{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,7,30]],"date-time":"2026-07-30T11:49:41Z","timestamp":1785412181050,"version":"3.56.0"},"reference-count":19,"publisher":"Beilstein Institut","license":[{"start":{"date-parts":[[2023,1,31]],"date-time":"2023-01-31T00:00:00Z","timestamp":1675123200000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0"},{"start":{"date-parts":[[2023,1,31]],"date-time":"2023-01-31T00:00:00Z","timestamp":1675123200000},"content-version":"am","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0"},{"start":{"date-parts":[[2023,1,31]],"date-time":"2023-01-31T00:00:00Z","timestamp":1675123200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0"}],"funder":[{"DOI":"10.13039\/501100000925","name":"National Health and Medical Research Council","doi-asserted-by":"publisher","award":["APP1024314"],"award-info":[{"award-number":["APP1024314"]}],"id":[{"id":"10.13039\/501100000925","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Beilstein J. Org. Chem."],"accepted":{"date-parts":[[2023,1,13]]},"abstract":"<jats:p>\n                    Nine new fluorinated analogues were synthesised by late-stage functionalisation using Diversinate\u2122 chemistry on the Open Source Malaria (OSM) triazolopyrazine scaffold (Series 4). The structures of all analogues were fully characterised by NMR, UV and MS data analysis; three triazolopyrazines were confirmed by X-ray crystal structure analysis. The inhibitory activity of all compounds against the growth of the malaria parasite\n                    <jats:italic>Plasmodium falciparum<\/jats:italic>\n                    (3D7 and Dd2 strains) and the cytotoxicity against a human embryonic kidney (HEK293) cell line were tested. Some of the compounds demonstrated moderate antimalarial activity with IC\n                    <jats:sub>50<\/jats:sub>\n                    values ranging from 0.2 to &gt;80 \u00b5M; none of the compounds displayed any cytotoxicity against HEK293 cells at 80 \u00b5M. Antimalarial activity was significantly reduced when C-8 of the triazolopyrazine scaffold was substituted with CF\n                    <jats:sub>3<\/jats:sub>\n                    and CF\n                    <jats:sub>2<\/jats:sub>\n                    H moieties, whereas incorporation of a CF\n                    <jats:sub>2<\/jats:sub>\n                    Me group at the same position completely abolished antiplasmodial effects.\n                  <\/jats:p>","DOI":"10.3762\/bjoc.19.11","type":"journal-article","created":{"date-parts":[[2023,1,31]],"date-time":"2023-01-31T05:29:34Z","timestamp":1675142974000},"page":"107-114","source":"Crossref","is-referenced-by-count":4,"title":["Synthesis and characterisation of new antimalarial fluorinated triazolopyrazine compounds"],"prefix":"10.3762","volume":"19","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-9843-7814","authenticated-orcid":false,"given":"Kah 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