Dataset Information

Design, Synthesis, and Biological Evaluation of EdAP, a 4'-Ethynyl-2'-Deoxyadenosine 5'-Monophosphate Analog, as a Potent Influenza a Inhibitor.

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 ?2-6-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.

SUBMITTER: Takeuchi T

PROVIDER: S-EPMC6681032 | biostudies-literature | 2019 Jul

REPOSITORIES: biostudies-literature

ACCESS DATA

Publications

Design, Synthesis, and Biological Evaluation of EdAP, a 4'-Ethynyl-2'-Deoxyadenosine 5'-Monophosphate Analog, as a Potent Influenza a Inhibitor.

Takeuchi Toshifumi T Sriwilaijaroen Nongluk N Sakuraba Ayako A Hayashi Ei E Kamisuki Shinji S Suzuki Yasuo Y Ohrui Hiroshi H Sugawara Fumio F

Molecules (Basel, Switzerland) 20190717 14

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 (<b>5</b>). EdAP exhibited ...[more]

PMID: 31319565

Dataset Information

Design, Synthesis, and Biological Evaluation of EdAP, a 4'-Ethynyl-2'-Deoxyadenosine 5'-Monophosphate Analog, as a Potent Influenza a Inhibitor.

Publications

Design, Synthesis, and Biological Evaluation of EdAP, a 4'-Ethynyl-2'-Deoxyadenosine 5'-Monophosphate Analog, as a Potent Influenza a Inhibitor.

Similar Datasets

OmicsDI is part of the ELIXIR infrastructure

Tweets

Similar Datasets

4'-Ethynyl-2-fluoro-2'-deoxyadenosine, MK-8591: a novel HIV-1 reverse transcriptase translocation inhibitor.
| S-EPMC6449048 | biostudies-literature

Structural basis of HIV inhibition by translocation-defective RT inhibitor 4'-ethynyl-2-fluoro-2'-deoxyadenosine (EFdA).
| S-EPMC4995989 | biostudies-literature

Design, synthesis and initial biological evaluation of a novel pladienolide analog scaffold.
| S-EPMC3171832 | biostudies-literature

Design, synthesis, and biological evaluation of potent FAK-degrading PROTACs.
| S-EPMC9455338 | biostudies-literature

Design, Synthesis and Biological Evaluation of Highly Potent Simplified Archazolids.
| S-EPMC7496434 | biostudies-literature

Design of a novel nucleoside analog as potent inhibitor of the NAD dependent deacetylase, SIRT2.
| S-EPMC3065595 | biostudies-literature

Design, synthesis and characterization of a highly effective inhibitor for analog-sensitive (as) kinases.
| S-EPMC3117834 | biostudies-literature

Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors.
| S-EPMC7125537 | biostudies-literature

Design and synthesis of benzenesulfonamide derivatives as potent anti-influenza hemagglutinin inhibitors.
| S-EPMC4018120 | biostudies-literature

Synthesis and biological evaluation of a phosphonate analog of the natural acetyl cholinesterase inhibitor cyclophostin.
| S-EPMC2726048 | biostudies-literature