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Novel 1,3,5-triphenyl-2-pyrazolines as anti-infective agents
Ponnurengan Malliappan Sivakumar,
Published in
2010
PMID: 20385494
Volume: 20
   
Issue: 10
Pages: 3169 - 3172
Abstract
Sixteen 1,3,5-triphenyl-2-pyrazolines were synthesized and their anti-infective activities (against Mycobacterium tuberculosis H37Rv, six bacterial and four fungal strains) were tested. Only compound with SO2CH3 in the para position of the A-ring was active against the tubercular strain at 100 μg/ml concentration. All compounds showed good anti infective activity against Escherichia coli and poor activity against Staphylococcus aureus. Compounds 4, 12, 13 and 14 exhibited reasonable activity against all the organisms tested (<0.309 μM except against S. aureus. The activity of these compounds correlated with their lipophilic/hydrophilic nature. Compounds 4, 10 and 16 showed very good activity (>88% reduction) against four fungi studied at 2 mg/ml. All these compounds possess halogen substitutions. Compound 11 showed very high activity (>90%) against three fungi. Majority of the compounds showed more than 90% inhibition against one or two fungi. Since pyrazolines are reported to inhibit the activity of p-glycoprotein, they may prevent drug resistance developed by microorganism. © 2010 Elsevier Ltd. All rights reserved.
About the journal
JournalBioorganic and Medicinal Chemistry Letters
ISSN0960894X
Open AccessNo
Concepts (37)
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    1,3,5 TRIPHENYL 2 PYRAZOLINE DERIVATIVE
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    Antiinfective agent
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    GLYCOPROTEIN P
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    Unclassified drug
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    Antibacterial activity
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    Antibiotic resistance
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    Antifungal activity
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    Article
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    ASPERGILLUS FLAVUS
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    Aspergillus niger
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    Bacillus subtilis
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    CANDIDA TROPICALIS
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    Chemical modification
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    Controlled study
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    Drug structure
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    Drug synthesis
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    ENTEROBACTER AEROGENES
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    Escherichia coli
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    FUSARIUM PROLIFERATUM
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    Hydrophilicity
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    In vitro study
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    Infrared spectroscopy
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    Lipophilicity
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    Minimum inhibitory concentration
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    Mycobacterium tuberculosis
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    Nonhuman
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    Nuclear magnetic resonance spectroscopy
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    PROTEUS VULGARIS
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    Salmonella typhi
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    Staphylococcus aureus
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    Structure activity relation
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    Anti-infective agents
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    Microbial sensitivity tests
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    P-glycoprotein
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    Pyrazoles
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    Bacteria (microorganisms)
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    Fungi