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The compounds were screened in\u2005vitro against <jats:italic>Plasmodium falciparum<\/jats:italic> (<jats:italic>Pf<\/jats:italic>) and <jats:italic>Mycobacterium tuberculosis<\/jats:italic> (<jats:italic>Mtb<\/jats:italic>). Antimalarial activities (IC<jats:sub>50<\/jats:sub>) against <jats:italic>Pf<\/jats:italic> drug\u2010sensitive NF54, and drug\u2010resistant K1 and W2 strains ranged from 0.03\u20132.6, 0.03\u20131.9, and 0.02\u20131.7\u2005\u03bc<jats:sc>m<\/jats:sc>. Although the compounds are less active than the precursor artemisinin derivatives, the cholesterol moiety renders the compounds relatively insoluble in the culture medium, and variation in solubilities among the different compounds may reflect in the range of efficacies observed. Activities against <jats:italic>Mtb<\/jats:italic> H37Rv were assessed using a standardized colony\u2010forming unit (CFU) assay after 24\u2005h pretreatment of cultures with each of the compounds. Percentage inhibition ranged from 3\u201338\u2009% and 18\u201352\u2009% at 10 and 80\u2005\u03bc<jats:sc>m<\/jats:sc>, respectively. Thus, in contrast to the comparator drug artemether, the conjugates display enhanced activities. The immediate aims include the preparation of conjugates with enhanced aqueous solubilities, assays against malaria and TB in\u2005vivo, and for TB, assays using an infected macrophage model and assessment of granuloma influx.<\/jats:p>","DOI":"10.1002\/cmdc.201700579","type":"journal-article","created":{"date-parts":[[2017,11,29]],"date-time":"2017-11-29T10:39:30Z","timestamp":1511951970000},"page":"67-77","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":18,"title":["Preliminary Evaluation of Artemisinin\u2013Cholesterol Conjugates as Potential Drugs for the Treatment of Intractable Forms of Malaria and Tuberculosis"],"prefix":"10.1002","volume":"13","author":[{"given":"Mokhitli","family":"Morake","sequence":"first","affiliation":[{"name":"Centre of Excellence for Pharmaceutical Sciences, Faculty of Health Sciences North-West University  Potchefstroom 2520 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Dina","family":"Coertzen","sequence":"additional","affiliation":[{"name":"Department of Biochemistry, Centre for Sustainable Malaria Control University of Pretoria  Private Bag X20 Hatfield 0028 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Andile","family":"Ngwane","sequence":"additional","affiliation":[{"name":"DST\/NRF Centre of Excellence for Biomedical Tuberculosis Research, MRC Centre for Molecular and Cellular Biology, Division of Molecular Biology and Human Genetics, Faculty of Medicine and Health Sciences Stellenbosch University  Tygerberg 7505 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Johannes F.","family":"Wentzel","sequence":"additional","affiliation":[{"name":"Centre of Excellence for Pharmaceutical Sciences, Faculty of Health Sciences North-West University  Potchefstroom 2520 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ho Ning","family":"Wong","sequence":"additional","affiliation":[{"name":"Centre of Excellence for Pharmaceutical Sciences, Faculty of Health 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, Faculty of Health Sciences North-West University  Potchefstroom 2520 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lyn\u2010Marie","family":"Birkholtz","sequence":"additional","affiliation":[{"name":"Department of Biochemistry, Centre for Sustainable Malaria Control University of Pretoria  Private Bag X20 Hatfield 0028 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ray\u2010Dean","family":"Pietersen","sequence":"additional","affiliation":[{"name":"DST\/NRF Centre of Excellence for Biomedical Tuberculosis Research, MRC Centre for Molecular and Cellular Biology, Division of Molecular Biology and Human Genetics, Faculty of Medicine and Health Sciences Stellenbosch University  Tygerberg 7505 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Bienyameen","family":"Baker","sequence":"additional","affiliation":[{"name":"DST\/NRF Centre of Excellence for Biomedical Tuberculosis Research, MRC Centre for Molecular and Cellular Biology, Division of Molecular Biology and Human Genetics, Faculty of Medicine and Health Sciences Stellenbosch University  Tygerberg 7505 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ian","family":"Wiid","sequence":"additional","affiliation":[{"name":"DST\/NRF Centre of Excellence for Biomedical Tuberculosis Research, MRC Centre for Molecular and Cellular Biology, Division of Molecular Biology and Human Genetics, Faculty of Medicine and Health Sciences Stellenbosch University  Tygerberg 7505 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"David D.","family":"N'Da","sequence":"additional","affiliation":[{"name":"Centre of Excellence for Pharmaceutical Sciences, Faculty of Health Sciences North-West University  Potchefstroom 2520 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Richard K.","family":"Haynes","sequence":"additional","affiliation":[{"name":"Centre of Excellence for Pharmaceutical Sciences, Faculty of Health Sciences North-West University  Potchefstroom 2520 South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2017,12,15]]},"reference":[{"key":"e_1_2_7_1_1","unstructured":"WHO World Malaria Report 2015 http:\/\/www.who.int\/malaria\/publications\/world-malaria-report-2015\/report\/en\/ 2015 (accessed September 22 2016); 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