Biased and unbiased strategies to identify biologically active small molecules

The genus Enterovirus combines a portion of small (+)ssRNA-containing viruses and is divided into 10 species of true enteroviruses and three species of rhinoviruses. These viruses are causative agents of the widest spectrum of severe and deadly epidemic diseases of higher vertebrates, including humans. Their ubiquitous distribution and high pathogenicity motivate active search to counteract enterovirus infections. There are no sufficiently effective drugs targeted against enteroviral diseases, thus treatment is reduced to supportive and symptomatic measures. This makes it extremely urgent to develop drugs that directly affect enteroviruses and hinder their development and spread in infected organisms. In this review, we cover the classification of enteroviruses, mention the most common enterovirus infections and their clinical manifestations, and consider the current state of development of anti-enteroviral drugs. One of the most promising targets for such antiviral drugs is the viral Internal Ribosome Entry Site (IRES). The classification of these elements of the viral mRNA translation system is also examined.

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“…Peptide inhibitors and small molecules are extensive ly used in medicine [168,169]. These peptides usually consist of 5 40 a.a.…”

Section: Iress Of Viral Rnas As a Pharmaceutical Targetmentioning

confidence: 99%

“…Currently, small molecules are preferred drugs [169]. There are new approaches directed toward generation of libraries of small molecules with desired properties [169].…”

Section: Iress Of Viral Rnas As a Pharmaceutical Targetmentioning

confidence: 99%

Enteroviruses: Classification, diseases they cause, and approaches to development of antiviral drugs

Nikonov

Chernykh

Garber

et al. 2017

Biochemistry Moscow

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“…If the number of drugs reaching the clinic is the yardstick, it must be concluded that this approach has not worked. This is considered to be largely due to the limited structural diversity inherent in conventional combinatorial libraries, and indeed has prompted renewed interest in the development of drugs from natural sources [93][94][95]. However, natural product drug discovery has its limitations too, including difficulties with the resupply of raw materials, difficulties with the repeated isolation of known compounds, and difficulties with synthesizing natural compounds of interest [94].…”

Section: Drug Discovery Strategiesmentioning

confidence: 99%

“…This is considered to be largely due to the limited structural diversity inherent in conventional combinatorial libraries, and indeed has prompted renewed interest in the development of drugs from natural sources [93][94][95]. However, natural product drug discovery has its limitations too, including difficulties with the resupply of raw materials, difficulties with the repeated isolation of known compounds, and difficulties with synthesizing natural compounds of interest [94]. More recently, hybrid approaches have been developed whereby combinatorial libraries incorporate the broader chemical diversity of natural products [96,97].…”

Section: Drug Discovery Strategiesmentioning

confidence: 99%

Selective Modulators of α<sub>5</sub>-Containing GABA<sub>A</sub> Receptors and their Therapeutic Significance

Soh

Lynch

2015

CDT

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“…We preferred a diversity-oriented synthesis strategy with the aim of generating both skeletal and appendage diversity 15 and were attracted to the so-called "build couple pair" approach ( Figure 1). …”

mentioning

confidence: 99%

New heteroatom-rich ring systems from N,N-dialkyl-N’-chlorosulfonyl chloroformamidines

Francis¹

2016

Arkivoc

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N,N-Dialkyl-N'-chlorosulfonyl chloroformamidines constitute a class of readily available and very versatile bis-electrophiles. This Account describes the application of these unusual + C=N-S + building blocks for construction of a cornucopia of previously unknown or uncommon heterocyclic ring systems. Regioselectivity encountered during heterocycle formation and some properties and chemistry of the newly-formed ring systems are also discussed.

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Biased and unbiased strategies to identify biologically active small molecules

Cited by 15 publications

References 115 publications

Enteroviruses: Classification, diseases they cause, and approaches to development of antiviral drugs

Enteroviruses: Classification, diseases they cause, and approaches to development of antiviral drugs

Selective Modulators of α<sub>5</sub>-Containing GABA<sub>A</sub> Receptors and their Therapeutic Significance

New heteroatom-rich ring systems from N,N-dialkyl-N’-chlorosulfonyl chloroformamidines

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