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Title: Derivatives of imidazotriazine and pyrrolotriazine C-nucleosides as potential new anti-HCV agents
Authors: Draffan, AG
Frey, B
Fraser, BH
Pool, B
Gannon, C
Tyndall, EM
Cianci, J
Harding, M
Lilly, M
Hufton, R
Halim, R
Jahangiri, S
Bond, S
Jeynes, TP
Nguyen, VTT
Wirth, V
Luttick, A
Tilmanis, D
Pryor, M
Porter, K
Morton, CJ
Lin, B
Duan, J
Bethell, RC
Kukojl, G
Simoneau, B
Tucker, SP
Keywords: Viral diseases
Infectious hepatitis
Issue Date: 1-Nov-2014
Publisher: Elsevier B.V.
Citation: Draffan, A. G., Frey, B., Fraser, B. H., Pool, B., Gannon, C., Tyndall, E. M., Cianci, J., Harding, M., Lilly, M., Hufton, R., Halim, R., Jahangiri, S., Bond., Jeynes, T. P., Nguyen V. T. T., Wirth, V., Luttick, A., Tilmanis, D., Pryor, M., Porter, K., Morton, C. J., Lin, B., Duan, J., Bethell, R. C., Kukolj, G., Sinoneau, B., & Tucker, S. P. (2014). Derivatives of imidazotriazine and pyrrolotriazine C-nucleosides as potential new anti-HCV agents. Bioorganic & Medicinal Chemistry Letters, 24(21), 4984-4988. doi:10.1016/j.bmcl.2014.09.030
Abstract: Previous investigations identified 2′-C-Me-branched ribo-C-nucleoside adenosine analogues, 1, which contains a pyrrolo[2,1-f][1,2,4]triazin-4-amine heterocyclic base, and 2, which contains an imidazo[2,1-f][1,2,4]triazin-4-amine heterocyclic base as two compounds with promising anti-HCV in vitro activity. This Letter describes the synthesis and evaluation of a series of novel analogues of these compounds substituted at the 2-, 7-, and 8-positions of the heterocyclic bases. A number of active new HCV inhibitors were identified but most compounds also demonstrated unacceptable cytotoxicity. However, the 7-fluoro analogue of 1 displayed good potency with a promising cytotherapeutic margin. © 2014 Elsevier Ltd.
Gov't Doc #: 8743
ISSN: 0960-894X
Appears in Collections:Journal Articles

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