433330-64-4Relevant academic research and scientific papers
Discovery of a new series of potent prostacyclin receptor agonists with in vivo activity in rat
Tran, Thuy-Anh,Shin, Young-Jun,Kramer, Bryan,Choi, Juyi,Zou, Ning,Vallar, Pureza,Martens, Peter,Douglas Boatman,Adams, John W.,Ramirez, Juan,Shi, Yunqing,Morgan, Michael,Unett, David J.,Chang, Steve,Shu, Hsin-Hui,Tung, Shiu-Feng,Semple, Graeme
supporting information, p. 1030 - 1035 (2015/02/19)
The design and synthesis of two closely related series of prostacyclin receptor agonist compounds that showed excellent human IP receptor potency and efficacy is described. Compounds from this series showed in vivo activity after SC dosing in the monocrotaline model of PAH in rat.
Pyridazines. Part 35: Traceless solid phase synthesis of 4,5- and 5,6-diaryl-3(2H)-pyridazinones
Sotelo, Eddy,Ravi?a, Enrique
, p. 1113 - 1116 (2007/10/03)
A new method for the traceless solid phase synthesis of 3(2H)-pyridazinones has been developed employing dihydropyran-functionalized resin. The procedure has permitted the preparation of several diarylpyridazinones through a Suzuki cross-coupling reaction and cleavage conditions that promoted a retro-ene fragmentation.
Mono- and di-substituted 5,6-diphenyl-3-alkylaminopyridazines active as ACAT inhibitors
Toma, Lucio,Giovannoni, Maria Paola,Dal Piaz, Vittorio,Kwon, Byoung-Mog,Kim, Young-Kook,Gelain, Arianna,Barlocco, Daniela
, p. 39 - 46 (2007/10/03)
A series of mono- or di-para-substituted 5,6-diphenyl-3-alkylaminopyridazines were synthesized and their inhibitory activity against acyl-CoA:cholesterol acyltransferase (ACAT) was tested on the enzyme prepared from rat liver microsomes. The compound which combines a chlorine atom on the 6-phenyl ring and a n-hexylamino chain showed a significant enhancement of activity with respect to the unsubstituted derivative. Attempts to correlate the activity of the compounds to their structural features, also through theoretical calculations, are reported.
Pyridazines. Part 26: Efficient and regioselective Pd-catalysed arylation of 4-bromo-6-chloro-3-phenylpyridazine
Sotelo, Eddy,Ravin?a, Enrique
, p. 223 - 226 (2007/10/03)
The regioselective arylation at position 4 of 4-bromo-6-chloro-3-phenylpyridazine has been performed using a Suzuki cross-coupling reaction. This route allows access to a wide-ranging series of pharmacologically useful pyridazine derivatives and confirms
