NDLI: Asymmetric synthesis of host-directed inhibitors of myxoviruses

Content Provider	PubMed Central
Author	Moore, Terry W. Sana, Kasinath Yan, Dan Pahk, Thepchatri Ndungu, John M. Saindane, Manohar T. Lockwood, Mark A. Natchus, Michael G. Liotta, Dennis C. Plemper, Richard K. Snyder, James P. Sun, Aiming
Editor	Jeffrey, Aubé
Copyright Year	2013
Abstract	High-throughput screening (HTS) previously identified benzimidazole 1 (JMN3-003) as a compound with broad antiviral activity against different influenza viruses and paramyxovirus strains. In pursuit of a lead compound from this series for development, we sought to increase both the potency and the aqueous solubility of 1. Lead optimization has achieved compounds with potent antiviral activity against a panel of myxovirus family members (EC50 values in the low nanomolar range) and much improved aqueous solubilities relative to that of 1. Additionally, we have devised a robust synthetic strategy for preparing 1 and congeners in an enantio-enriched fashion, which has allowed us to demonstrate that the (S)-enantiomers are generally 7- to 110-fold more potent than the corresponding (R)-isomers.
Related Links	http://dx.doi.org/10.3762/bjoc.9.23
Ending Page	203
Page Count	7
Starting Page	197
File Format	PDF
ISSN	18605397
e-ISSN	18605397
Journal	Beilstein Journal of Organic Chemistry
Volume Number	9
Language	English
Publisher	Beilstein-Institut
Publisher Date	2013-01-01
Access Restriction	Open
Rights Holder	Beilstein-Institut
Subject Keyword	Organic Chemistry Research in Higher Education
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry

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