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  3. Further studies on hepatitis C virus NS5B RNA-dependent RNA polymerase inhibitors toward improved replicon cell activities: benzimidazole and structurally related compounds bearing the 2-morpholinophenyl moiety

Further studies on hepatitis C virus NS5B RNA-dependent RNA polymerase inhibitors toward improved replicon cell activities: benzimidazole and structurally related compounds bearing the 2-morpholinophenyl moiety

  • Bioorg Med Chem Lett. 2007 Jun 1;17(11):3181-6. doi: 10.1016/j.bmcl.2007.03.027.
Shintaro Hirashima 1,  Takahiro Oka,  Kazutaka Ikegashira,  Satoru Noji,  Hiroshi Yamanaka,  Yoshinori Hara,  Hiroyuki Goto,  Ryo Mizojiri,  Yasushi Niwa,  Toru Noguchi,  Izuru Ando,  Satoru Ikeda,  Hiromasa Hashimoto
Affiliations

Affiliation

  • 1 Central Pharmaceutical Research Institute, Japan Tobacco Inc., 1-1 Murasaki-cho, Takatsuki, Osaka 569-1125, Japan. hiromasa.hashimoto@ims.jti.co.jp
PMID: 17383878 DOI: 10.1016/j.bmcl.2007.03.027
Abstract

Following the discovery of JTK-109 (1) as a potent inhibitor of hepatitis C virus NS5B RNA-dependent RNA polymerase, [(a) Hirashima, S.; Suzuki, T.; Ishida, T.; Noji, S.; Yata, S.; Ando, I.; Komatsu, M.; Ikeda, S.; Hashimoto, H. J. Med. Chem.2006, 49, 4721. (b) Hashimoto, H.; Mizutani, K.; Yoshida, A. Int. Patent Appl. WO 01/47883, 2001.] further studies toward the improvement of the cellular potency have been performed. A greater than 40-fold improvement was achieved through replacing the biphenyl moiety with a 2-morpholinophenyl group and the benzimidazole ring with the tetracyclic scaffold to afford compound 7 with an excellent replicon potency (EC(50)=7.6 nM).

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