Abstract

The outbreak of SARS-CoV-2 has drastically changed our everyday life and the life of scientists from all over the world. In the last year, the scientific community has faced this worldwide threat using any tool available in order to find an effective response. The recent formulation, production, and ongoing administration of vaccines represent a starting point in the battle against SARS-CoV-2, but they cannot be the only aid available. In this regard, the use of drugs capable to mitigate and fight the virus is a crucial aspect of the pharmacological strategy. Among the plethora of approved drugs, a consistent element is a heterocyclic framework inside its skeleton. Heterocycles have played a pivotal role for decades in the pharmaceutical industry due to their high bioactivity derived from anticancer, antiviral, and anti-inflammatory capabilities. In this context, the development of new performing and sustainable synthetic strategies to obtain heterocyclic molecules has become a key focus of scientists. In this review, we present the recent trends in metal-promoted heterocyclization, and we focus our attention on the construction of heterocycles associated with the skeleton of drugs targeting SARS-CoV-2 coronavirus.

Highlights

  • The novel coronavirus disease (COVID-19) has resulted in a worldwide pandemic, with increasingly large numbers of infections [1]

  • We describe recent otal scaffolds associated with molecules showing anti-COVID-19 properties

  • This review presented recent methodologies applied to produce various aromatic and nonaromatic heterocyclic scaffolds that have gained interest in the fight against the ongoing SARS-CoV-2 outbreak

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Summary

Introduction

The novel coronavirus disease (COVID-19) has resulted in a worldwide pandemic, with increasingly large numbers of infections [1]. Promising strategies based on interferons [8] and monoclonal antibodies [9], as well as cell-based and immunopathology therapies, have resulted to be time- and cost-consuming and, they cannot be considered valuable alternatives in the current conditions [10] Researchers have focused their attention on current small molecules used as anti-influenza, antimalarial, and anti-HIV drugs. Drugs containing a heterocyclic moiety inside their structure show antitumor, mor, anti-inflammatory, antifungal, antidepressant, anti-HIV, antimalarial, and antiviral anti-inflammatory, antifungal, antidepressant, anti-HIV, antimalarial, and antiviral propproperties [20,21,22] The latter properties are central theagainst fight against erties [20,21,22].

Chloroquine and Hydroxychloroquine
Critical
Critical in Gupton
Alternative
Arbidol
A Nenitzescu reaction
Telmisartan
36. Tandem
37. Neutral
Quercetin and Luteolin
SARS-CoV-2 3CL Protease Target Drugs
Conclusions
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