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- Title
Design, Synthesis, and Biological Evaluation of EdAP, a 4′-Ethynyl-2′-Deoxyadenosine 5′-Monophosphate Analog, as a Potent Influenza a Inhibitor.
- Authors
Takeuchi, Toshifumi; Sriwilaijaroen, Nongluk; Sakuraba, Ayako; Hayashi, Ei; Kamisuki, Shinji; Suzuki, Yasuo; Ohrui, Hiroshi; Sugawara, Fumio
- Abstract
Influenza A viruses leading to infectious respiratory diseases cause seasonal epidemics and sometimes periodic global pandemics. Viral polymerase is an attractive target in inhibiting viral replication, and 4′-ethynyladenosine, which has been reported as a highly potent anti-human immunodeficiency virus (HIV) nucleoside derivative, can work as an anti-influenza agent. Herein, we designed and synthesized a 4′-ethynyl-2′-deoxyadenosine 5′-monophosphate analog called EdAP (5). EdAP exhibited potent inhibition against influenza virus multiplication in Madin–Darby canine kidney (MDCK) cells transfected with human α2-6-sialyltransferase (SIAT1) cDNA and did not show any toxicity toward the cells. Surprisingly, this DNA-type nucleic acid analog (5) inhibited the multiplication of influenza A virus, although influenza virus is an RNA virus that does not generate DNA.
- Subjects
NEURAMINIDASE; INFLUENZA viruses; RESPIRATORY diseases; RNA viruses; INFLUENZA; NUCLEOSIDE derivatives
- Publication
Molecules, 2019, Vol 24, Issue 14, p2603
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules24142603