844875-95-2Relevant articles and documents
Discovery of pyrrolopyridazines as novel DGAT1 inhibitors
Fox, Brian M.,Iio, Kiyosei,Li, Kexue,Choi, Rebeka,Inaba, Takashi,Jackson, Simon,Sagawa, Shoichi,Shan, Bei,Tanaka, Masahiro,Yoshida, Atsuhito,Kayser, Frank
scheme or table, p. 6030 - 6033 (2010/11/05)
A new structural class of DGAT1 inhibitors was discovered and the structure-activity relationship was explored. The pyrrolotriazine core of the original lead molecule was changed to a pyrrolopyridazine core providing an increase in potency. Further exploration resulted in optimization of the propyl group at C7 and the discovery that the ester at C6 could be replaced by five-membered heterocyclic rings. The analogs prepared have DGAT1 IC 50 values ranging from >10 μM to 48 nM.
Synthesis and analgesic activity of some 4,6-disubstituted-3(2H)- pyridazinone derivatives
Suekueroglu, Murat,Kuepeli, Esra,Banoglu, Erden,Uenlue, Serdar,Yesilada, Erdem,Sahin, Mustafa Fethi
, p. 337 - 345 (2007/10/03)
A series of 6-morpholino-4-aryl-3(2H)-pyridazinone alkanoic acids, their ester and amide derivatives were prepared and tested for their in vivo analgesic activity by using the p-benzoquinone-induced writhing test. The analgesic activity of the compounds 6