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In the absence of protective vaccines, the management of the disease banks solely on chemotherapy. However, the clinical usefulness of current antileishmanial drugs is threatened by their toxicity and the emergence of multidrug\u2010resistant strains of the causative pathogens. This emphasizes the imperative for the development of new and effective antileishmanial agents. In this regard, we synthesized and evaluated <jats:italic>in\u2005vitro<\/jats:italic> the antileishmanial activity and cytotoxicity profile of a series of nitrofurantoin\u2010triazole hybrids. The nitrofurantoin derivative <jats:bold>1<\/jats:bold> featuring propargyl moiety was distinctively the most active of all, was nontoxic to human cells and possessed submicromolar cellular activity selectively directed towards the pathogens of the life threatening visceral leishmaniasis. Hence it was identified as potential antileishmanial lead for further investigation into its prospective to act as alternative to therapies.<\/jats:p>","DOI":"10.1002\/cmdc.202200023","type":"journal-article","created":{"date-parts":[[2022,4,7]],"date-time":"2022-04-07T05:07:05Z","timestamp":1649308025000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":27,"title":["Synthesis, <i>in\u2005vitro<\/i> Antileishmanial Efficacy and Hit\/Lead Identification of Nitrofurantoin\u2010Triazole Hybrids"],"prefix":"10.1002","volume":"17","author":[{"given":"Nonkululeko H.","family":"Zuma","sequence":"first","affiliation":[{"name":"Centre of Excellence for Pharmaceutical Sciences (Pharmacen) Faculty of Health Sciences North-West University  11 Hoffmann Street Potchefstroom 2520 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Janine","family":"Aucamp","sequence":"additional","affiliation":[{"name":"Centre of Excellence for Pharmaceutical Sciences (Pharmacen) Faculty of Health Sciences North-West University  11 Hoffmann Street Potchefstroom 2520 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Maryna","family":"Viljoen","sequence":"additional","affiliation":[{"name":"School of Pharmacy, Faculty of Health Sciences North-West University  11 Hoffmann Street Potchefstroom 2520 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"David D.","family":"N'Da","sequence":"additional","affiliation":[{"name":"Centre of Excellence for Pharmaceutical Sciences (Pharmacen) Faculty of Health Sciences North-West University  11 Hoffmann Street Potchefstroom 2520 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2022,5,2]]},"reference":[{"key":"e_1_2_11_1_1","unstructured":"WHO Leishmaniasis https:\/\/www.who.int\/news-room\/fact-sheets\/detail\/leishmaniasis[Date of access: 08 January 2022] 2022."},{"key":"e_1_2_11_2_1","unstructured":"\u00a0"},{"key":"e_1_2_11_3_2","first-page":"561","volume":"3","author":"Cheraghipour K.","year":"2018","journal-title":"AIMS J."},{"key":"e_1_2_11_4_2","doi-asserted-by":"publisher","DOI":"10.1007\/s00253-020-10856-w"},{"key":"e_1_2_11_5_1","doi-asserted-by":"publisher","DOI":"10.1371\/journal.pntd.0005641"},{"key":"e_1_2_11_6_1","doi-asserted-by":"publisher","DOI":"10.1038\/s41392-020-00213-8"},{"key":"e_1_2_11_7_1","doi-asserted-by":"publisher","DOI":"10.1038\/nm.4306"},{"key":"e_1_2_11_8_1","doi-asserted-by":"publisher","DOI":"10.2174\/1568026619666190619115735"},{"key":"e_1_2_11_9_1","doi-asserted-by":"publisher","DOI":"10.1017\/S0031182017000993"},{"key":"e_1_2_11_10_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0378-4274(02)00238-2"},{"key":"e_1_2_11_11_1","doi-asserted-by":"publisher","DOI":"10.1124\/jpet.110.172981"},{"key":"e_1_2_11_12_1","unstructured":"\u00a0"},{"key":"e_1_2_11_13_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.exppara.2016.01.007"},{"key":"e_1_2_11_14_2","doi-asserted-by":"publisher","DOI":"10.1371\/journal.pntd.0007790"},{"key":"e_1_2_11_15_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.pt.2009.05.010"},{"key":"e_1_2_11_16_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.freeradbiomed.2007.12.013"},{"key":"e_1_2_11_17_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.chembiol.2012.05.017"},{"key":"e_1_2_11_18_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1574-6976.2008.00107.x"},{"key":"e_1_2_11_19_1","doi-asserted-by":"publisher","DOI":"10.1111\/bph.13571"},{"key":"e_1_2_11_20_1","unstructured":"\u00a0"},{"key":"e_1_2_11_21_2","doi-asserted-by":"publisher","DOI":"10.1289\/ehp.8564309"},{"key":"e_1_2_11_22_2","doi-asserted-by":"publisher","DOI":"10.1016\/0014-5793(85)80732-8"},{"key":"e_1_2_11_23_1","doi-asserted-by":"crossref","unstructured":"B.\u2005E. 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