| Structural highlights
Publication Abstract from PubMed
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 that possess multiple additional vectors for further exploration. The binding mode and pharmacokinetic (PK) properties of select examples, including: 13-cyclohexyl-6-oxo-6,7-dihydro-5H-indolo[2,1-d][1,4]benzodiazepine-10-car boxylic acid (7) (IC(50)=0.07muM, %F=18), are reported.
Syntheses and initial evaluation of a series of indolo-fused heterocyclic inhibitors of the polymerase enzyme (NS5B) of the hepatitis C virus.,Zheng X, Hudyma TW, Martin SW, Bergstrom C, Ding M, He F, Romine J, Poss MA, Kadow JF, Chang CH, Wan J, Witmer MR, Morin P, Camac DM, Sheriff S, Beno BR, Rigat KL, Wang YK, Fridell R, Lemm J, Qiu D, Liu M, Voss S, Pelosi L, Roberts SB, Gao M, Knipe J, Gentles RG Bioorg Med Chem Lett. 2011 Mar 23. PMID:21486696[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Zheng X, Hudyma TW, Martin SW, Bergstrom C, Ding M, He F, Romine J, Poss MA, Kadow JF, Chang CH, Wan J, Witmer MR, Morin P, Camac DM, Sheriff S, Beno BR, Rigat KL, Wang YK, Fridell R, Lemm J, Qiu D, Liu M, Voss S, Pelosi L, Roberts SB, Gao M, Knipe J, Gentles RG. Syntheses and initial evaluation of a series of indolo-fused heterocyclic inhibitors of the polymerase enzyme (NS5B) of the hepatitis C virus. Bioorg Med Chem Lett. 2011 Mar 23. PMID:21486696 doi:10.1016/j.bmcl.2011.03.067
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