ArticleBioorganic & medicinal chemistry letters2013
Lead optimization of an acylhydrazone scaffold possessing antiviral activity against Lassa virus.
Article in Bioorganic & medicinal chemistry letters, 2013. 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, 22 citations in OpenAlex.
- Molecular organization of the New World arenavirus spike glycoprotein complex.Nature microbiology · 2025Article
- Purification and characterization of the Lassa virus transmembrane domain.Biochemistry and biophysics reports · 2023Article
- Characterizing the Lassa Virus Envelope Glycoprotein Membrane Proximal External Region for Its Role in Fusogenicity.Virologica Sinica · 2021Article
- Identification of Clotrimazole Derivatives as Specific Inhibitors of Arenavirus Fusion.Journal of virology · 2019Article
- Structure-activity relationship optimization for lassa virus fusion inhibitors targeting the transmembrane domain of GP2.Protein & cell · 2019Article
- Diagnostics for Lassa fever virus: a genetically diverse pathogen found in low-resource settings.BMJ global health · 2019Article
- Article
- Screening and Identification of Lassa Virus Entry Inhibitors from an FDA-Approved Drug Library.Journal of virology · 2018Article
- Substituted tetrazoles as multipurpose screening compounds.Molecular diversity · 2017Article
- Small-Molecule Fusion Inhibitors Bind the pH-Sensing Stable Signal Peptide-GP2 Subunit Interface of the Lassa Virus Envelope Glycoprotein.Journal of virology · 2016Article
- Computer aided drug discovery of highly ligand efficient, low molecular weight imidazopyridine analogs as FLT3 inhibitors.European journal of medicinal chemistry · 2015Article
- Tractable synthesis of multipurpose screening compounds with under-represented molecular features for an open access screening platform.Molecular diversity · 2014Article
- Microwave-assisted synthesis and evaluation of acylhydrazones as potential inhibitors of bovine glutathione peroxidase.Molecular diversity · 2014Article
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
Abstract
Previously we reported the optimization of antiviral scaffolds containing benzimidazole and related heterocycles possessing activity against a variety of arenaviruses. These series of compounds were discovered through an HTS campaign of a 400,000 small molecule library using lentivirus-based pseudotypes incorporated with the Lassa virus envelope glycoprotein (LASV GP). This screening also uncovered an alternate series of very potent arenavirus inhibitors based upon an acylhydrazone scaffold. Subsequent SAR analysis of this chemical series involved various substitutions throughout the chemical framework along with assessment of the preferred stereochemistry. These studies led to an optimized analog (ST-161) possessing subnanomolar activity against LASV and submicromolar activity against a number of other viruses in the Arenaviridae family.
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