sars cov-1

PF-00835231 is a CoV-2 cysteine 3C-like protease (3CLpro) inhibitor, with IC50s of 0.27 nM and 4 nM for SARS CoV-2 and SARS CoV-1 3CLpro, respectively. PF-00835231 is the active compound of the first anti-3CLpro regimen in clinical trials.

Tipranavir is a protease inhibitor that inhibits HIV-1 resistant to more than 1 protease inhibitor .Tipranavir effectively inhibits HIV-1 protease enzyme activity and dimerisation and has potent activity against multiple protease inhibitor (PI) HIV-1 isolates (IC50 of 66-410 nM). Tipranavir inhibits SARS-CoV-2 3CLpro activity.

YH-53 is a potent peptidomimetic 3CLpro inhibitor featuring a unique benzothiazolyl ketone pharmacophore that displays low-nanomolar inhibition of SARS-CoV-1 and SARS-CoV-2 main proteases and effectively blocks SARS-CoV-2 replication, thereby providing a structurally distinctive and mechanistically validated compound for antiviral and COVID-19 research.

Chloroquine is a Toll-like receptor inhibitor that inhibits autophagy. Chloroquine has anti-malarial and anti-inflammatory activity and is widely used in the treatment of malaria and rheumatoid arthritis. Chloroquine also has anti-SARS-CoV-2 (COVID-19) activity and anti-HIV-1 activity.

CTP Synthetase-IN-1 Ammonium salt is an orally active and potent cytidine 5'-triphosphate synthetase (CTPS) inhibitor with potential antimicrobial, anti-inflammatory and antitumor activity for the study of SARS-CoV-2 viral infections.

PLpro/RBD-IN-1 is a dual inhibitor of SARS-CoV-2 PLpro and the spiny protein RBD, with anti-novel coronavirus activity, and is seen for the study of viral infections.

SARS-CoV-2 Mpro-IN-9 (compound c7), a nonpeptidic, noncovalent inhibitor of SARS-CoV-2 main protease (Mpro), exhibits potent inhibitory action (IC50 = 0.085 μM) and improved physicochemical and drug metabolism and pharmacokinetics (DMPK) properties. It effectively suppresses viral replication in SARS-CoV-2-infected Vero E6 cells (EC50 = 1.10 μM) and demonstrates low cytotoxicity (CC50 > 50 μM) [1].

Piperazine,1-(4-fluorophenyl)-4-[(3,4,5-trimethoxyphenyl)methyl]- is a piperazine derivative with anti-SARS-CoV-2 activity.

Atazanavir sulfate (BMS-232632 sulfate) is an azapeptide and HIV-protease inhibitor used in the treatment of HIV infections and AIDS in combination with other anti-HIV agents.

Atazanavir (BMS-232632)(BMS-232632) is an highly effective HIV-1 protease inhibitor.

Mefloquine hydrochloride (Mefloquin hydrochloride) is a quinoline derivative used for the prevention and therapy of P. falciparum malaria.

Mizoribine (NSC-289637) belongs to the family of 1-Ribosyl-imidazolecarboxamides. Mizoribine has been investigated for the treatment of Rheumatoid Arthritis.

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

Ritonavir (ABT 538) is a peptidomimetic agent that inhibits both HIV-1 and HIV-2 proteases. Ritonavir is highly inhibited by serum proteins but boosts the effect of other HIV proteases by blocking their degradation by cytochrome P450.

Lopinavir (ABT-378) is a peptidomimetic HIV protease inhibitor effective against HIV protease with the Val 82 mutation. It is less affected by serum protein binding compared to the structurally related drug ritonavir.

Velpatasvir (GS-5816), also known as GS-5816, is a potent and selective Hepatitis C virus NS5A inhibitor. GS-5816 has demonstrated pan-genotypic activity and a high barrier to resistance in HCV replicon assays. GS-5816 demonstrated pangenotypic antiviral activity in patients with genotype 1-4 HCV infection. It will be further evaluated in combination with other pangenotypic direct-acting antivirals to achieve the goal of developing a well-tolerated, highly effective treatment for all HCV genotypes.

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

Umifenovir is a potent, orally active broad-spectrum antiviral agent with activity against enveloped and non-enveloped viruses, suppressing virus propagation and modulating the expression of inflammatory cytokines for use as an anti-influenza virus agent [3]. It effectively inhibits the fusion of the virus with host cells [1] [2] and is an efficient inhibitor of SARS-CoV-2 in vitro [2].

SARS-CoV-2-IN-39 is a SARS-CoV-2 inhibitor with an EC50 of 1 μM. SARS-CoV-2-IN-39 has antiviral activity and inhibits SARS-CoV-2 by inhibiting SKP2 protein and stabilizing BECN1.

MERS-CoV-IN-1 exhibits excellent inhibitory activity against coronavirus and is useful as a pharmaceutical composition for preventing coronavirus-induced diseases (MERS-CoV and SARS).

Azelastine (Azelastinum) is a phthalazine derivative, and is an histamine antagonist and mast cell stabilizer.

Azelastine hydrochloride (Astelin) is a phthalazinone derivative with antihistaminergic activity.

Mefloquine (Ro 215998), a quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine is also a K+ channel (KvQT1/minK) antagonist with an IC50 of ~1 μM. Mefloquine can be used for malaria, systemic lupus erythematosus, and cancer research.

Ecteinascidin 770 inhibits SARS-CoV-2 and Mycobacterium tuberculosis by inhibiting cancer cell viability through RDRP1 (RNA-dependent RNA polymerase 1).