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dc.contributor.authorCesur, Nesrin
dc.contributor.authorNAESENS, Lieve
dc.contributor.authorCesur, Zafer
dc.contributor.authorSTEVAERT, Annelies
dc.contributor.authorApaydin, Cagla Begum
dc.date.accessioned2021-03-04T11:50:22Z
dc.date.available2021-03-04T11:50:22Z
dc.date.issued2019
dc.identifier.citationApaydin C. B. , Cesur N., STEVAERT A., NAESENS L., Cesur Z., "Synthesis and anti-coronavirus activity of a series of 1-thia-4-azaspiro[4.5]decan-3-one derivatives", ARCHIV DER PHARMAZIE, cilt.352, sa.6, 2019
dc.identifier.issn0365-6233
dc.identifier.othervv_1032021
dc.identifier.otherav_745a712b-ea76-430c-aee9-9b1638bb91e5
dc.identifier.urihttp://hdl.handle.net/20.500.12627/79973
dc.identifier.urihttps://doi.org/10.1002/ardp.201800330
dc.description.abstractA series of 1-thia-4-azaspiro[4.5]decan-3-ones bearing an amide group at C-4 and various substitutions at C-2 and C-8 were synthesized and evaluated against human coronavirus and influenza virus. Compounds 7m, 7n, 8k, 8l, 8m, 8n, and 8p were found to inhibit human coronavirus 229E replication. The most active compound was N-(2-methyl-8-tert-butyl-3-oxo-1-thia-4-azaspiro[4.5]decan-4-yl)-3-phenylpropanamide (8n), with an EC50 value of 5.5 mu M, comparable to the known coronavirus inhibitor, (Z)-N-[3-[4-(4-bromophenyl)-4-hydroxypiperidin-1-yl]-3-oxo-1-phenylprop-1-en-2-yl]benzamide (K22). Compound 8n and structural analogs were devoid of anti-influenza virus activity, although their scaffold is shared with a previously discovered class of H3 hemagglutinin-specific influenza virus fusion inhibitors. These findings point to the 1-thia-4-azaspiro[4.5]decan-3-one scaffold as a versatile chemical structure with high relevance for antiviral drug development.
dc.language.isoeng
dc.subjectEczacılık
dc.subjectTemel Eczacılık Bilimleri
dc.subjectYaşam Bilimleri
dc.subjectBiyokimya
dc.subjectAlkoloidler
dc.subjectTemel Bilimler
dc.subjectFARMAKOLOJİ VE ECZACILIK
dc.subjectFarmakoloji ve Toksikoloji
dc.subjectYaşam Bilimleri (LIFE)
dc.subjectSağlık Bilimleri
dc.subjectKİMYA, MULTİDİSİPLİNER
dc.subjectTemel Bilimler (SCI)
dc.subjectKimya
dc.subjectKİMYA, TIP
dc.titleSynthesis and anti-coronavirus activity of a series of 1-thia-4-azaspiro[4.5]decan-3-one derivatives
dc.typeMakale
dc.relation.journalARCHIV DER PHARMAZIE
dc.contributor.departmentKU Leuven , ,
dc.identifier.volume352
dc.identifier.issue6
dc.contributor.firstauthorID100948


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