1421637-26-4Relevant 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 (2019/01/04)
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.
A short and straightforward approach towards 6-amino and 6-aminoalkyl thiazolo[4,5-c]pyridazines
Stella, Alessandro,De Jonghe, Steven,Segers, Kenneth,Herdewijn, Piet
, p. 830 - 833 (2013/02/25)
A facile and efficient synthesis of 6-amino and 6-aminoalkyl thiazolo[4,5-c]pyridazines is reported. The key step for the construction of this novel bicyclic scaffold was the reaction between 3-amino-4-bromopyridazine derivatives and alkylisothiocyanates.