AUTHOR=Kumar Sumit , Bains Trpta , Won Kim Ashley Sae , Tam Christina , Kim Jong , Cheng Luisa W. , Land Kirkwood M. , Debnath Anjan , Kumar Vipan 

TITLE=Highly Potent 1H-1,2,3-Triazole-Tethered Isatin-Metronidazole Conjugates Against Anaerobic Foodborne, Waterborne, and Sexually-Transmitted Protozoal Parasites

JOURNAL=Frontiers in Cellular and Infection Microbiology

VOLUME=8

YEAR=2018

URL=https://www.frontiersin.org/journals/cellular-and-infection-microbiology/articles/10.3389/fcimb.2018.00380

DOI=10.3389/fcimb.2018.00380

ISSN=2235-2988

ABSTRACT=<p>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<italic>H</italic>-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 <italic>Trichomonas vaginalis, Tritrichomonas foetus, Entamoeba histolytica</italic>, and <italic>Giardia lamblia</italic>. While activities against <italic>T. vaginalis</italic> and <italic>T. foetus</italic> were comparable to that of the standard drug MTZ, better activities were observed against <italic>E. histolytica</italic> and <italic>G. lamblia</italic>. Conjugates <bold>9d</bold> and <bold>10a</bold> were found to be 2–3-folds more potent than MTZ against <italic>E. histolytica</italic> and 8–16-folds more potent than MTZ against <italic>G. lamblia</italic>. Further analysis of these compounds on fungi and bacteria did not show inhibitory activity, demonstrating their specific anti-protozoal properties.</p>