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This induction of quiescence is linked to artemisinin resistance. Thus, we have turned to structurally disparate artemisinins that are incapable of providing DHA on metabolism. Accordingly, 11\u2010azaartemisinin <jats:bold>5<\/jats:bold> and selected <jats:italic>N<\/jats:italic>\u2010sulfonyl derivatives were screened against intraerythrocytic asexual stages of drug\u2010sensitive <jats:italic>Pf<\/jats:italic> NF54 and drug\u2010resistant K1 and W2 parasites. Most displayed appreciable activities against all three strains, with IC<jats:sub>50<\/jats:sub> values &lt;10.5\u2005n<jats:sc>m<\/jats:sc>. The <jats:italic>p<\/jats:italic>\u2010trifluoromethylbenzenesulfonyl\u201011\u2010azaartemisinin derivative <jats:bold>11<\/jats:bold> [(4\u2032\u2010trifluoromethyl)benzenesulfonylazaartemisinin] was the most active, with IC<jats:sub>50<\/jats:sub> values between 2 and 3\u2005n<jats:sc>m<\/jats:sc>. The compounds were screened against <jats:italic>Pf<\/jats:italic> NF54 early and transmissible late intraerythrocytic\u2010stage gametocytes using luciferase and parasite lactate dehydrogenase (pLDH) assays. The 2\u2032\u2010thienylsulfonyl derivative <jats:bold>16<\/jats:bold> (2\u2032\u2010thiophenesulfonylazaartemisinin) was notably active against late\u2010stage (IV\u2013V) gametocytes with an IC<jats:sub>50<\/jats:sub> value of 8.7\u2005n<jats:sc>m<\/jats:sc>. All compounds were relatively nontoxic to human fetal lung WI\u201038 fibroblasts, showing selectivity indices of &gt;2000 toward asexual parasites. Overall, the readily accessible 11\u2010azaartemisinin <jats:bold>5<\/jats:bold> and the sulfonyl derivatives <jats:bold>11<\/jats:bold> and <jats:bold>16<\/jats:bold> represent potential candidates for further development, in particular for transmission blocking of artemisinin\u2010resistant parasites.<\/jats:p>","DOI":"10.1002\/cmdc.201700599","type":"journal-article","created":{"date-parts":[[2017,12,8]],"date-time":"2017-12-08T05:36:46Z","timestamp":1512711406000},"page":"2086-2093","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":20,"title":["Activities of 11\u2010Azaartemisinin and <i>N<\/i>\u2010Sulfonyl Derivatives against Asexual and Transmissible Malaria Parasites"],"prefix":"10.1002","volume":"12","author":[{"given":"Rozanne","family":"Harmse","sequence":"first","affiliation":[{"name":"Centre of Excellence for Pharmaceutical Sciences North-West University  Potchefstroom 2520 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Dina","family":"Coertzen","sequence":"additional","affiliation":[{"name":"Department of Biochemistry Institute for Sustainable Malaria Control University of Pretoria  Pretoria 0002 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ho Ning","family":"Wong","sequence":"additional","affiliation":[{"name":"Centre of Excellence for Pharmaceutical Sciences North-West University  Potchefstroom 2520 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Frans J.","family":"Smit","sequence":"additional","affiliation":[{"name":"Centre of Excellence for Pharmaceutical Sciences North-West University  Potchefstroom 2520 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mariette E.","family":"van\u2005der\u2005Watt","sequence":"additional","affiliation":[{"name":"Department of Biochemistry Institute for Sustainable Malaria Control University of Pretoria  Pretoria 0002 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Janette","family":"Reader","sequence":"additional","affiliation":[{"name":"Department of Biochemistry Institute for Sustainable Malaria Control University of Pretoria  Pretoria 0002 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sindiswe H.","family":"Nondaba","sequence":"additional","affiliation":[{"name":"Department of Biochemistry Institute for Sustainable Malaria Control University of Pretoria  Pretoria 0002 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lyn\u2010Marie","family":"Birkholtz","sequence":"additional","affiliation":[{"name":"Department of Biochemistry Institute for Sustainable Malaria Control University of Pretoria  Pretoria 0002 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Richard K.","family":"Haynes","sequence":"additional","affiliation":[{"name":"Centre of Excellence for Pharmaceutical Sciences North-West University  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 North-West University  Potchefstroom 2520 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2017,12,8]]},"reference":[{"key":"e_1_2_7_1_1","unstructured":"World Malaria Report 2016 World Health Organization (WHO) Geneva (Switzerland) ISBN: 978\u2005924\u20051511711;http:\/\/www.who.int\/malaria\/publications\/world-malaria-report-2016\/report\/en\/(accessed November 29 2017)."},{"key":"e_1_2_7_2_1","unstructured":"\u00a0"},{"key":"e_1_2_7_3_2","doi-asserted-by":"publisher","DOI":"10.1086\/322858"},{"key":"e_1_2_7_4_2","doi-asserted-by":"publisher","DOI":"10.1038\/nature00813"},{"key":"e_1_2_7_5_2","doi-asserted-by":"publisher","DOI":"10.1016\/S1473-3099(02)00239-6"},{"key":"e_1_2_7_6_2","doi-asserted-by":"publisher","DOI":"10.1126\/science.1098876"},{"key":"e_1_2_7_7_1","unstructured":"\u00a0"},{"key":"e_1_2_7_8_2","first-page":"811","volume":"92","author":"Research Qinghaosu Antimalaria Coordinating","year":"1979","journal-title":"Chin. 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