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Structural Modifica...
Structural Modifications and Biological Evaluations of Rift Valley Fever Virus Inhibitors Identified from Chemical Library Screening
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- Islam, Koushikul, 1985- (author)
- Umeå universitet,Institutionen för klinisk mikrobiologi
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- Carlsson, Marcus (author)
- Umeå universitet,Kemiska institutionen
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- Enquist, Per-Anders (author)
- Umeå universitet,Kemiska institutionen
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- Qian, Weixing (author)
- Umeå universitet,Kemiska institutionen
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- Marttila, Marko (author)
- Umeå universitet,Institutionen för klinisk mikrobiologi
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- Strand, Mårten, 1982- (author)
- Umeå universitet,Institutionen för klinisk mikrobiologi
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- Ahlm, Clas, 1956- (author)
- Umeå universitet,Institutionen för klinisk mikrobiologi
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- Evander, Magnus (author)
- Umeå universitet,Institutionen för klinisk mikrobiologi
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(creator_code:org_t)
- 2022-02-16
- 2022
- English.
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In: ACS Omega. - : American Chemical Society (ACS). - 2470-1343. ; 7:8, s. 6854-6868
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Abstract
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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.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinsk bioteknologi -- Medicinsk bioteknologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Medical Biotechnology -- Medical Biotechnology (hsv//eng)
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- ref (subject category)
- art (subject category)
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ACS Omega
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Islam, Koushikul ...
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Carlsson, Marcus
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Enquist, Per-And ...
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Qian, Weixing
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Marttila, Marko
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Strand, Mårten, ...
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show more...
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Ahlm, Clas, 1956 ...
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Evander, Magnus
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- About the subject
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Medical Biotechn ...
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and Medical Biotechn ...
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ACS Omega
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Umeå University