Discovery of a potent dual inhibitor of wild-type and mutant respiratory syncytial virus fusion proteins through the modulation of atropisomer interconversion properties.

doi:10.1016/j.bmc.2020.115818

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Article

Discovery of a potent dual inhibitor of wild-type and mutant respiratory syncytial virus fusion proteins through the modulation of atropisomer interconversion properties.

Bioorganic & medicinal chemistry - 15 Dec 2020

Yamaguchi-Sasaki Toru, Kawaguchi Takanori, Okada Atsushi, Tokura Seiken, Tanaka-Yamamoto Nozomi, Takeuchi Tomoki, Ogata Yuya, Takahashi Ryo, Kurimoto-Tsuruta Risa, Tamaoki Tomokazu, Sugaya Yutaka, Abe-Kumasaka Tomoko, Arikawa Kaho, Yoshida Ippei, Sugiyama Hiroyuki, Kanuma Kosuke, Yoshinaga Mitsukane

Abstract excerpt

The development of effective respiratory syncytial virus (RSV) fusion glycoprotein (F protein) inhibitors against both wild-type and the D486N-mutant F protein is urgently required. We recently reported a 15-membered macrocyclic pyrazolo[1,5-a]pyrimidine derivative 4 that exhibited potent anti-RSV activities against not only wild-type, but also D486N-mutant F protein. However, NMR studies revealed that the...

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PMID: 33190073
DOI: 10.1016/j.bmc.2020.115818

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