scholarly journals Recent Advances in Tetrazole Derivatives as Potential Antiviral Agents

2021 ◽  
Vol 33 (11) ◽  
pp. 2599-2607
Author(s):  
Ruchika Yogesh ◽  
Noopur Srivastava
Keyword(s):  
Antiviral Agents ◽  
Acid Amide ◽  
Host Cells ◽  
Carboxylic Acid Amide ◽  
Synthetic Compounds ◽  
Scientific Databases ◽  
The Past ◽  
Antiviral Compounds ◽  
Pharmaceutical Agents ◽  
Tetrazole Derivatives

Viruses use the host cell’s biochemical machinery for replication and survival; and also undergo mutations to evade the immune response and achieve better transmission. These features make it challenging to develop selective drugs to kill viruses only and not the host cells. New and effective pharmaceutical agents are required to overcome this challenge. Tetrazole moiety, as a bio-isostere of carboxylic acid/amide group, has been extensively used as a potent pharmacophore in several bioactivities. Intrigued by the necessity of finding new antiviral compounds and tendency of tetrazole scaffolds to render various bioactivity profiles, this review article comprising literature reports of tetrazole-based synthetic compounds with promising antiviral activity is presented. This review comprises significant literature reports from the scientific databases published during the past four decades. It is found that tetrazole based molecules are promising endeavor for the development of potential agents against influenza virus, HIV, HCV and other viruses.

scholarly journals Biological Evaluation of Molecules of the azaBINOL Class as Antiviral Agents: Specific Inhibition of HIV-1 RNase H Activity by 7-Isopropoxy-8-(naphth-1-yl)quinoline

2019 ◽  
Author(s):  
Ross D. Overacker ◽  
Somdev Banerjee ◽  
George F. Neuhaus ◽  
Selena Milicevic Sephton ◽  
Alexander Herrmann ◽  
...  
Keyword(s):  
Viral Entry ◽  
Antiviral Agents ◽  
Biological Evaluation ◽  
Rnase H ◽  
Synthetic Compounds ◽  
Infectivity Assay ◽  
Antiviral Compounds ◽  
Specific Manner ◽  
Drug Leads ◽  
Hiv 1

AbstractInspired by bioactive biaryl-containing natural products found in plants and the marine environment, a series of synthetic compounds belonging to the azaBINOL chiral ligand family was evaluated for antiviral activity against HIV-1. Testing of 39 unique azaBINOLs in a singleround infectivity assay resulted in the identification of three promising antiviral compounds, including 7-isopropoxy-8-(naphth-1-yl)quinoline (azaBINOLB#24), which exhibited low-micromolar activity. The active compounds and several close structural analogues were further tested against three different HIV-1 envelope pseudotyped viruses as well as in a full-virus replication system (EASY-HIT). Mode-of-action studies using a time-of-addition assay indicated that azaBINOLB#24acts after viral entry but before viral assembly and budding. HIV-1 reverse transcriptase (RT) assays that individually test for polymerase and RNase H activity were used to demonstrate thatB#24inhibits RNase H activity, most likely allosterically. Further binding analysis using bio-layer interferometry (BLI) showed thatB#24interacts with HIV-1 RT in a highly specific manner. These results indicate that azaBINOLB#24is a potentially viable, novel lead for the development of new HIV-1 RNase H inhibitors. Furthermore, this study demonstrates that the survey of libraries of synthetic compounds, designed purely with the goal of facilitating chemical synthesis in mind, may yield unexpected and selective drug leads for the development of new antiviral agents.

scholarly journals Current Trends in SPR Biosensing of SARS-CoV-2 Entry Inhibitors

Chemosensors ◽  
2021 ◽  
Vol 9 (12) ◽  
pp. 330
Author(s):  
Elba Mauriz ◽  
Laura M. Lechuga
Keyword(s):  
High Throughput Screening ◽  
Antiviral Agents ◽  
Host Cells ◽  
Binding Affinities ◽  
Entry Inhibitors ◽  
Antiviral Compounds ◽  
Current Trends ◽  
Main Protease ◽  
Emerging Risk ◽  
Repurposed Drugs

The emerging risk of viral diseases has triggered the search for preventive and therapeutic agents. Since the beginning of the COVID-19 pandemic, greater efforts have been devoted to investigating virus entry mechanisms into host cells. The feasibility of plasmonic sensing technologies for screening interactions of small molecules in real time, while providing the pharmacokinetic drug profiling of potential antiviral compounds, offers an advantageous approach over other biophysical methods. This review summarizes recent advancements in the drug discovery process of Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) inhibitors using Surface Plasmon Resonance (SPR) biosensors. A variety of SPR assay formats are discussed according to the binding kinetics and drug efficacies of both natural products and repurposed drugs. Special attention has been given to the targeting of antiviral agents that block the receptor binding domain of the spike protein (RBD-S) and the main protease (3CLpro) of SARS-CoV-2. The functionality of plasmonic biosensors for high-throughput screening of entry virus inhibitors was also reviewed taking into account experimental parameters (binding affinities, selectivity, stability), potential limitations and future applications.

Current Peptide HIV Type-1 Fusion Inhibitors

2009 ◽  
Vol 20 (1) ◽  
pp. 1-18 ◽  
Author(s):  
Wei Pang ◽  
Siu-Cheung Tam ◽  
Yong-Tang Zheng
Keyword(s):  
Antiviral Agents ◽  
Antiretroviral Drugs ◽  
Host Cells ◽  
Fixed Dose ◽  
Clinical Use ◽  
The Past ◽  
Fusion Inhibitors ◽  
Hiv Type 1 ◽  
Hiv 1

There are now 26 antiretroviral drugs and 6 fixed-dose combinations, including reverse transcriptase inhibitors, protease inhibitors, integrase inhibitors and fusion (or entry) inhibitors, approved by the US Food and Drug Administration for clinical use. Although they are clinically effective when used in combination, none of the existing drugs are considered ideal because of toxic side effects and the ascendance of inducing drug-resistant mutants. Development of new antiviral agents is essential. In the past decades, there has been great progress in understanding the structure of HIV type-1 (HIV-1) gp41 and the mechanism of HIV-1 entry into host cells. This opened up a promising avenue for rationally designed agents to interfere with this process. A number of fusion inhibitors have been developed to block HIV-1 replication. Enfuvirtide (T20) was one of those approved for clinical use. This signalled a new era in AIDS therapeutics. It is a synthetic polypeptide with potent inhibitory activity against HIV-1 infection. However, it is sensitive to proteolytic digestion and resistant virus strains are easily induced with multiple clinical use. One of the directions in designing new fusion inhibitors is to overcome these shortages. In the past years, large numbers of promising fusion inhibitory peptides have emerged. The antiviral activities are more potent or they can act differently from that of T20. Some of these new compounds have great potential to be further developed as therapeutic agents. This article reviewed some recent developments of these peptides and the possible role in anti-HIV-1 therapy.

scholarly journals Review of Phytochemical Compounds as Antiviral Agents Against Arboviruses from the Genera Flavivirus and Alphavirus

2020 ◽  
Vol 17 (4) ◽  
pp. 484-497
Author(s):  
Samira Sardari ◽  
Mahmoud Rafieian-Kopaei ◽  
Khojasteh Malekmohammad ◽  
Robert D.E. Sewell
Keyword(s):  
Antiviral Agents ◽  
Emerging Infectious Diseases ◽  
Diverse Group ◽  
Inhibitory Effects ◽  
Public Health Perspective ◽  
The Past ◽  
Antiviral Compounds ◽  
Viral Mutation ◽  
The World ◽  
Phytochemical Compounds

Arboviruses are a diverse group of viruses that are among the major causes of emerging infectious diseases. Arboviruses from the genera flavivirus and alphavirus are the most important human arboviruses from a public health perspective. During recent decades, these viruses have been responsible for millions of infections and deaths around the world. Over the past few years, several investigations have been carried out to identify antiviral agents to treat these arbovirus infections. The use of synthetic antiviral compounds is often unsatisfactory since they may raise the risk of viral mutation; they are costly and possess either side effects or toxicity. One attractive strategy is the use of plants as promising sources of novel antiviral compounds that present significant inhibitory effects on these viruses. In this review, we describe advances in the exploitation of compounds and extracts from natural sources that target the vital proteins and enzymes involved in arbovirus replication.

scholarly journals Antiviral Potential of Algae Polysaccharides Isolated from Marine Sources: A Review

2015 ◽  
Vol 2015 ◽  
pp. 1-10 ◽  
Author(s):  
Azin Ahmadi ◽  
Soheil Zorofchian Moghadamtousi ◽  
Sazaly Abubakar ◽  
Keivan Zandi
Keyword(s):  
Protein Synthesis ◽  
Antiviral Agents ◽  
Pharmaceutical Research ◽  
Mechanisms Of Action ◽  
Host Cells ◽  
Chemical Compositions ◽  
The Past ◽  
Antiviral Activities ◽  
Pharmaceutical Industries ◽  
Algal Polysaccharides

From food to fertilizer, algal derived products are largely employed in assorted industries, including agricultural, biomedical, food, and pharmaceutical industries. Among different chemical compositions isolated from algae, polysaccharides are the most well-established compounds, which were subjected to a variety of studies due to extensive bioactivities. Over the past few decades, the promising results for antiviral potential of algae-derived polysaccharides have advocated them as inordinate candidates for pharmaceutical research. Numerous studies have isolated various algal polysaccharides possessing antiviral activities, including carrageenan, alginate, fucan, laminaran, and naviculan. In addition, different mechanisms of action have been reported for these polysaccharides, such as inhibiting the binding or internalization of virus into the host cells or suppressing DNA replication and protein synthesis. This review strives for compiling previous antiviral studies of algae-derived polysaccharides and their mechanism of action towards their development as natural antiviral agents for future investigations.

Phytochemical and Pharmacological Review on Two Herbs of Baijiangcao: Patrinia scabiosaefolia Fisch. ex Trev. and Patrinia villosa (Thunb.) Juss

2020 ◽  
Vol 17 (5) ◽  
pp. 496-517
Author(s):  
Yangcheng Liu ◽  
Wei Liu ◽  
Jiaqi Wang ◽  
Yang Liu ◽  
Changlan Chen ◽  
...  
Keyword(s):  
Chemical Constituents ◽  
Volatile Components ◽  
Research Papers ◽  
Pharmacological Activities ◽  
Comprehensive Review ◽  
Scientific Databases ◽  
The Past ◽  
Current State ◽  
Patrinia Scabiosaefolia ◽  
Antiviral Activities

Patrinia scabiosaefolia Fisch. Trev. and Patrinia villosa (Thunb.) Juss, are two species of Patrinia recorded in the Chinese Pharmacopoeia with the same Chinese name “Baijiangcao” and similar therapeutic effect in traditional Chinese medicine. The present article is the first comprehensive review on the chemical composition and pharmacological activities of these herbs. In this review, data on chemical constituents and pharmacological profile of the two herbs are provided. This review discusses all the classes of the 223 compounds (phenylpropanoids, flavonoids, terpenes, saponins and volatile components, etc.) detected in the two herbs providing information on the current state of knowledge of the phytochemicals present in them. In the past three years, our research group has isolated and identified about more than 100 ingredients from the two herbs. Therefore, we published a systematic review of our research papers and studies on the two herbs were carried out using resources such as classic books about Chinese herbal medicine and scientific databases including Pubmed, Web of Science, SciFinder, CNKI. etc. The present review discusses the most thoroughly studied pharmacological activities (antioxidant, anti-inflammatory, immunomodulatory, antimicrobial, antitumor and antiviral activities) of the two herbs. This comprehensive review will be informative for scientists searching for new properties of these herbs and will be important and significant for the discovery of bioactive compounds from the two herbs and in complete utilization of Patrinia scabiosaefolia Fisch. ex Trev. and Patrinia villosa (Thunb.) Juss.

A Brief outlook on possible available solutions, therapies and suggestions for COVID-19

Coronaviruses ◽  
2020 ◽  
Vol 01 ◽  
Author(s):  
Rashmi Saxena Pal ◽  
Yogendra Pal ◽  
Pranay Wal ◽  
Ankita Wal ◽  
Nikita Saraswat
Keyword(s):  
United States ◽  
Plasma Therapy ◽  
Social Distancing ◽  
The Past ◽  
Antiviral Compounds ◽  
Global Pandemic ◽  
Case Count ◽  
Current Scenario ◽  
Hiv Drugs

Background: WHO declared COVID-19 a global pandemic. New cases are being added every day, as the case count in United States are to the maximum. No drugs or biologics are yet found to be effective for the prevention or treatment of COVID-19. Objective: To discuss the possibilities of available treatments available. Materials & Methods: Brief out-look is undertaken over the past issues available over the similar situations occurred with respect to the current scenario and prospectives. Results: There can be various possibilities in form of convalescent plasma therapy. The known drugs as HIV drugs, antimalarial medicines and antiviral compounds can serve as suggestive option. Conclusion: Till a confirm medicine or vaccine is sorted out for Covid-19, we need to take natural immune-boosters, along with precautionary steps, social distancing and other preventions as instructed for the benefit of everyone with an optimistic mind and attitude.

scholarly journals Nexus between COVID-19 and periodontal disease

2021 ◽  
Vol 49 (3) ◽  
pp. 030006052110026
Author(s):  
Kanchana Sukumar ◽  
Anupama Tadepalli
Keyword(s):  
Periodontal Disease ◽  
Host Cells ◽  
Multifactorial Disease ◽  
Tissue Destruction ◽  
The Past ◽  
Appropriate Care ◽  
Bacterial Stimulation ◽  
Plaque Control ◽  
Disease Understanding ◽  
Pro Inflammatory Cytokines

Over the past several decades, studies have demonstrated the existence of bi-directional relationships between periodontal disease and systemic conditions. Periodontitis is a polymicrobial and multifactorial disease involving both host and environmental factors. Tissue destruction is primarily associated with hyperresponsiveness of the host resulting in release of inflammatory mediators. Pro-inflammatory cytokines play a major role in bacterial stimulation and tissue destruction. In addition, these cytokines are thought to underlie the associations between periodontitis and systemic conditions. Current research suggests that increased release of cytokines from host cells, referred to as the cytokine storm, is associated with disease progression in patients with coronavirus disease 2019 (COVID-19). An intersection between periodontitis and pulmonary disease is biologically plausible. Hence, we reviewed the evidence linking COVID-19, cytokines, and periodontal disease. Plaque control is essential to prevent exchange of bacteria between the mouth and the lungs, reducing the risk of lung disease. Understanding these associations may help identify individuals at high risk and deliver appropriate care at early stages.

scholarly journals Bromodomain and Extraterminal Protein Inhibitor, Apabetalone (RVX-208), Reduces ACE2 Expression and Attenuates SARS-Cov-2 Infection In Vitro

Biomedicines ◽  
2021 ◽  
Vol 9 (4) ◽  
pp. 437
Author(s):  
Dean Gilham ◽  
Audrey L. Smith ◽  
Li Fu ◽  
Dalia Y. Moore ◽  
Abenaya Muralidharan ◽  
...  
Keyword(s):  
Antiviral Agents ◽  
Host Cells ◽  
Protein Inhibitor ◽  
Angiotensin Converting Enzyme 2 ◽  
Dipeptidyl Peptidase 4 ◽  
Surface Receptors ◽  
Bet Inhibitor ◽  
Epigenetic Machinery ◽  
Unexplored Area

Effective therapeutics are urgently needed to counter infection and improve outcomes for patients suffering from COVID-19 and to combat this pandemic. Manipulation of epigenetic machinery to influence viral infectivity of host cells is a relatively unexplored area. The bromodomain and extraterminal (BET) family of epigenetic readers have been reported to modulate SARS-CoV-2 infection. Herein, we demonstrate apabetalone, the most clinical advanced BET inhibitor, downregulates expression of cell surface receptors involved in SARS-CoV-2 entry, including angiotensin-converting enzyme 2 (ACE2) and dipeptidyl-peptidase 4 (DPP4 or CD26) in SARS-CoV-2 permissive cells. Moreover, we show that apabetalone inhibits SARS-CoV-2 infection in vitro to levels comparable to those of antiviral agents. Taken together, our study supports further evaluation of apabetalone to treat COVID-19, either alone or in combination with emerging therapeutics.

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