Name: Pyrrophenone
Rating: 5 (10 reviews)

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HIT ID:HIT214321604
Cas No:341973-06-6
常用名:Pyrrophenone
IUPAC:N-{[(2S,4R)-1-[2-(2,4-difluorobenzoyl)benzoyl]-4-[(triphenylmethyl)sulfanyl]pyrrolidin-2-yl]methyl}-4-{[(5Z)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl}benzamide
IUPAC:N-{[(2S,4R)-1-[2-(2,4-difluorobenzoyl)benzoyl]-4-[(triphenylmethyl)sulfanyl]pyrrolidin-2-yl]methyl}-4-{[(5Z)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl}benzamide
InChI key:XSCZRVUQXBBTRO-GYCZXHFISA-N

分子式:C49H37F2N3O5S2
分子量:849.97
氢键供体数 (HBD):
氢键受体数 (HBA):
LogP:
SMILES:Fc1ccc(C(=O)c2ccccc2C(=O)N2C[C@@H](C[C@H]2CNC(=O)c2ccc(\C=C3/SC(=O)NC3=O)cc2)SC(c2ccccc2)(c2ccccc2)c2ccccc2)c(F)c1
SMILES:Fc1ccc(C(=O)c2ccccc2C(=O)N2C[C@@H](C[C@H]2CNC(=O)c2ccc(\C=C3/SC(=O)NC3=O)cc2)SC(c2ccccc2)(c2ccccc2)c2ccccc2)c(F)c1

The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid (AA) from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins (PGs) and leukotrienes (LTs). Pyrrophenone inhibits cPLA2α with an IC50 of 4.2 nM in enzyme assays and potently blocks the release of AA and the production of PGE2 and LTC4 in cells (IC50 = 24, 25, and 14 nM, respectively). Its action is reversible and selective, as pyrrophenone inhibits the secretory type IB and IIA PLA2s with more than a hundred-fold less potency. Pyrrophenone has also been shown to inhibit calcium ionophore (A23187)-stimulated AA release from monocytic cells, interleukin-1-induced PGE2 synthesis in mesangial cells, and the production of PGE2, LTs, and platelet-activating factor by human neutrophils, always with maximal inhibition at concentrations below 1 μM.

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