Antiviral Library
Designed for discovery of new Nucleoside-like antivirals
3 200 compounds
In spite of significant success in medicine in last decades, development of effective new antiviral agents and vaccines continue to be a challenging task for the modern drug discovery. Viruses share most of the metabolic processes of host cells, thereby making difficult search of selective antiviral agents. However, some enzymes are only present in viruses and these are potential and most attractive targets for antiviral drugs.
For instance, there are several key enzymes, which are involved in the processes with nucleic acids like DNA- and RNA-polymerases. Also, reverse transcriptases possess high potential as antiviral targets. The success of previously approved anti-HCV drug Sofosbuvir has demonstrated the potency of small molecules and the important role of viral RNA-polymerases as drug targets. The series of new drug candidates with nucleoside-like scaffolds introduced by Gilead have shown promising results in treating of serious viral infections such as recently emerged Coronavirus, Ebola and RSV.
Examples of nucleoside mimetics as antiviral agents
RemdesivirEbola, Junin and MERS viruses studied against Coronaviruses, 2019-nCoV
Sofosbuvir Hepatitis C
Entacavir Hepatitis B virus
Galidesivir Ebola & Marburg viruses
Ribavirin RSV infection, hemorrhagic fevers
To meet growing needs in new antivirals Enamine has designed the library of nucleoside-like small molecules, enriched with recently synthesized series of nucleoside-like compounds. The library of carefully selected 3 200 compounds has been pre-plated for most convenient access and prompt delivery in various customized formats.
Typical Formats
Catalog No.
AVR-3200-Y-0
Compounds
3 200
9 plates
Amount
Up to 300 nL of 2 mM DMSO solutions
Plates and formats
384-well Echo Qualified plates,
320 compounds per plate,
1, 2 and 23, 24 columns empty
Price
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Catalog No.
AVR-3200-Y-10
Compounds
3 200
9 plates
Amount
10 µL of 10 mM DMSO stock solutions
Plates and formats
384-well plates Greiner 781280,
320 compounds per plate,
first two and last two columns empty
Price
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Catalog No.
AVR-3200-X-50
Compounds
3 200
40 plates
Amount
50 µL of 10 mM DMSO solutions
Plates and formats
96-well plates, Greiner Cat. No 650201, round (U) bottom,
80 compounds per plate,
1 & 12 columns empty
Price
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Catalog No.
AVR-3200
Compounds
3 200
Amount
Custom
Plates and formats
Any custom format
Price
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Library Design
Analyzing the structures of known inhibitors we found that most of them are AVR-3200 side mimetics which are not distinguished from the nucleosides by virus enzymes in the active site.
Therefore taking into account pharmacophores and topology of nucleosides and reported nucleoside-like antiviral agents we carefully selected the set of Nucleoside mimetics from our screening collection. The compounds from the set contain natural-like moieties and diverse heterocycles as bioisosters of nucleosides. Additionally, special emphasis has been made on compounds that possess several H-bond donors and potentially can form similar interactions with the protein nucleoside-binding sites as a native nucleoside.
Examples of representative compounds from Antiviral Library
Molecular Profile of the library
Selected compounds have attractive drug/lead-like physical chemical and structural properties that are characteristic for nucleosides and their mimetics: MW 150…400, ClogP -2…4; TPSA <150, RotBonds <7; HBD 1…5, HBA 1…7.
The library is considered to be a convenient starting point for a wide range of antiviral drug discovery projects.
