132187-71-4Relevant academic research and scientific papers
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)
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.
Potential cardiotonic agents. 10. Synthesis and positive inotropic action of 5-(4-pyridinyl)- and 5-phenyl-substituted 2-alkylthio-3-cyan-pyridines and their S-oxidation products
Rumler,Hagen,Hagen
, p. 657 - 659 (2007/10/02)
The alkylation of the 5-(4-pyridinyl)- and 5-phenyl-substituted 3-cyan-2(1H)-pyridinethiones 1 with alkyl iodides and halomethylcarbonyl compounds led to the 2-alkylthio-pyridines 3a-c, 3e, 3f and the thieno[2,3-b]pyridines 4, respectively. In an other wa
