105538-07-6Relevant articles and documents
Design and Evaluation of Heterobivalent PAR1-PAR2 Ligands as Antagonists of Calcium Mobilization
Majewski, Mark W.,Gandhi, Disha M.,Rosas, Ricardo,Kodali, Revathi,Arnold, Leggy A.,Dockendorff, Chris
, p. 121 - 126 (2019)
A novel class of bivalent ligands targeting putative protease-activated receptor (PAR) heteromers has been prepared based upon reported antagonists for the subtypes PAR1 and PAR2. Modified versions of the PAR1 antagonist RWJ-58259 containing alkyne adapters were connected via cycloaddition reactions to azide-capped polyethylene glycol (PEG) spacers attached to imidazopyridazine-based PAR2 antagonists. Initial studies of the PAR1-PAR2 antagonists indicated that they inhibited G alpha q-mediated calcium mobilization in endothelial and cancer cells driven by both PAR1 and PAR2 agonists. Compounds of this novel class hold promise for the prevention of restenosis, cancer cell metastasis, and other proliferative disorders.
Mild and direct access to 7-substituted-4-trifluoromethylpyrimido[1,2- b ]pyridazin-2-one systems
Petrignet, Julien,Thiery, Emilie,Silpa, Laurence,Abarbri, Mohamed
, p. 947 - 954 (2014/04/03)
New and efficient methods for the synthesis of 7-substituted-4- trifluoromethylpyrimido[1,2-b]pyridazin-2-one derivatives using either two-step Suzuki/heterocyclization, or two-step heterocyclization/substitution sequences are developed. A variety of substituted products are obtained in good to excellent yields from 3-amino-6-chloropyridazine and ethyl 4,4,4-trifluorobut-2- ynoate. Georg Thieme Verlag Stuttgart · New York.
Microwave-enhanced synthesis of 2,3,6-trisubstituted pyridazines: Application to four-step synthesis of gabazine (SR-95531)
Gavande, Navnath,Johnston, Graham A. R.,Hanrahan, Jane R.,Chebib, Mary
supporting information; experimental part, p. 4131 - 4136 (2010/10/18)
Microwave-enhanced, highly efficient protocols for the synthesis of synthetically and biologically important 2,3,6-trisubstituted pyridazine architectures have been developed by sequential amination/Suzuki coupling/alkylation reactions. This powerful strategy is an economical and highly chemoselective protocol for the synthesis of diversified pyridazines. The total synthesis of gabazine (SR-95531) has been achieved using a versatile strategy in four steps and 73% overall yield.