Abstract
Thiosemicarbazones of p-aminobenzoic acid (PABA) were synthesized and tested for their antimicrobial and anticancer activity. Hydroxamate derivatives 4a-4l were found to have better antimicrobial and anticancer activity than their acid counterpart. Compound 4d was found to have good antimicrobial activity against Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus, Vibrio cholerae, and Bacillus subtilis with IC(50) value of about 1 µM. Compound 4f showed potent antifungal activity against Candida albicans (IC(50) = 1.29 µM) and compound 4h showed potent anticancer activity (IC(50) = 0.07 µM).
Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
MeSH terms
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Amidohydrolases / antagonists & inhibitors
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Anti-Infective Agents / chemical synthesis*
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Anti-Infective Agents / chemistry
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Anti-Infective Agents / pharmacology*
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Drug Screening Assays, Antitumor / methods
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HT29 Cells
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Humans
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Hydroxamic Acids / chemistry
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Microbial Sensitivity Tests / methods
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Molecular Structure
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Structure-Activity Relationship
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Thiosemicarbazones / chemical synthesis*
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Thiosemicarbazones / chemistry
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Thiosemicarbazones / pharmacology*
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para-Aminobenzoates*
Substances
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Anti-Infective Agents
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Antineoplastic Agents
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Hydroxamic Acids
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Thiosemicarbazones
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para-Aminobenzoates
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Amidohydrolases
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peptide deformylase