69917-84-6Relevant academic research and scientific papers
- and pyrroles as Thromboxane Synthetase Inhibitors
Martinez, Gregory R.,Walker, Keith A. M.,Hirschfeld, Donald R.,Maloney, Patrick J.,Yang, Diana S.,Rosenkranz, Roberto P.
, p. 890 - 897 (2007/10/02)
Several and pyrroles were prepared and evaluated in vitro as thromboxane synthetase inhibitors in human platelet aggregation studies.A number of structures, e.g. 10b,f,g,i (respective IC50 values: 1 μM, 50 nM, 42 nM, 44 nM) showed superior in vitro inhibition of TXA2 synthetase when compared to the standard dazoxiben (1).However, it was found that in vitro potency did not translate into nor correlate with in vivo activity when these compounds were evaluated in mice in a collagen-epinephrine-induced pulmonary thromboembolism model. (E)-1-Methyl-2--5-(2-carboxyprop-1-enyl)pyrrole (10b) was found to offer protection against collagen-epinephrine-induced mortality in mice, thereby demonstrating that oral administration is an effective route for absorption of this drug.Additional evidence for the oral effectiveness of 10b in lowering serum TXB2 levels was obtained by performing ex vivo radioimmunoassay experiments with rats.A 13-week study of 10b in rats with reduced renal mass was conducted in order to evaluate the role of TXA2 production in hypertension and renal dysfunction.Although serum and urinary TXB2 levels in rats were found to be lowered during this study by 10b, the levels of urinary protein excretion remained comparable to that of the control group.
Utilisation of 13C N.M.R. Spectroscopy for the Identification of E- and Z-α,β-Unsaturated Esters, Ketones and Nitriles.
Gregory, Barrie,Hinz, Werner,Jones, R. Alan,Arques, Jose Sepulveda
, p. 2801 - 2821 (2007/10/02)
Measurement of 3JCO,H coupling constants provides an unambiguous procedure for the configurational analysis of substituted 2- and 3-arylpropenoic esters and of E- and Z-2-arylbut-2-en-1,4-dioates, even when only one of the isomers is available for analysis.An analogous procedure can also be used for the configurational analysis of 3-arylpropenonitriles and of 4-arylbut-3-en-2-ones.
