Imide and isatin derivatives as γ-lactam mimics of ß-lactam antibiotics

Hadfield, Peter S.; Casey, Lorraine A.; Galt, R. H. B.; Vilanova, Bartolomé; Page, Michael I.

doi:10.3998/ark.5550190.0003.612

Cited by 3 publications

References 11 publications

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Synthesis and preliminary in vitro activity of mono- and bis-1H-1,2,3-triazole-tethered β-lactam–isatin conjugates against the human protozoal pathogen Trichomonas vaginalis

et al. 2014

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Synthesis and preliminary in vitro activity of monoand bis-1H-1,2,3-triazole-tethered b-lactam-isatin conjugates against the human protozoal pathogen Trichomonas vaginalis Abstract In this study, we describe the synthesis of mono-and bis-1H-1,2,3-triazole-tethered b-lactam-isatin conjugates using copper-catalysed azide-alkyne cycloaddition reaction between mono-and di-propargylated azetidin-2-ones and N-alkylazido isatins. The synthesized conjugates were evaluated for their preliminary in vitro analysis against Trichomonas vaginalis at 50 lM. The efficacy of synthesized hybrids was observed to depend on the substituent at N-1 position of b-lactam ring, as well as the presence of single/double 1H-1,2,3-triazole linker. Among the synthesized conjugates, the presence of a ptolyl substituent at N-1 of b-lactam ring was preferred for good activity profiles while the increase in spacer length did not influence the efficacy of the compounds. Compounds with high levels of potency were further analysed to determine their IC 50 values, as well as cytotoxicity profiles against mammalian cells. The most active compound in the synthesized conjugates displayed an IC 50 value of 10.49 lM against cultured G3 strain of T. vaginalis and was non-toxic to cultured mammalian HeLa cells at the same concentration.

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Synthesis and preliminary in vitro activity of mono- and bis-1H-1,2,3-triazole-tethered β-lactam–isatin conjugates against the human protozoal pathogen Trichomonas vaginalis

et al. 2014

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Synthesis, spectral characterization, antioxidant and anticancer evaluation of 1, 2, 3-trisubstituted-γ-lactams

Khalifa¹,

Magtoof²,

Kredy³

2022

PROCEEDING OF THE 1ST INTERNATIONAL CONFERENCE ON ADVANCED RESEARCH IN PURE AND APPLIED SCIENCE (ICARPAS2021): Third Annual Con

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Antimicrobial Evaluation of Maleimide Monomers, Homopolymers and Copolymers Containing Azo, Sulphonamide and Thiazole Groups

Bapna

Hiran

Jain

2016

JAC

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New maleimide Monomers, homopolymers and copolymers containing azo, sulfonamide and thiazole groups were synthesized. The structures of newly synthesized compounds have been characterized on the basis of their spectroscopic data (FT-IR and 1H-NMR). Antimicrobial studies of synthesized compounds were performed using agar well diffusion method. All the compounds showed pronounced activity against bacterial strains in comparison to activity against fungal strains.The highest antibacterial potency was exhibited by the homopolymer HPSPMI against Escherichia coli, Klebsiella pneumoniae and Bacillus subtilis. The activity of HPSPMI against later two was more pronounced than the standard drug used. Only Selected compounds showed antifungal activity. Appreciable results were found against Aspergillus fumigates but not with Candida albicans. HPSPMI showed highest activity against Aspergillus fumigates. Surprisingly after homo and copolymerization, maximum compounds exhibited not only pronounced antibacterial activity but also antifungal activity.

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Imide and isatin derivatives as γ-lactam mimics of ß-lactam antibiotics

Abstract: Activated γ-lactams, which are derivatives of succinimide, phthalimide and isatin with suitable elements of molecular recognition, have been synthesised as mimics of the ß-lactam antibiotics and their chemical and biological reactivity determined.

Cited by 3 publications

References 11 publications

Synthesis and preliminary in vitro activity of mono- and bis-1H-1,2,3-triazole-tethered β-lactam–isatin conjugates against the human protozoal pathogen Trichomonas vaginalis

Synthesis and preliminary in vitro activity of mono- and bis-1H-1,2,3-triazole-tethered β-lactam–isatin conjugates against the human protozoal pathogen Trichomonas vaginalis

Synthesis, spectral characterization, antioxidant and anticancer evaluation of 1, 2, 3-trisubstituted-γ-lactams

Antimicrobial Evaluation of Maleimide Monomers, Homopolymers and Copolymers Containing Azo, Sulphonamide and Thiazole Groups

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