antiviral drugs

Amantadine hydrochloride (CI-719) is an antiviral that is used in the prophylactic or symptomatic treatment of influenza A and Parkinson disease.

Amantadine (1-Aminoadamantane) is an antiviral, is a weak antagonist of the NMDA-type glutamate receptor, increases dopamine release, and blocks dopamine reuptake.

Pixatimod (also known as PG-545) is a synthetic modified heparan sulfate mimetic and an agonist of Toll-like receptor 9 (TLR9), showcasing potential immunostimulatory, antitumor, and antiviral properties. It effectively inhibits SARS-CoV-2 by disrupting the interaction between the spike protein and ACE2. Moreover, Pixatimod blocks cancer-promoting processes such as cell proliferation, invasion, metastasis, angiogenesis, and epithelial-mesenchymal transition. These activities have demonstrated significant efficacy across various murine cancer models, including approximately 30 xenograft models and 20 syngeneic models. Pixatimod has been tested in combination with several approved anticancer compounds, underscoring its clinical potential, with drugs like gemcitabine, paclitaxel, sorafenib, platinum-based compounds, and an anti-PD-1 antibody.

3′-Deoxy CTP trisodium is the sodium salt form of 3′-Deoxy CTP. This compound is a nucleotide analog known as a chain terminator. By lacking a 3′-hydroxyl group, it causes chain termination and inhibits the RNA synthesis activity of the HCV non-structural protein (NS5B) polymerase, thereby blocking viral replication. 3′-Deoxy CTP trisodium is utilized in the study of chain termination mechanisms of HCV polymerase and the development of antiviral drugs.

SARS-CoV-2 Mpro-IN-44 (Compound 25) is a broad-spectrum inhibitor of the main protease (Mpro) for coronaviruses. It exhibits inhibitory activity against several high-risk coronaviruses, including SARS-CoV-2 and PEDV, with an IC50 of less than 0.6 μM. The broad inhibition of coronaviruses by SARS-CoV-2 Mpro-IN-44 is achieved through enhanced interaction with conserved sites of Mpro. This compound is a potential candidate for the development of antiviral drugs against coronaviruses.

SARS-CoV-2 nsp13-IN-7 (Compound 6r) is an inhibitor of SARS-CoV-2 nsp13, with an IC50 of 0.28 μM. This compound disrupts the helicase function of nsp13 by binding to its 5' RNA site and ATP binding site, and it serves as a lead compound for developing antiviral drugs targeting SARS-CoV-2 nsp13.

3′-Deoxy CTP is a nucleotide analog that functions as a potent chain terminator. By lacking a 3′-hydroxyl group, 3′-Deoxy CTP induces chain termination, thereby inhibiting the RNA synthesis activity of HCV non-structural protein (NS5B) polymerase and halting viral replication. This compound is useful for studying the chain termination mechanism of HCV polymerases and for developing antiviral drugs.

3-Hydroxyterphenyllin is a p-terphenyl fungal metabolite originally isolated from A. candidus that has diverse biological activities, including antioxidant, antiproliferative, antibacterial, and antiviral properties.1,2,3,4 It has a 96% scavenging effect on 2,2-diphenyl-1-picrylhydrazyl radicals when used at a concentration of 100 μg/ml.2 3-Hydroxyterphenyllin inhibits the growth of HeLa cervical, A549 lung, and HepG2 liver cancer cells (IC50s = 23, 36, and 32 μM, respectively), as well as methicillin-resistant S. aureus (MRSA) and V. vulnificus bacteria (MIC = 31 μg/ml for both).3 It also inhibits HIV-1 integrase in both coupled and strand transfer assays (IC50s = 2.8 and 12.1 μM, respectively).4References1. Kurobane, I., Vining, L.C., McInnes, A.G., et al. 3-Hydroxyterphenyllin, a new metabolite of Aspergillus candidus. Structure elucidation by 1H and 13C nuclear magnetic resonance spectroscopy. J. Antibiot. (Tokyo) 32(6), 559-564 (1979).2. Yen, G.-C., Chang, Y.-C., Sheu, F., et al. Isolation and characterization of antioxidant compounds from Aspergillus candidus broth filtrate. J. Agric. Food Chem. 49(3), 1426-1431 (2001).3. Wang, W., Liao, Y., Tang, C., et al. Cytotoxic and antibacterial compounds from the coral-derived fungus Aspergillus tritici SP2-8-1. Mar. Drugs 15(11), E348 (2017).4. Singh, S.B., Jayasuriya, H., Dewey, R., et al. Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites. J. Ind. Microbiol. Biotechnol. 30(12), 721-731 (2003). 3-Hydroxyterphenyllin is a p-terphenyl fungal metabolite originally isolated from A. candidus that has diverse biological activities, including antioxidant, antiproliferative, antibacterial, and antiviral properties.1,2,3,4 It has a 96% scavenging effect on 2,2-diphenyl-1-picrylhydrazyl radicals when used at a concentration of 100 μg/ml.2 3-Hydroxyterphenyllin inhibits the growth of HeLa cervical, A549 lung, and HepG2 liver cancer cells (IC50s = 23, 36, and 32 μM, respectively), as well as methicillin-resistant S. aureus (MRSA) and V. vulnificus bacteria (MIC = 31 μg/ml for both).3 It also inhibits HIV-1 integrase in both coupled and strand transfer assays (IC50s = 2.8 and 12.1 μM, respectively).4 References1. Kurobane, I., Vining, L.C., McInnes, A.G., et al. 3-Hydroxyterphenyllin, a new metabolite of Aspergillus candidus. Structure elucidation by 1H and 13C nuclear magnetic resonance spectroscopy. J. Antibiot. (Tokyo) 32(6), 559-564 (1979).2. Yen, G.-C., Chang, Y.-C., Sheu, F., et al. Isolation and characterization of antioxidant compounds from Aspergillus candidus broth filtrate. J. Agric. Food Chem. 49(3), 1426-1431 (2001).3. Wang, W., Liao, Y., Tang, C., et al. Cytotoxic and antibacterial compounds from the coral-derived fungus Aspergillus tritici SP2-8-1. Mar. Drugs 15(11), E348 (2017).4. Singh, S.B., Jayasuriya, H., Dewey, R., et al. Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites. J. Ind. Microbiol. Biotechnol. 30(12), 721-731 (2003).

SARS-CoV-2-IN-10 is a powerful and non-toxic inhibitor of SARS-CoV-2 3CL protease, with IC50 and EC50 values of 0.13 nM and 1.03 nM, respectively. The SARS-CoV-2 3C-like protease (3CLpro) is critical for viral replication and serves as an ideal target for intervention. By targeting the SARS-CoV-2 3CL protease, SARS-CoV-2-IN-10 has the potential to facilitate the development of effective antiviral drugs specific to SARS-CoV-2.

6-ethenylquinoline is a structurally unique aromatic heterocyclic compound that is an important intermediate in the production of other aromatic compounds. It has also been used as a starting material for the synthesis of a variety of drugs, including antifungal, antiparasitic and antiviral agents. It has been shown to be an inhibitor of a variety of enzymes involved in drug metabolism, including cytochrome P450, aldehyde oxidase and xanthine oxidase.

SARS-CoV-2 3CLpro-IN-1 (Compound 14c) is a highly potent inhibitor specifically designed to target and inhibit the activity of SARS-CoV-2 3CL pro, a cysteine protease found in the main coronaviruses. This enzyme is a promising target for antiviral drug development, positioning SARS-CoV-2 3CLpro-IN-1 as significant for advancing research in infectious diseases [1].

L-Xylulose is an intermediate in certain metabolic pathways and is classified as a rare sugar. It shows important physiological effects such as acting as an inhibitor of α-glucosidase and decreasing blood glucose, and it can be employed to produce other significant rare sugars, such as L-ribose and L-xylose which contribute to the production of antiviral drugs.

Nucleoside Derivatives –6-Modified purine nucleosides;N-Methylated nucleosides; Drugs and Inhibitors; Antiviral agent

Nucleoside Derivatives - 7-Deaza-purine nucleosides; Drugs and Inhibitors; Antiviral agent, anti-HCV

2'-Azido-2'-deoxycytidine is a nucleoside analogue and azido-modified cytidine that can undergo click chemistry reactions with molecules containing alkyne, DBCO, or BCN groups.

Nucleoside Derivatives - 3'-Deoxy nucleosides; Drugs and Inhibitors; Antiviral agent

Nucleoside Derivatives - 6-Modified purine nucleosides; Drugs and Inhibitors; Antiviral agent, cytokinin nucleoside

3-Deoxy-1,2;5,6-di-O-isopropylidene-D-glucofuranose is a polysaccharide oligosaccharide. It is used in glycosylation synthesis and can be custom synthesized for use as a carbohydrate in drugs. It has antiviral activity against Epstein-Barr virus by inhibiting viral protein synthesis.

2',3'-Bis-(O-t-butyldimethylsilyl)uridine is a nucleoside derivative with the ability to protect the NH2 OH groups of nucleosides. It has important applications in the synthesis of nucleoside analogs and antiviral drugs (e.g. AZT and acyclovir). The inhibitory effect on viral replication makes it useful in the fight against diseases such as AIDS and herpes.

Nucleoside Derivatives - Fluoro-modified nucleosides; 2',3'-Dideoxy nucleosides; Drugs and Inhbitors; Antiviral agent

Nucleoside Derivatives - 5-Modified pyrimidine nucleosides; Azido-nucleosides; 2',3'-Dideoxy nucleosides; Drugs and Inhibitors; Antiviral agent

8-Aminoquinoline is a molecular block that is a nitrogen-containing heterocyclic skeleton common in many natural products, functional materials and useful drugs. It has antibacterial, antiviral and anti-tumor activities, and can be used as an active ingredient in insecticides and herbicides.