusion method against Escherichia coli (E.coli) ATCC 25922 and Staphylococcus aureus (S. aureus) S48/81 demonstrated that bis(acylthiourea) N¹,N⁴-bis[(2-chlorophenyl)carbamothioyl]terephthalamide (4) and N¹,N⁴-bis[(2-bromophenyl)carbamothioyl]terephthalamide (7) bearing Cl and Br at the ortho position exhibited excellent activities against both bacteria strains compared to ampicillin standard.