Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10595537 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
Abstract
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.
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Guanglin Luo, Ling Chen, Shuanghua Hu, Yazhong Huang, Gail Mattson, Lawrence G. Iben, John W. Russell, Wendy J. Clarke, John B. Hogan, Ildiko Antal-Zimanyi, Graham S. Poindexter,