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Discovery of pyrrolopyridazines as novel DGAT1 inhibitors

…, R Choi, T Inaba, S Jackson, S Sagawa, B Shan…

文献索引:Fox, Brian M.; Iio, Kiyosei; Li, Kexue; Choi, Rebeka; Inaba, Takashi; Jackson, Simon; Sagawa, Shoichi; Shan, Bei; Tanaka, Masahiro; Yoshida, Atsuhito; Kayser, Frank Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 20 p. 6030 - 6033

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被引用次数: 24

摘要

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 ...