Highly Potent 1-1,2,3-Triazole-Tethered Isatin-Metronidazole Conjugates Against Anaerobic Foodborne, Waterborne, and Sexually-Transmitted Protozoal Parasites.
Clicks: 269
ID: 58289
2018
Parasitic infections like amebiasis, trichomoniasis, and giardiasis are major health threats in tropical and subtropical regions of the world. Metronidazole (MTZ) is the current drug of choice for amebiasis, giardiasis, and trichomoniasis but it has several adverse effects and potential resistance is a concern. In order to develop alternative antimicrobials, a library of 1-1,2,3-triazole-tethered metronidazole-isatin conjugates was synthesized using Huisgen's azide-alkyne cycloaddition reaction and evaluated for their amebicidal, anti-trichomonal, and anti-giardial potential. Most of the synthesized conjugates exhibited activities against , and . While activities against and were comparable to that of the standard drug MTZ, better activities were observed against and . Conjugates and were found to be 2-3-folds more potent than MTZ against and 8-16-folds more potent than MTZ against . Further analysis of these compounds on fungi and bacteria did not show inhibitory activity, demonstrating their specific anti-protozoal properties.
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| Authors | Kumar, Sumit;Bains, Trpta;Won Kim, Ashley Sae;Tam, Christina;Kim, Jong;Cheng, Luisa W;Land, Kirkwood M;Debnath, Anjan;Kumar, Vipan; |
| Journal | Frontiers in cellular and infection microbiology |
| Year | 2018 |
| DOI | 10.3389/fcimb.2018.00380 |
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