| Iupac name | N3-cyclopropyl-7-[(4-propan-2-ylphenyl)methyl]pyrrolo[3,2-f]quinazoline-1,3-diamine |
|---|---|
| Width | 220 |
| Cas number | 1216720-69-2 |
| Pubchem | 4259181 |
| Chemspiderid | 3466882 |
| Chebi | 94998 |
| C | 23 |
| H | 25 |
| N | 5 |
| Smiles | CC(C)C1=CC=C(C=C1)CN2C=CC3=C2C=CC4=C3C(=NC(=N4)NC5CC5)N |
| Stdinchi | 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) |
| Stdinchikey | 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
- ^ 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
- ^ 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
- ^ Semenikhina M, Bogovyk R, Fedoriuk M, Nikolaienko O, Al Kury LT, Savotchenko A, Krishtal O, Isaeva E (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
- ^ Pontecorvi P, Banki MA, Zampieri C, Zalfa C, Azmoon P, Kounnas MZ, Marchese C, Gonias SL, Mantuano E (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
- ^ Yokono Y, Hanada K, Narita M, Tatara Y, Kawamura Y, Miura N, Kitayama K, Nakata M, Nozaka M, Kato T, Kudo N, Tsushima M, Toyama Y, Itoh K, Tomita H (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). doi:10.1161/JAHA.119.015616. PMC 7429042. PMID 32495720
- ^ Gupta N, Liu R, Shin S, Sinha R, Pogliano J, Pogliano K, Griffin JH, Nizet V, Corriden R (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
- ^ Martin JK, Sheehan JP, Bratton BP, Moore GM, Mateus A, Li SH, Kim H, Rabinowitz JD, Typas A, Savitski MM, Wilson MZ, Gitai Z (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