{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,1,18]],"date-time":"2026-01-18T11:40:51Z","timestamp":1768736451056,"version":"3.49.0"},"reference-count":45,"publisher":"MDPI AG","issue":"24","license":[{"start":{"date-parts":[[2020,12,15]],"date-time":"2020-12-15T00:00:00Z","timestamp":1607990400000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100001321","name":"National Research Foundation","doi-asserted-by":"publisher","award":["116282"],"award-info":[{"award-number":["116282"]}],"id":[{"id":"10.13039\/501100001321","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>A second generation of 4-aminoquinoline- and 8-aminoquinoline-based tetrazoles and lactams were synthesized via the Staudinger and Ugi multicomponent reactions. These compounds were subsequently evaluated in vitro for their potential antiplasmodium activity against a multidrug-resistant K1 strain and for their antitrypanosomal activity against a cultured T. b. rhodesiense STIB900 strain. Several of these compounds (4a\u2013g) displayed good antiplasmodium activities (IC50 = 0.20\u20130.62 \u00b5M) that were comparable to the reference drugs, while their antitrypanosomal activity was moderate (&lt;20 \u00b5M). Compound 4e was 2-fold more active than primaquine and was also the most active (IC50 = 7.01 \u00b5M) against T. b. rhodesiense and also exhibited excellent aqueous solubility (&gt;200 \u00b5M) at pH 7.<\/jats:p>","DOI":"10.3390\/molecules25245941","type":"journal-article","created":{"date-parts":[[2020,12,15]],"date-time":"2020-12-15T09:12:57Z","timestamp":1608023577000},"page":"5941","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":4,"title":["Synthesis and In Vitro Antiprotozoan Evaluation of 4-\/8-Aminoquinoline-based Lactams and Tetrazoles"],"prefix":"10.3390","volume":"25","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-1844-3614","authenticated-orcid":false,"given":"Matshawandile","family":"Tukulula","sequence":"first","affiliation":[{"name":"School of Chemistry and Physics, University of KwaZulu Natal, Durban 4000, South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-3122-8812","authenticated-orcid":false,"given":"Stefan","family":"Louw","sequence":"additional","affiliation":[{"name":"Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa"},{"name":"Department of Chemistry and Biochemistry, University of Namibia, Windhoek 10005, Namibia"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1276-2224","authenticated-orcid":false,"given":"Mathew","family":"Njoroge","sequence":"additional","affiliation":[{"name":"Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Kelly","family":"Chibale","sequence":"additional","affiliation":[{"name":"Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa"},{"name":"Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa"},{"name":"South African Medical Research Council Drug Discovery and Development Research Unit, Department of Chemistry University of Cape Town, Rondebosch 7701, South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2020,12,15]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"1493","DOI":"10.3389\/fimmu.2018.01493","article-title":"Human kinetoplastic protozoan infections: Where are we going next?","volume":"9","author":"Filardy","year":"2018","journal-title":"Front. 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