{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,12]],"date-time":"2025-10-12T01:57:07Z","timestamp":1760234227675,"version":"build-2065373602"},"reference-count":51,"publisher":"MDPI AG","issue":"5","license":[{"start":{"date-parts":[[2021,4,27]],"date-time":"2021-04-27T00:00:00Z","timestamp":1619481600000},"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>An N-acylated furazan-3-amine of a Medicines for Malaria Venture (MMV) project has shown activity against different strains of Plasmodium falciparum. Seventeen new derivatives were prepared and tested in vitro for their activities against blood stages of two strains of Plasmodium falciparum. Several structure\u2013activity relationships were revealed. The activity strongly depended on the nature of the acyl moiety. Only benzamides showed promising activity. The substitution pattern of their phenyl ring affected the activity and the cytotoxicity of compounds. In addition, physicochemical parameters were calculated (log P, log D, ligand efficiency) or determined experimentally (permeability) via a PAMPA. The N-(4-(3,4-diethoxyphenyl)-1,2,5-oxadiazol-3-yl)-3-(trifluoromethyl)benzamide possessed good physicochemical properties and showed high antiplasmodial activity against a chloroquine-sensitive strain (IC50(NF54) = 0.019 \u00b5M) and even higher antiplasmodial activity against a multiresistant strain (IC50(K1) = 0.007 \u00b5M). Compared to the MMV compound, the permeability and the activity against the multiresistant strain were improved.<\/jats:p>","DOI":"10.3390\/ph14050412","type":"journal-article","created":{"date-parts":[[2021,4,27]],"date-time":"2021-04-27T21:18:20Z","timestamp":1619558300000},"page":"412","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":3,"title":["New Acyl Derivatives of 3-Aminofurazanes and Their Antiplasmodial Activities"],"prefix":"10.3390","volume":"14","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-5267-7852","authenticated-orcid":false,"given":"Theresa","family":"Hermann","sequence":"first","affiliation":[{"name":"Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Schubertstra\u00dfe 1, A-8010 Graz, Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-3995-2186","authenticated-orcid":false,"given":"Patrick","family":"Hochegger","sequence":"additional","affiliation":[{"name":"Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Schubertstra\u00dfe 1, A-8010 Graz, Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Johanna","family":"Dolensky","sequence":"additional","affiliation":[{"name":"Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Schubertstra\u00dfe 1, A-8010 Graz, Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Werner","family":"Seebacher","sequence":"additional","affiliation":[{"name":"Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Schubertstra\u00dfe 1, A-8010 Graz, Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Robert","family":"Saf","sequence":"additional","affiliation":[{"name":"Institute for Chemistry and Technology of Materials (ICTM), Graz University of Technology, Stremayrgasse 9, A-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, Socinstra\u00dfe 57, CH-4002 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, Socinstra\u00dfe 57, CH-4002 Basel, Switzerland"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Robert","family":"Weis","sequence":"additional","affiliation":[{"name":"Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Schubertstra\u00dfe 1, A-8010 Graz, Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2021,4,27]]},"reference":[{"key":"ref_1","unstructured":"WHO (2020). 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