Discovery of 3‑({5-Chloro-1-[3-(methylsulfonyl)propyl]‑1H‑indol-2-yl}methyl)-1-(2,2,2-trifluoroethyl)-1,3-dihydro‑2H‑imidazo[4,5‑c]pyridin-2-one
(JNJ-53718678), a Potent and Orally Bioavailable Fusion Inhibitor
of Respiratory Syncytial Virus
Posted on 2020-06-15 - 16:06
Respiratory
syncytial virus (RSV) is a seasonal virus that infects
the lungs and airways of 64 million children and adults every year.
It is a major cause of acute lower respiratory tract infection and
is associated with significant morbidity and mortality. Despite the
large medical and economic burden, treatment options for RSV-associated
bronchiolitis and pneumonia are limited and mainly consist of supportive
care. This publication covers the medicinal chemistry efforts resulting
in the identification of JNJ-53718678, an orally bioavailable RSV
inhibitor that was shown to be efficacious in a phase 2a challenge
study in healthy adult subjects and that is currently being evaluated
in hospitalized infants and adults. Cocrystal structures of several
new derivatives helped in rationalizing some of the structure–activity
relationship (SAR) trends observed.
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Vendeville, Sandrine; Tahri, Abdellah; Hu, Lili; Demin, Samuel; Cooymans, Ludwig; Vos, Ann; et al. (2020). Discovery of 3‑({5-Chloro-1-[3-(methylsulfonyl)propyl]‑1H‑indol-2-yl}methyl)-1-(2,2,2-trifluoroethyl)-1,3-dihydro‑2H‑imidazo[4,5‑c]pyridin-2-one
(JNJ-53718678), a Potent and Orally Bioavailable Fusion Inhibitor
of Respiratory Syncytial Virus. ACS Publications. Collection. https://doi.org/10.1021/acs.jmedchem.0c00226