475046-86-7Relevant academic research and scientific papers
Characterization and structure-activity relationship study of iminodipyridinopyrimidines as novel hepatitis C virus inhibitor
Park, Dong-Sik,Jo, Eunji,Choi, Jihyun,Lee, MyungEun,Kim, Soohyun,Kim, Hee-Young,Nam, Jiyon,Ahn, Sujin,Hwang, Jong Yeon,Windisch, Marc Peter
, p. 65 - 73 (2017/09/20)
Upon high-throughput screening of synthetic small molecule libraries with the infectious hepatitis C virus (HCV) cell culture system, we identified an iminodipyridinopyrimidine (IDPP) scaffold. IDPP did not inhibit HCV replication, but exhibited very potent inhibitory activity on early and late steps of HCV life cycle. Applying an intensive structure-activity relationship (SAR) study, a promising IDPP Lead compound (12c) with excellent potency (EC50 = 10 nM), high safety margin (SI > 2000), and an acceptable stability in human and rat liver microsomes (t1/2 >60 min) was identified. Overall, our results suggest that the IDPP scaffold could be used for the development of novel HCV interventions.
Generation of NH-azomethine imine intermediates through the 1,2-hydrogen shift of hydrazones and their intermolecular cycloaddition reaction with olefinic dipolarophiles
Noguchi, Michihiko,Matsumoto, Satoshi,Shirai, Masashi,Yamamoto, Hidetoshi
, p. 4123 - 4133 (2007/10/03)
The thermal 1,2-hydrogen shift of the hydrazone generates the NH-azomethine imine intermediate in the 4-oxo-4H-pyrido[1,2-a]pyrimidine-3-carbaldehyde system under mild conditions. Therein, the resulting NH-azomethine imine should be stabilized by forming an internal hydrogen bond with the carbonyl oxygen at the 4-position. Its smooth stereoselective intermolecular cycloaddition reaction with olefinic dipolarophiles giving pyrazolidine derivatives is discussed.
