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Novel 1,3,5-triphenyl-2-pyrazolines as anti-infective agents

2010; Elsevier BV; Volume: 20; Issue: 10 Linguagem: Inglês

10.1016/j.bmcl.2010.03.083

1464-3405

Ponnurengam Malliappan Sivakumar, S. Prabhu Seenivasan, Vanaja Kumar, Mukesh Doble,

Click Chemistry and Applications

Sixteen 1,3,5-triphenyl-2-pyrazolines were synthesized and their anti-infective activities (against Mycobacterium tuberculosis H(37)Rv, six bacterial and four fungal strains) were tested. Only compound with SO(2)CH(3) in the para position of the A-ring was active against the tubercular strain at 100 microg/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 ( 88% reduction) against four fungi studied at 2mg/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.