Bhagwat, Shripad S.; Gude, Candido; Boswell, Clay; Contardo, Nicolina; Cohen, David S.; Dotson, Ronald; Mathis, Janice; Lee, Warren; Furness, Patricia; Zoganas, Harry published the artcile< Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-[3-(3-pyridinyl)propyl]octanoic acid and analogs>, Application of C11H16O2, the main research area is chlorophenylsulfonylaminopyridinylpropyloctanoic acid preparation thromboxane antagonist; arylsulfonylaminopyridinylpropyloctanoic acid analog preparation thromboxane antagonist; thromboxane receptor antagonist synthase inhibitor arylsulfonylaminopyridinylpropyloctanoic.
The title compound [I, A = (CH2)2CO2H, B = (CH2)3Py, X = Cl; Py = 3-pyridyl] (II) and its analogs were synthesized and found to possess two activities, the inhibition of the biosynthesis of thromboxane A2 and antagonism of its receptors. Thus, II was prepared via arylsulfonylation of Et 6-amino-2-[(3-pyridinyl)propyl)]hexanoate, reduction, Wittig reaction with Ph3P:CHCO2Me, and treatment with NaBH4/CoCl2/MeOH. The in vitro and in vivo profile of these compounds as thromboxane receptor antagonists (TxRAs) and thromboxane synthase inhibitors (TxSls) is described. II and its analogs I [A = CO2H, NHCOCO2H, (CH2)3OH, SCH2CO2H, etc., B = (CH2)2OPy, CH2CH:CHPy, (CH2)2Im, X = F, OMe, N3, CF3, SO2Me; Im = 1-imidazolyl] displayed very potent TxRA activity in human washed platelets (IC50 ≈ 10-7-10-9 M) and dog saphenous vein (pA2 ≈ 9) and also potent TxSl activity (IC50 ≈ 10-9 M). The good bioavailability and the long duration of action of some of these compounds was demonstrated using ex vivo measurement of the TxRA and TxSl activities upon oral administration to guinea pigs. I [A = (CH2)2CO2H, B = (CH2)2OPy, X = Cl; A = SCH2CO2H, B = (CH2)3Py, X = Cl] and II potently inhibited arachidonic acid induced bronchoconstriction in guinea pigs.
Journal of Medicinal Chemistry published new progress about Thromboxane receptor TBXA2R Role: RCT (Reactant), RACT (Reactant or Reagent). 52244-70-9 belongs to class ethers-buliding-blocks, and the molecular formula is C11H16O2, Application of C11H16O2.
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem