SCH-79797

Last updated
SCH-79797
SCH-79797 structure.png
Identifiers
  • N3-cyclopropyl-7-[(4-propan-2-ylphenyl)methyl]pyrrolo[3,2-f]quinazoline-1,3-diamine
CAS Number
PubChem CID
ChemSpider
ChEBI
Chemical and physical data
Formula C23H25N5
Molar mass 371.488 g·mol−1
3D model (JSmol)
  • CC(C)C1=CC=C(C=C1)CN2C=CC3=C2C=CC4=C3C(=NC(=N4)NC5CC5)N
  • InChI=1S/C23H25N5/c1-14(2)16-5-3-15(4-6-16)13-28-12-11-18-20(28)10-9-19-21(18)22(24)27-23(26-19)25-17-7-8-17/h3-6,9-12,14,17H,7-8,13H2,1-2H3,(H3,24,25,26,27)
  • Key:AVXQPEKZIGPIJW-UHFFFAOYSA-N

SCH-79797 is a drug which acts as a potent and selective antagonist of the thrombin receptor proteinase activated receptor 1 (PAR1). [1] It has anticoagulant, anticonvulsant and antiinflammatory effects and has been researched as a treatment for heart attack and stroke, though never developed for medical use. [2] [3] [4] [5] It also shows antibiotic actions which are not shared with other PAR1 antagonists such as vorapaxar, so may be mediated through a different target than PAR1. [6] [7]

References

  1. ↑ Ahn HS, Foster C, Boykow G, Stamford A, Manna M, Graziano M (November 2000). "Inhibition of cellular action of thrombin by N3-cyclopropyl-7-{[4-(1-methylethyl)phenyl]methyl}-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine (SCH 79797), a nonpeptide thrombin receptor antagonist". Biochemical Pharmacology. 60 (10): 1425–34. doi:10.1016/s0006-2952(00)00460-3. PMID   11020444.
  2. ↑ Yang JN, Chen J, Xiao M (February 2017). "A protease-activated receptor 1 antagonist protects against global cerebral ischemia/reperfusion injury after asphyxial cardiac arrest in rabbits". Neural Regeneration Research. 12 (2): 242–249. doi: 10.4103/1673-5374.199011 . PMC   5361508 . PMID   28400806.
  3. ↑ Semenikhina M, Bogovyk R, Fedoriuk M, Nikolaienko O, Al Kury LT, Savotchenko A, et al. (January 2019). "Inhibition of protease-activated receptor 1 ameliorates behavioral deficits and restores hippocampal synaptic plasticity in a rat model of status epilepticus". Neuroscience Letters. 692: 64–68. doi:10.1016/j.neulet.2018.10.058. PMID   30391321. S2CID   53217829.
  4. ↑ Pontecorvi P, Banki MA, Zampieri C, Zalfa C, Azmoon P, Kounnas MZ, et al. (December 2019). "Fibrinolysis protease receptors promote activation of astrocytes to express pro-inflammatory cytokines". Journal of Neuroinflammation. 16 (1): 257. doi: 10.1186/s12974-019-1657-3 . PMC   6896679 . PMID   31810478.
  5. ↑ Yokono Y, Hanada K, Narita M, Tatara Y, Kawamura Y, Miura N, et al. (June 2020). "Blockade of PAR-1 Signaling Attenuates Cardiac Hypertrophy and Fibrosis in Renin-Overexpressing Hypertensive Mice". Journal of the American Heart Association. 9 (12) e015616. doi: 10.1161/JAHA.119.015616 . PMC   7429042 . PMID   32495720.
  6. ↑ Gupta N, Liu R, Shin S, Sinha R, Pogliano J, Pogliano K, et al. (June 2018). "SCH79797 improves outcomes in experimental bacterial pneumonia by boosting neutrophil killing and direct antibiotic activity". The Journal of Antimicrobial Chemotherapy. 73 (6): 1586–1594. doi: 10.1093/jac/dky033 . PMC   5961356 . PMID   29514266.
  7. ↑ Martin JK, Sheehan JP, Bratton BP, Moore GM, Mateus A, Li SH, et al. (May 2020). "A Dual-Mechanism Antibiotic Kills Gram-Negative Bacteria and Avoids Drug Resistance". Cell. 181 (7): 1518–1532.e14. doi:10.1016/j.cell.2020.05.005. PMC   7780349 . PMID   32497502. S2CID   219300022.
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