{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,12]],"date-time":"2025-10-12T01:34:43Z","timestamp":1760232883030,"version":"build-2065373602"},"reference-count":41,"publisher":"MDPI AG","issue":"12","license":[{"start":{"date-parts":[[2022,12,2]],"date-time":"2022-12-02T00:00:00Z","timestamp":1669939200000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Pharmaceuticals"],"abstract":"<jats:p>MMV\u2019s Malaria Box compound MMV030666 shows multi-stage activity against various strains of Plasmodium falciparum and lacks resistance development. To evaluate the importance of its diarylether partial structure, diarylthioethers and diphenylamines with varying substitution patterns were prepared. A number of evident structure-activity relationships were revealed. Physicochemical and pharmacokinetic parameters were determined experimentally (passive permeability) or calculated. Compared to the lead compound a diarylthioether was more active and less cytotoxic resulting in an excellent selectivity index of 850. In addition, pharmacokinetic and physicochemical parameters were improved.<\/jats:p>","DOI":"10.3390\/ph15121503","type":"journal-article","created":{"date-parts":[[2022,12,2]],"date-time":"2022-12-02T03:00:36Z","timestamp":1669950036000},"page":"1503","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":3,"title":["New Derivatives of the Multi-Stage Active Malaria Box Compound MMV030666 and Their Antiplasmodial Potencies"],"prefix":"10.3390","volume":"15","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-5267-7852","authenticated-orcid":false,"given":"Theresa","family":"Hermann","sequence":"first","affiliation":[{"name":"Pharmaceutical Chemistry, Institute of Pharmaceutical Sciences, University of Graz, Schubertstra\u00dfe 1, 8010 Graz, Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Robin","family":"Wallner","sequence":"additional","affiliation":[{"name":"Pharmaceutical Chemistry, Institute of Pharmaceutical Sciences, University of Graz, Schubertstra\u00dfe 1, 8010 Graz, Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Johanna","family":"Dolensky","sequence":"additional","affiliation":[{"name":"Pharmaceutical Chemistry, Institute of Pharmaceutical Sciences, University of Graz, Schubertstra\u00dfe 1, 8010 Graz, Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-5673-0470","authenticated-orcid":false,"given":"Werner","family":"Seebacher","sequence":"additional","affiliation":[{"name":"Pharmaceutical Chemistry, Institute of Pharmaceutical Sciences, University of Graz, Schubertstra\u00dfe 1, 8010 Graz, Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8327-0732","authenticated-orcid":false,"given":"Eva-Maria","family":"Pferschy-Wenzig","sequence":"additional","affiliation":[{"name":"Pharmacognosy, Institute of Pharmaceutical Sciences, University of Graz, Beethovenstra\u00dfe 8, 8010 Graz, Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1785-7302","authenticated-orcid":false,"given":"Marcel","family":"Kaiser","sequence":"additional","affiliation":[{"name":"Swiss Tropical and Public Health Institute, Kreuzstra\u00dfe 2, Allschwil, CH-4123 Basel, Switzerland"},{"name":"Faculty of Philosophy and Natural Sciences, Swiss Tropical and Public Health Institute Petersplatz 1, University of Basel, CH-4003 Basel, Switzerland"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-3122-1941","authenticated-orcid":false,"given":"Pascal","family":"M\u00e4ser","sequence":"additional","affiliation":[{"name":"Swiss Tropical and Public Health Institute, Kreuzstra\u00dfe 2, Allschwil, CH-4123 Basel, Switzerland"},{"name":"Faculty of Philosophy and Natural Sciences, Swiss Tropical and Public Health Institute Petersplatz 1, University of Basel, CH-4003 Basel, Switzerland"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-7174-6673","authenticated-orcid":false,"given":"Robert","family":"Weis","sequence":"additional","affiliation":[{"name":"Pharmaceutical Chemistry, Institute of Pharmaceutical Sciences, University of Graz, Schubertstra\u00dfe 1, 8010 Graz, Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2022,12,2]]},"reference":[{"key":"ref_1","unstructured":"WHO (2021). 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