Molecules, Vol. 24, Pages 2603: Design, Synthesis, and Biological Evaluation of EdAP, a 4 ′-Ethynyl-2′-Deoxyadenosine 5′-Monophosphate Analog, as a Potent Influenza a Inhibitor

Molecules, Vol. 24, Pages 2603: Design, Synthesis, and Biological Evaluation of EdAP, a 4′-Ethynyl-2′-Deoxyadenosine 5′-Monophosphate Analog, as a Potent Influenza a Inhibitor Molecules doi: 10.3390/molecules24142603 Authors: Toshifumi Takeuchi Nongluk Sriwilaijaroen Ayako Sakuraba Ei Hayashi Shinji Kamisuki Yasuo Suzuki Hiroshi Ohrui Fumio Sugawara 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.
Source: Molecules - Category: Chemistry Authors: Tags: Article Source Type: research