121348-15-0Relevant articles and documents
Discovery and optimization of thienopyridine derivatives as novel urea transporter inhibitors
Zhao, Yan,Li, Min,Li, Bowen,Zhang, Shun,Su, Aoze,Xing, Yongning,Ge, Zemei,Li, Runtao,Yang, Baoxue
, p. 131 - 142 (2019/04/08)
Urea transporters (UTs) play an important role in the urine concentrating mechanism and are recognized as novel targets for developing small molecule inhibitors with salt-sparing diuretic activity. Thienoquinoline derivatives, a class of novel UT-B inhibitors identified by our group, play a significant diuresis in animal model. However, the poor solubility and low bioavailability limited its further development. To overcome these shortcomings, the structure modification of thienoquinoline was carried out in this study, which led to the discovery of novel thienopyridine derivatives as specific urea transporter inhibitors. Further optimization obtained the promising preclinical candidate 8n with not only excellent inhibition effect on urea transporters and diuretic activity on rat model, but also suitable water solubility and Log P value.
Substituted pyridylethanolamine livestock production promoters
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, (2008/06/13)
For promoting livestock production, the novel substituted pyridylethanolamines of the formula STR1 in which R1 represents CN, --COOR8 or --CONR9 R10, R2 represents optionally substituted alkyl, R3 represents hydrogen, alkyl or alkenyl, R4 represents hydrogen or optionally substituted alkyl or alkenyl, or R3 and R4 represent, together with the nitrogen atom to which they are bonded, an optionally substituted heterocyclic radical, R5 represents OH, acyloxy or alkoxy, R6 represents hydrogen or alkyl, R7 represents hydrogen, alkyl, cycloalkyl, substituted alkyl, optionally substituted aralkyl, aryl or heterocyclyl, R6 and R7 can, together with the nitrogen atom to which they are bonded, represent an optionally substituted heterocyclic radical, R8 represents alkyl, and R9 and R10, independently of one another, represent hydrogen, alkyl or alkenyl or, together with the nitrogen atom to which they are bonded, represent an optionally substituted heterocyclic radical, or a physiologically tolerated salt or N-oxide thereof. Some intermediates are also new.