ArticleJournal of medicinal chemistry2012
Novel inhibitors of neurotropic alphavirus replication that improve host survival in a mouse model of acute viral encephalitis.
Article in Journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 39 citations in OpenAlex.
- Western equine encephalitis virus: A comprehensive review of epidemics, transmission, hosts, and strategies for mitigation.Virulence · 2025Review
- Eastern equine encephalitis virus: Pathogenesis, immune response, and clinical manifestations.Infectious medicine · 2025Review
- Article
- Synthesis and biological activity of conformationally restricted indole-based inhibitors of neurotropic alphavirus replication: Generation of a three-dimensional pharmacophore.Bioorganic & medicinal chemistry letters · 2021Article
- Synthetic strategies, SAR studies, and computer modeling of indole 2 and 3-carboxamides as the strong enzyme inhibitors: a review.Molecular diversity · 2021Review
- A compendium of small molecule direct-acting and host-targeting inhibitors as therapies against alphaviruses.The Journal of antimicrobial chemotherapy · 2017Review
- Type-1 angiotensin receptor signaling in central nervous system myeloid cells is pathogenic during fatal alphavirus encephalitis in mice.Journal of neuroinflammation · 2016Article
- Discovery of anthranilamides as a novel class of inhibitors of neurotropic alphavirus replication.Bioorganic & medicinal chemistry · 2015Article
- Manipulation of host factors optimizes the pathogenesis of western equine encephalitis virus infections in mice for antiviral drug development.Journal of neurovirology · 2015Article
- Novel indole-2-carboxamide compounds are potent broad-spectrum antivirals active against western equine encephalitis virus in vivo.Journal of virology · 2014Article
- The role of HTS in drug discovery at the University of Michigan.Combinatorial chemistry & high throughput screening · 2014Review
- Optimization of novel indole-2-carboxamide inhibitors of neurotropic alphavirus replication.Journal of medicinal chemistry · 2013Article
- Article
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Authors and funding
9 authors at 1 institution in 1 country.
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Abstract
Arboviral encephalitis is a potentially devastating human disease with no approved therapies that target virus replication. We previously discovered a novel class of thieno[3,2-b]pyrrole-based inhibitors active against neurotropic alphaviruses such as western equine encephalitis virus (WEEV) in cultured cells. In this report, we describe initial development of these novel antiviral compounds, including bioisosteric replacement of the 4H-thieno[3,2-b]pyrrole core with indole to improve metabolic stability and the introduction of chirality to assess target enantioselectivity. Selected modifications enhanced antiviral activity while maintaining low cytotoxicity, increased stability to microsomal metabolism, and also revealed striking enantiospecific activity in cultured cells. Furthermore, we demonstrate improved outcomes (both symptoms and survival) following treatment with indole analogue 9h (CCG-203926) in an in vivo mouse model of alphaviral encephalitis that closely correlate with the enantiospecific in vitro antiviral activity. These results represent a substantial advancement in the early preclinical development of a promising class of novel antiviral drugs against virulent neurotropic alphaviruses.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.