42287-97-8Relevant academic research and scientific papers
Synthesis and in vitro evaluation of human FP-receptor selective prostaglandin analogues
DeLong, Mitchell A.,Amburgey, Jack,Taylor, Cynthia,Wos, John A.,Soper, David L.,Wang, Yili,Hicks, Renee
, p. 1519 - 1522 (2007/10/03)
The in vitro evaluation of a series of saturated prostaglandins revealed that compounds with omega chin aromatic rings retain nanomolar potency for the human prostaglandin F receptor (hFP receptor), exemplified by compound 8. In contrast, the double bonds are required for activity in the series with an acyclic omega chain as in PGF(2α). (C) 2000 Published by Elsevier Science Ltd.
Identification and initial structure-activity relationships of a novel class of nonpeptide inhibitors of blood coagulation factor Xa
Klein, Scott I.,Czekaj, Mark,Gardner, Charles J.,Guertin, Kevin R.,Cheney, Daniel L.,Spada, Alfred P.,Bolton, Scott A.,Brown, Karen,Colussi, Dennis,Heran, Christopher L.,Morgan, Suzanne R.,Leadley, Robert J.,Dunwiddie, Christopher T.,Perrone, Mark H.,Chu, Valeria
, p. 437 - 450 (2007/10/03)
The discovery and some of the basic structure-activity relationships of a series of novel nonpeptide inhibitors of blood coagulation Factor Xa is described. These inhibitors are functionalized β-alanines, exemplified by 2a. Docking experiments placing 2a in the active site of Factor Xa implied that the most expeditious route to enhancing in vitro potency was to modify the group occupying the S3 site of the enzyme. Increasing the hydrophobic contacts between the inhibitor and the enzyme in this region led to 8, which has served as the prototype for this series. In addition, an enantioselective synthesis of these substituted β-alanines was also developed.
Organic compounds and their pharmaceutical use
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, (2008/06/13)
There are provided anti-allergic pharmaceutical compounds of formula: STR1 in which n is 0, 1 or 2; R1 is a hydrocarbyl group containing 6 to 30 carbon atoms and optionally substituted with an optionally substituted phenyl group; R2
