TY - JOUR
T1 - (S)- N -(2,5-Dimethylphenyl)-1-(quinoline-8-ylsulfonyl)pyrrolidine-2- carboxamide as a small molecule inhibitor probe for the study of respiratory syncytial virus infection
AU - Moore, Blake P.
AU - Chung, Dong Hoon
AU - Matharu, Daljit S.
AU - Golden, Jennifer E.
AU - Maddox, Clinton
AU - Rasmussen, Lynn
AU - Noah, James W.
AU - Sosa, Melinda I.
AU - Ananthan, Subramaniam
AU - Tower, Nichole A.
AU - White, E. Lucile
AU - Jia, Fuli
AU - Prisinzano, Thomas E.
AU - Aubé, Jeffrey
AU - Jonsson, Colleen B.
AU - Severson, William E.
PY - 2012/10/25
Y1 - 2012/10/25
N2 - A high-throughput, cell-based screen was used to identify chemotypes as inhibitors for human respiratory syncytial virus (hRSV). Optimization of a sulfonylpyrrolidine scaffold resulted in compound 5o that inhibited a virus-induced cytopathic effect in the entry stage of infection (EC50 = 2.3 ± 0.8 μM) with marginal cytotoxicity (CC50 = 30.9 ± 1.1 μM) and reduced viral titer by 100-fold. Compared to ribavirin, sulfonylpyrrolidine 5o demonstrated an improved in vitro potency and selectivity index.
AB - A high-throughput, cell-based screen was used to identify chemotypes as inhibitors for human respiratory syncytial virus (hRSV). Optimization of a sulfonylpyrrolidine scaffold resulted in compound 5o that inhibited a virus-induced cytopathic effect in the entry stage of infection (EC50 = 2.3 ± 0.8 μM) with marginal cytotoxicity (CC50 = 30.9 ± 1.1 μM) and reduced viral titer by 100-fold. Compared to ribavirin, sulfonylpyrrolidine 5o demonstrated an improved in vitro potency and selectivity index.
UR - https://www.scopus.com/pages/publications/84867769390
UR - https://www.scopus.com/pages/publications/84867769390#tab=citedBy
U2 - 10.1021/jm300612z
DO - 10.1021/jm300612z
M3 - Article
C2 - 23043370
AN - SCOPUS:84867769390
SN - 0022-2623
VL - 55
SP - 8582
EP - 8587
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 20
ER -