863578-58-9Relevant academic research and scientific papers
Syntheses and initial evaluation of a series of indolo-fused heterocyclic inhibitors of the polymerase enzyme (NS5B) of the hepatitis C virus
Zheng, Xiaofan,Hudyma, Thomas W.,Martin, Scott W.,Bergstrom, Carl,Ding, Min,He, Feng,Romine, Jeffrey,Poss, Michael A.,Kadow, John F.,Chang, Chong-Hwan,Wan, John,Witmer, Mark R.,Morin, Paul,Camac, Daniel M.,Sheriff, Steven,Beno, Brett R.,Rigat, Karen L.,Wang, Ying-Kai,Fridell, Robert,Lemm, Julie,Qiu, Dike,Liu, Mengping,Voss, Stacey,Pelosi, Lenore,Roberts, Susan B.,Gao, Min,Knipe, Jay,Gentles, Robert G.
, p. 2925 - 2929 (2011/06/26)
Herein, we present initial SAR studies on a series of bridged 2-arylindole-based NS5B inhibitors. The introduction of bridging elements between the indole N1 and the ortho-position of the 2-aryl moiety resulted in conformationally constrained heterocycles
INHIBITORS OF HCV REPLICATION
-
Page/Page column 76, (2010/11/28)
Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Different forms and compositions comprising the compounds are also described as well as methods of
Discovery of conformationally constrained tetracyclic compounds as potent hepatitis C virus NS5B RNA polymerase inhibitors
Ikegashira, Kazutaka,Oka, Takahiro,Hirashima, Shintaro,Noji, Satoru,Yamanaka, Hiroshi,Hara, Yoshinori,Adachi, Tsuyoshi,Tsuruha, Jun-Ichiro,Doi, Satoki,Hase, Yasunori,Noguchi, Toru,Ando, Izuru,Ogura, Naoki,Ikeda, Satoru,Hashimoto, Hiromasa
, p. 6950 - 6953 (2007/10/03)
We report a new series of hepatitis C virus NS5B RNA polymerase inhibitors containing a conformationally constrained tetracyclic scaffold. SAR studies led to the identification of 6,7-dihydro-5H-benzo[5,6][1,4]diazepino[7,1-a]indoles (19 and 20) bearing a basic pendent group with high biochemical and cellular potencies. These compounds displayed a very small shift in cellular potency when the replicon assay was performed in the presence of human serum albumin.
Inhibitors of HCV replication
-
Page/Page column 45, (2010/10/20)
Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Different forms and compositions comprising the compounds are also described as well as methods of preparing the compounds.
