370867-83-7Relevant academic research and scientific papers
Ligand-free PdCl2-catalyzed heck reaction of arylboronic acids and olefins under reusable TBAB/H2O conditions
Tang, Bo-Xiao,Fang, Xiao-Niu,Kuang, Ren-Yun,Hu, Rong-Hua,Wang, Ji-Wei,Li, Ping,Li, Xiao-Hang
, p. 2971 - 2976 (2013/11/06)
A novel method was developed for Heck reaction of olefins and arylboronic acids using a ligand-free PdCl2 catalyst to afford the coupling products with excellent regio- and stereoselectivity. It is noteworthy that the PdCl2/CuSO4/K2CO3/TBAB/H 2O system can be recovered and used for three cycles directly. Georg Thieme Verlag Stuttgart, New York.
Arylcyclopropanecarboxyl guanidines as novel, potent, and selective inhibitors of the sodium hydrogen exchanger isoform-1
Ahmad,Doweyko,Dugar,Grazier,Ngu,Wu,Yost,Chen,Gougoutas,DiMarco,Lan,Gavin,Chen,Dorso,Serafino,Kirby,Atwal
, p. 3302 - 3310 (2007/10/03)
A novel series of arylcyclopropanecarboxyl guanidines was synthesized and evaluated for activity against the sodium hydrogen exchanger isoform-1 (NHE-1). In biological assays conducted in an AP1 cell line expressing the human NHE-1 isoform, the starting cyclopropane 3a (IC50 = 3.5 μM) shows inhibitory activity comparable to cariporide (IC50 = 3.4 μM). Structure-activity relationships are used to optimize the affinity of various acyl guanidines for NHE-1 by screening the effect of substituents at both aryl and cyclopropyl rings. It is demonstrated that introduction of appropriate hydrophobic groups at the phenyl ring and a gem-dimethyl group at the cyclopropane ring enhances the NHE-1 inhibitory activity by up to 3 orders of magnitude (compound 7f, IC50 = 0.003 μM). In addition, the gem-dimethyl series of analogues seem to display improved oral bioavailability and longer plasma half-life in rats. Furthermore, the lead benzodihydrofuranyl analogue 1 (BMS-284640) shows over 380-fold increased NHE-1 inhibitory activity as well as improved selectivity for NHE-1 over NHE-2 compared to cariporide.
