Wikipedia

N-0385

N-0385 is an experimental small molecule TMPRSS2-inhibitor being investigated for its potential use in the prevention and treatment of COVID-19.[1][2][3][4]

N-0385
Clinical data
Other namesMs-QFR-Kbt
Routes of
administration		Intranasal
Identifiers
  • (2S)-N-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2-(methanesulfonamido)pentanediamide
PubChem CID
Chemical and physical data
FormulaC28H36N8O6S2
Molar mass644.77 g·mol−1
3D model (JSmol)
  • CS(=O)(=O)NC(CCC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(CCCN=C(N)N)C(=O)C2=NC3=CC=CC=C3S2
  • InChI=1S/C28H36N8O6S2/c1-44(41,42)36-20(13-14-23(29)37)25(39)34-21(16-17-8-3-2-4-9-17)26(40)33-19(11-7-15-32-28(30)31)24(38)27-35-18-10-5-6-12-22(18)43-27/h2-6,8-10,12,19-21,36H,7,11,13-16H2,1H3,(H2,29,37)(H,33,40)(H,34,39)(H4,30,31,32)/t19-,20-,21-/m0/s1
  • Key:JTHVOFMYRRNGPA-ACRUOGEOSA-N

Mechanism of action edit

N-0385 is thought to have antiviral effects by targeting key proteins involved in the viral entry process, including TMPRSS2, ACE2, and DPP4. By interfering with the interactions between these proteins and the SARS-CoV-2 spike protein, N-0385 effectively blocks the virus from gaining access to host cells.[3][4] Additionally, N-0385 appears to modify the immune responses and inflammatory pathways associated with the infection by regulating TLR7, NLRP3, and IL-10, potentially reducing the severity of COVID-19 symptoms and reducing tissue damage associated with the infection.[4]

References edit

  1. ^ Sankaran, Vishwam (30 March 2022). "New nasal spray found 'effective' in preventing and treating Covid in mice". The Independent. Retrieved 16 November 2023.
  2. ^ Reynolds, Sharon (11 April 2022). "Nasal antiviral blocks SARS-CoV-2 infection in mice". Institutes of Health (NIH). Retrieved 16 November 2023.
  3. ^ a b Shapira T, Monreal IA, Dion SP, Buchholz DW, Imbiakha B, Olmstead AD, Jager M, Désilets A, Gao G, Martins M, Vandal T, Thompson C, Chin A, Rees WD, Steiner T, Nabi IR, Marsault E, Sahler J, Diel DG, Van de Walle GR, August A, Whittaker GR, Boudreault PL, Leduc R, Aguilar HC, Jean F (May 2022). "A TMPRSS2 inhibitor acts as a pan-SARS-CoV-2 prophylactic and therapeutic". Nature. 605 (7909): 340–348. Bibcode:2022Natur.605..340S. doi:10.1038/s41586-022-04661-w. PMC 9095466. PMID 35344983.
  4. ^ a b c Cao JF, Yang X, Xiong L, Wu M, Chen S, Xiong C, He P, Zong Y, Zhang L, Fu H, Qi Y, Ying X, Liu D, Hu X, Zhang X (October 2022). "Mechanism of N-0385 blocking SARS-CoV-2 to treat COVID-19 based on molecular docking and molecular dynamics". Frontiers in Microbiology. 13. doi:10.3389/fmicb.2022.1013911. PMC 9622768. PMID 36329841.


 

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