ACS Medicinal Chemistry Letters p. 244 - 248 (2014)
Update date:2022-08-03
Topics:
Chen, Kevin X.
Venkatraman, Srikanth
Anilkumar, Gopinadhan N.
Zeng, Qingbei
Lesburg, Charles A.
Vibulbhan, Bancha
Velazquez, Francisco
Chan, Tin-Yau
Bennet, Frank
Jiang, Yueheng
Pinto, Patrick
Huang, Yuhua
Selyutin, Oleg
Agrawal, Sony
Huang, Hsueh-Cheng
Li, Cheng
Cheng, Kuo-Chi
Shih, Neng-Yang
Kozlowski, Joseph A.
Rosenblum, Stuart B.
Njoroge, F. George
Starting from indole-based hepatitis C virus (HCV) NS5B polymerase inhibitor lead compound 1, structure modifications were performed at multiple indole substituents to improve potency and pharmacokinetic (PK) properties. Bicyclic quinazolinone was found to be the best substituent at indole nitrogen, while 4,5-furanylindole was identified as the best core. Compound 11 demonstrated excellent potency. Its C2 N,N-dimethylaminoethyl ester prodrug 12 (SCH 900188) demonstrated significant improvement in PK and was selected as the development candidate.
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