Other substances

N-[(2S)-1-[[(3S)-1-(benzenesulfonyl)-5-phenylpentan-3-yl]amino]-1-oxo-3-phenylpropan-2-yl]-4-methylpiperazine-1-carboxamide

A cysteine protease inhibitor.

Phase of research

Potential treatment - pre-clinical evidence

How it helps

Antiviral

Drug status

Experimental

1
 Supporting references
0
 Contradictory references
1
 AI-suggested references
1
 Clinical trials

General information

N-[(2S)-1-[[(3S)-1-(benzenesulfonyl)-5-phenylpentan-3-yl]amino]-1-oxo-3-phenylpropan-2-yl]-4-methylpiperazine-1-carboxamide is a potent irreversible covalent inhibitor of cathepsin L and certain other cysteine proteases. It displays anti-SARS-CoV-2 activity in vitro (Mellott et al., 2021).

N-[(2S)-1-[[(3S)-1-(benzenesulfonyl)-5-phenylpentan-3-yl]amino]-1-oxo-3-phenylpropan-2-yl]-4-methylpiperazine-1-carboxamide on PubChem

Synonyms

K777; K11777; S-001; SLV213; 4-methyl-N-((S)-1-oxo-3-phenyl-1-(((S)-1-phenyl-5-(phenylsulfonyl)pentan-3-yl)amino)propan-2-yl)piperazine-1-carboxamide

 

Structure image - N-[(2S)-1-[[(3S)-1-(benzenesulfonyl)-5-phenylpentan-3-yl]amino]-1-oxo-3-phenylpropan-2-yl]-4-methylpiperazine-1-carboxamide

CN1CCN(CC1)C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)N[C@@H](CCC3=CC=CC=C3)CCS(=O)(=O)C4=CC=CC=C4


 

Supporting references

Link Tested on Impact factor Notes Publication date
A Clinical-Stage Cysteine Protease Inhibitor blocks SARS-CoV-2 Infection of Human and Monkey Cells
Cathepsin L Small molecule Enzyme assay In vitro 		in vitro enzyme assay; Vero E6 cells; HeLa-ACE2 cells; Caco-2 cells; A549-ACE2 cells; Calu-3 cells; SARS-CoV-2 isolate USA_WA1/2020 4.43

The compound inhibited cathepsin L in vitro (with a KI of ca. 50 nM). It was also effective in blocking SARS-CoV-2 infection in various cell lines with an EC50 as low as 4 nM in Hela-ACE2 but being cell line-dependent.

 Mar/31/2021

AI-suggested references

Link Publication date
The C-C Chemokine Receptor Type 4 Is an Immunomodulatory Target of Hydroxychloroquine.
Aug/28/2020

Clinical trials

ID Title Status Phase Start date Completion date
NCT04843787 SLV213 Treatment in COVID-19 Patients Not yet recruiting Phase 2 May/01/2021 Oct/01/2021
  • Alternative id - SLV213-02
  • Interventions - Drug: SLV213|Drug: Placebo
  • Study type - Interventional
  • Study results - No Results Available
  • Locations -
  • Study designs - Allocation: Randomized|Intervention Model: Sequential Assignment|Masking: Quadruple (Participant, Care Provider, Investigator, Outcomes Assessor)|Primary Purpose: Treatment
  • Enrollment - 81
  • Age - 18 Years and older   (Adult, Older Adult)
  • Outcome measures - Treatment-Emergent Adverse Events|COVID-19 Symptom Improvements|COVID-19 Symptom Resolution|Negative SARC-CoV-2 Testing|SARS-CoV-2 Viral Load Change|SpO2/FiO2 Ratio Change|Oxygen Support|Hospitalization|COVID-19 Related Death
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