1443331-89-2Relevant academic research and scientific papers
Heterocyclic modification of a novel bicyclo[3.1.0]hexane NPY1 receptor antagonist
Luo, Guanglin,Chen, Ling,Hu, Shuanghua,Huang, Yazhong,Mattson, Gail,Iben, Lawrence G.,Russell, John W.,Clarke, Wendy J.,Hogan, John B.,Antal-Zimanyi, Ildiko,Poindexter, Graham S.
, p. 3814 - 3817 (2013/07/27)
A convergent synthesis route for the heterocyclic modification of a novel bicyclo[3.1.0]hexane NPY1 antagonist 2 was developed and the structure activity relationship of these modifications on NPY1 binding is reported. Two heterocyclic analogs 9 and 10 showed comparable Y1 binding potency to 2, but with improved aqueous solubility. Compound 9 demonstrated reduced spontaneous nocturnal food intake in a rat model when dosed ip. Compound 9 was also shown to be orally bioavailable and brain penetrable.
