868063-55-2Relevant academic research and scientific papers
Structure-activity studies in the development of a hydrazone based inhibitor of adipose-triglyceride lipase (ATGL)
Mayer, Nicole,Schweiger, Martina,Melcher, Michaela-Christina,Fledelius, Christian,Zechner, Rudolf,Zimmermann, Robert,Breinbauer, Rolf
, p. 2904 - 2916 (2015/03/30)
Adipose triglyceride lipase (ATGL) catalyzes the degradation of cellular triacylglycerol stores and strongly determines the concentration of circulating fatty acids (FAs). High serum FA levels are causally linked to the development of insulin resistance a
Discovery and structure-activity relationship of thienopyridine derivatives as bone anabolic agents
Saito, Keiji,Nakao, Akira,Shinozuka, Tsuyoshi,Shimada, Kousei,Matsui, Satoshi,Oizumi, Kiyoshi,Yano, Kazuki,Ohata, Keiko,Nakai, Daisuke,Nagai, Yoko,Naito, Satoru
, p. 1628 - 1642 (2013/04/24)
A cell-based assay was performed for the discovery of novel bone anabolic agents. Alkaline phosphatase (ALPase) activity of ST2 cells was utilized as an indicator of osteoblastic differentiation, and thienopyridine derivative 1 was identified as a hit compound. 3-Aminothieno[2,3-b]pyridine-2-carboxamide was confirmed to be a necessary core structure for the enhancement of ALPase activity, and then optimization of the C4-substituent on the thienopyridine ring was carried out. Introduction of cyclic amino groups to the C4-position of the thienopyridine ring improved the activity. Especially, N-phenyl-homopiperazine derivatives were found to be strong enhancers of ALPase among this new series. Furthermore, 3-amino-4-(4-phenyl-1,4-diazepan-1-yl)thieno[2,3-b]pyridine-2- carboxamide (15k) was orally administered to ovariectomized (OVX) rats over 6 weeks for evaluating the effects on areal bone mineral density (aBMD), and statistically significant improvements in aBMD were observed from the dosage of 10 mg/kg/day.
An improved synthesis of N-aryl and N-heteroaryl substituted homopiperazines-from conventional thermal conditions to scaling-up using microwave heating
Sch?n, Uwe,Messinger, Josef,Buckendahl,Prabhu,Konda
experimental part, p. 8125 - 8131 (2009/12/26)
An efficient Pd(0)-catalyzed Buchwald-Hartwig protocol for the facile preparation of N-aryl and N-heteroaryl substituted homopiperazines is described. The syntheses proceeded with aryl- and heteroaryl halides in high yields using X-Phos as best ligand. Th
