| Structural highlights
Publication Abstract from PubMed
Herein we report the successful incorporation of a lactam as an amide replacement in the design of hepatitis C virus NS5B Site II thiophene carboxylic acid inhibitors. Optimizing potency in a replicon assay and minimizing potential risk for CYP3A4 induction led to the discovery of inhibitor 22a. This lead compound has a favorable pharmacokinetic profile in rats and dogs.
Design and synthesis of lactam-thiophene carboxylic acids as potent hepatitis C virus polymerase inhibitors.,Barnes-Seeman D, Boiselle C, Capacci-Daniel C, Chopra R, Hoffmaster K, Jones CT, Kato M, Lin K, Ma S, Pan G, Shu L, Wang J, Whiteman L, Xu M, Zheng R, Fu J Bioorg Med Chem Lett. 2014 Aug 15;24(16):3979-85. doi:, 10.1016/j.bmcl.2014.06.031. Epub 2014 Jun 20. PMID:24986660[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
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References
- ↑ Barnes-Seeman D, Boiselle C, Capacci-Daniel C, Chopra R, Hoffmaster K, Jones CT, Kato M, Lin K, Ma S, Pan G, Shu L, Wang J, Whiteman L, Xu M, Zheng R, Fu J. Design and synthesis of lactam-thiophene carboxylic acids as potent hepatitis C virus polymerase inhibitors. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3979-85. doi:, 10.1016/j.bmcl.2014.06.031. Epub 2014 Jun 20. PMID:24986660 doi:http://dx.doi.org/10.1016/j.bmcl.2014.06.031
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