PH-797804

PH-797804
Identifiers
	IUPAC name 3-[3-bromo-4-[(2,4-difluorophenyl)methoxy]-6-methyl-2-oxopyridin-1-yl]-N,4-dimethylbenzamide;
CAS Number	586379-66-0;
PubChem CID	22049997;
IUPHAR/BPS	7818;
DrugBank	DB07941;
ChemSpider	10796940;
UNII	SI09I1V827;
ChEBI	CHEBI:82715;
ChEMBL	ChEMBL1088751;
CompTox Dashboard (EPA)	DTXSID70207342 ;
Chemical and physical data
Formula	C22H19BrF2N2O3
Molar mass	477.306 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=C(C=C(C=C1)C(=O)NC)N2C(=CC(=C(C2=O)Br)OCC3=C(C=C(C=C3)F)F)C;
	InChI InChI=1S/C22H19BrF2N2O3/c1-12-4-5-14(21(28)26-3)9-18(12)27-13(2)8-19(20(23)22(27)29)30-11-15-6-7-16(24)10-17(15)25/h4-10H,11H2,1-3H3,(H,26,28); Key:KCAJXIDMCNPGHZ-UHFFFAOYSA-N;

PH-797804 is a drug which acts as a selective inhibitor of the enzyme p38 mitogen-activated protein kinase (p38 MAPK). It has antiinflammatory effects and has been researched for the treatment of inflammatory lung conditions such as chronic obstructive pulmonary disease and COVID-19. While it has not been adopted for clinical use, it remains widely used in research.^[1]^[2]^[3]^[4]^[5]

References

^ Hope HR, Anderson GD, Burnette BL, Compton RP, Devraj RV, Hirsch JL, et al. (December 2009). "Anti-inflammatory properties of a novel N-phenyl pyridinone inhibitor of p38 mitogen-activated protein kinase: preclinical-to-clinical translation". The Journal of Pharmacology and Experimental Therapeutics. 331 (3): 882–895. doi:10.1124/jpet.109.158329. PMID 19720877.
^ Selness SR, Devraj RV, Devadas B, Walker JK, Boehm TL, Durley RC, et al. (July 2011). "Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase". Bioorganic & Medicinal Chemistry Letters. 21 (13): 4066–4071. doi:10.1016/j.bmcl.2011.04.121. PMID 21641211.
^ MacNee W, Allan RJ, Jones I, De Salvo MC, Tan LF (August 2013). "Efficacy and safety of the oral p38 inhibitor PH-797804 in chronic obstructive pulmonary disease: a randomised clinical trial". Thorax. 68 (8): 738–745. doi:10.1136/thoraxjnl-2012-202744. PMID 23539534.
^ Chaudhary O, Narayan V, Lelis F, Linz B, Watkins M, Veazey R, et al. (August 2018). "Inhibition of p38 MAPK in combination with ART reduces SIV-induced immune activation and provides additional protection from immune system deterioration". PLOS Pathogens. 14 (8): e1007268. doi:10.1371/journal.ppat.1007268. PMC 6135519. PMID 30161247.
^ Faist A, Schloer S, Mecate-Zambrano A, Janowski J, Schreiber A, Boergeling Y, et al. (January 2023). "Inhibition of p38 signaling curtails the SARS-CoV-2 induced inflammatory response but retains the IFN-dependent antiviral defense of the lung epithelial barrier". Antiviral Research. 209: 105475. doi:10.1016/j.antiviral.2022.105475. PMC 9677559. PMID 36423831.

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[1] Hope HR, Anderson GD, Burnette BL, Compton RP, Devraj RV, Hirsch JL, et al. (December 2009). "Anti-inflammatory properties of a novel N-phenyl pyridinone inhibitor of p38 mitogen-activated protein kinase: preclinical-to-clinical translation". The Journal of Pharmacology and Experimental Therapeutics. 331 (3): 882–895. doi:10.1124/jpet.109.158329. PMID 19720877.

[2] Selness SR, Devraj RV, Devadas B, Walker JK, Boehm TL, Durley RC, et al. (July 2011). "Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase". Bioorganic & Medicinal Chemistry Letters. 21 (13): 4066–4071. doi:10.1016/j.bmcl.2011.04.121. PMID 21641211.

[3] MacNee W, Allan RJ, Jones I, De Salvo MC, Tan LF (August 2013). "Efficacy and safety of the oral p38 inhibitor PH-797804 in chronic obstructive pulmonary disease: a randomised clinical trial". Thorax. 68 (8): 738–745. doi:10.1136/thoraxjnl-2012-202744. PMID 23539534.

[4] Chaudhary O, Narayan V, Lelis F, Linz B, Watkins M, Veazey R, et al. (August 2018). "Inhibition of p38 MAPK in combination with ART reduces SIV-induced immune activation and provides additional protection from immune system deterioration". PLOS Pathogens. 14 (8): e1007268. doi:10.1371/journal.ppat.1007268. PMC 6135519. PMID 30161247.

[5] Faist A, Schloer S, Mecate-Zambrano A, Janowski J, Schreiber A, Boergeling Y, et al. (January 2023). "Inhibition of p38 signaling curtails the SARS-CoV-2 induced inflammatory response but retains the IFN-dependent antiviral defense of the lung epithelial barrier". Antiviral Research. 209: 105475. doi:10.1016/j.antiviral.2022.105475. PMC 9677559. PMID 36423831.

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See also

References