Abstract
A novel set of 16 hybrids of bromopyrrole alkaloids with aroyl hydrazone were designed, synthesized and evaluated for antibacterial and antibiofilm activities against methicillin-resistant Staphylococcus aureus (MRSA; ATCC 43866), methicillin-susceptible Staphylococcus aureus (MSSA; ATCC 35556) and Staphylococcus epidermidis (SE, S. epidermidis ATCC 35984). Of the 16 tested hybrids, 14 exhibited equal or superior antibiofilm activity against MSSA and MRSA relative to standard vancomycin. Compound 4m showed highest potency with antibiofilm activity of 0.39 µg/mL and 0.78 µg/mL against MSSA and MRSA, respectively. Thus, this compound could act as a potential lead for further development of new antistaphylococcal drugs.
Keywords:
Antistaphylococcal activity; bromopyrrole alkaloids; hydrazide derivatives.
MeSH terms
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Alkaloids / chemical synthesis*
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Alkaloids / chemistry
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Alkaloids / pharmacology
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Animals
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Anti-Bacterial Agents / chemical synthesis*
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / pharmacology
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Biofilms / drug effects*
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Biofilms / growth & development
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Drug Design
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Drug Resistance, Bacterial
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Hydrazones / chemistry
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Methicillin-Resistant Staphylococcus aureus / drug effects*
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Methicillin-Resistant Staphylococcus aureus / growth & development
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Microbial Sensitivity Tests
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Microbial Viability / drug effects
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Porifera / chemistry
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Pyrroles / chemical synthesis*
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Pyrroles / chemistry
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Pyrroles / pharmacology
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Staphylococcus epidermidis / drug effects*
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Staphylococcus epidermidis / growth & development
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Thiazolidines / chemistry
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Vancomycin / pharmacology
Substances
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Alkaloids
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Anti-Bacterial Agents
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Hydrazones
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Pyrroles
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Thiazolidines
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Vancomycin