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Structural Modifica...
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Islam, Koushikul,1985-Umeå universitet,Institutionen för klinisk mikrobiologi
(author)
Structural Modifications and Biological Evaluations of Rift Valley Fever Virus Inhibitors Identified from Chemical Library Screening
- Article/chapterEnglish2022
Publisher, publication year, extent ...
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2022-02-16
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American Chemical Society (ACS),2022
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electronicrdacarrier
Numbers
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LIBRIS-ID:oai:DiVA.org:umu-192961
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https://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-192961URI
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https://doi.org/10.1021/acsomega.1c06513DOI
Supplementary language notes
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Language:English
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Summary in:English
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Subject category:ref swepub-contenttype
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Subject category:art swepub-publicationtype
Notes
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The Rift Valley fever virus (RVFV) is an emerging high-priority pathogen endemic in Africa with pandemic potential. There is no specific treatment or approved antiviral drugs for the RVFV. We previously developed a cell-based high-throughput assay to screen small molecules targeting the RVFV and identified a potential effective antiviral compound (1-N-(2-(biphenyl-4-yloxy)ethyl)propane-1,3-diamine) as a lead compound. Here, we investigated how structural modifications of the lead compound affected the biological properties and the antiviral effect against the RVFV. We found that the length of the 2-(3-aminopropylamino)ethyl chain of the compound was important for the compound to retain its antiviral activity. The antiviral activity was similar when the 2-(3-aminopropylamino)ethyl chain was replaced with a butyl piperazine chain. However, we could improve the cytotoxicity profile of the lead compound by changing the phenyl piperazine linker from the para-position (compound 9a) to the meta-position (compound 13a). Results from time-of-addition studies suggested that compound 13a might be active during virus post-entry and/or the replication phase of the virus life cycle and seemed to affect the K+ channel. The modifications improved the properties of our lead compound, and our data suggest that 13a is a promising candidate to evaluate further as a therapeutic agent for RVFV infection.
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Carlsson, MarcusUmeå universitet,Kemiska institutionen(Swepub:umu)mascan97
(author)
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Enquist, Per-AndersUmeå universitet,Kemiska institutionen(Swepub:umu)peen0006
(author)
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Qian, WeixingUmeå universitet,Kemiska institutionen(Swepub:umu)weqi0002
(author)
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Marttila, MarkoUmeå universitet,Institutionen för klinisk mikrobiologi(Swepub:umu)maomaa00
(author)
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Strand, Mårten,1982-Umeå universitet,Institutionen för klinisk mikrobiologi(Swepub:umu)mansnd02
(author)
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Ahlm, Clas,1956-Umeå universitet,Institutionen för klinisk mikrobiologi(Swepub:umu)clah0001
(author)
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Evander, MagnusUmeå universitet,Institutionen för klinisk mikrobiologi(Swepub:umu)maev0001
(author)
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Umeå universitetInstitutionen för klinisk mikrobiologi
(creator_code:org_t)
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In:ACS Omega: American Chemical Society (ACS)7:8, s. 6854-68682470-1343
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