sars-cov-2-in-11

SARS-CoV-2-IN-11 is a highly potent and non-toxic inhibitor of the 3C-like protease (3CLpro) of SARS-CoV-2, with IC50 and EC50 values of 0.17 nM and 1.45 nM, respectively. This compound targets the essential viral replication enzyme (3CLpro), making it an attractive candidate for intervention strategies and holds significant promise in the development of specific antivirals against SARS-CoV-2.

SARS-CoV-2-IN-110 (compound Bb1) is an inhibitor of SARS-CoV-2, demonstrating antiviral efficacy with an EC50 of 1.10 μM, and significantly reduced toxicity compared to Lapatinib. The compound exhibits a CC50 of greater than 100 μM against SARS-CoV-2, with a selectivity index (SI) exceeding 91.

SARS-CoV-2-IN-111 (compound 77) is a highly effective inhibitor of SARS-CoV-2, exhibiting an IC50 of 0.67 μM. It markedly decreases the presence of SARS-CoV-2 within Vero cells.

SARS-CoV-2-IN-115 (Compound 3e) is a potent inhibitor of SARS-CoV-2, showing strong antiviral activity in infected Calu-3 cells with an EC50 of 1.7 μM. It effectively inhibits human dihydroorotate dehydrogenase (HsDHODH) activity with an IC50 of 1.5 μM. Importantly, SARS-CoV-2-IN-115 maintains immune response without affecting the proliferation of CD4 T cells.

SARS-CoV-2-IN-114 (Compound 36) is an antiviral agent with significant activity against both the original SARS-CoV-2 strain and the Delta variant. It inhibits the cytopathic effect (CPE) of the original SARS-CoV-2 strain with an EC50 of 0.29 μM and 5.77 μM for the Delta variant. SARS-CoV-2-IN-114 exhibits low cytotoxicity, making it suitable for coronavirus research.

SARS-CoV-2-IN-112 (Compound 6f) is an orally active, non-peptidic inhibitor of the SARS-CoV-2 main protease with an IC50 of 6.48 μM. It exhibits potent antiviral activity while demonstrating low cytotoxicity against WI-38 cells (IC50: 53.81 μM). SARS-CoV-2-IN-112 is applicable for coronavirus COVID-19 research.

SARS-CoV-2-IN-113 (Compound 24) is a sulfonyl hydrazine derivative that exhibits antiviral activity against SARS-CoV-2 infection, with an IC50 of 8.320 μM. It effectively inhibits the entry and replication of SARS-CoV-2 by downregulating genes and proteins such as Spike, ACE-2, and RdRp. SARS-CoV-2-IN-113 shows high selectivity and low cytotoxicity, making it a valuable candidate for COVID-19 research.

SARS-CoV-2-IN-117 (Compound C19) is an inhibitor of the SARS-CoV-2 E protein. It effectively disrupts the interaction between the SARS-CoV-2 E protein and the host ZO-1 PDZ2 domain. This compound exhibits potent antiviral activity and significantly reduces viral replication. SARS-CoV-2-IN-117 is applicable for COVID-19 research.

SARS-CoV-2-IN-118 (compound A.13) is an inhibitor that targets the translation initiation element SL1 of SARS-CoV-2 RNA.

SARS-CoV-2-IN-116 (Compound (S,S)-4) is a highly selective inhibitor of angiotensin-converting enzyme 2 (ACE2) with a pIC50 of 7.61. It prevents the binding of the SARS-CoV-2 spike protein to ACE2 and holds promise for research related to COVID-19.

SARS-CoV-2 Mpro-IN-31 (Compound 18) is an inhibitor of SARS-CoV-2 MPro with an IC50 of 11 nM. Additionally, this compound effectively inhibits the enzymatic activity of the cysteine proteases cathepsin B and cathepsin L, with IC50 values of 24 nM and 1.8 nM, respectively.

Mpro inhibitor N3 hemihydrate is a potent antagonist of the SARS-CoV-2 main protease (Mpro), with an EC50 of 16.77 μM against SARS-CoV-2. It specifically inhibits Mpro in various coronaviruses, including SARS-CoV, MERS-CoV, HCoV-229E (IC50 4.0 μM), FIPV (IC50 8.8 μM), and MHV-A59 (IC50 2.7 μM) [1][2].

SARS-CoV-2-IN-15 (compound 11) is a niclosamide analogue exhibiting greater stability in human plasma and liver S9 enzyme assays compared to niclosamide. It enhances bioavailability and half-life upon oral administration and is a potent SARS-CoV-2 inhibitor with an IC50 of 0.49 μM [1].

Covidcil-19 binds to the revised attenuator hairpin structure of the SARS-CoV-2 frameshifting element (FSE) with high affinity (Kd = 11 nM). It stabilizes the hairpin's folded state and reduces frameshifting efficiency in cells. Covidcil-19 inhibits viral propagation and reduces viral infectivity by > 3.5 orders of magnitude.

SARS-CoV-2 3CLpro-IN-11(11d) is a broad-spectrum antiviral compound that inhibits the SARS-CoV-2 3CL protease with an IC50 of 140 nM, and also exhibits inhibitory activity against SARS-CoV-1 and MERS-CoV with IC50 values of 240 nM and 70 nM, respectively.

Bamlanivimab, an Anti-Human SARS-CoV-2 monoclonal antibody (mAb), was the first of its kind to receive Emergency Use Authorization (EUA) from the U.S. Food and Drug Administration (FDA) in November 2020 for COVID-19 treatment. However, its authorization was withdrawn in April 2021 due to emerging SARS-CoV-2 variants resistant to the antibody [1].

SARS-CoV-2-IN-92 (compound 11) effectively inhibits variants of SARS-CoV-2 (EC50= 0.48 μM), as well as SARS-CoV and MERS-CoV. Additionally, this compound robustly and selectively blocks ERα-Glu II.