54099-72-8Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of 1,2,3,7-tetrahydro-6H- purin-6-one and 3,7-dihydro-1H-purine-2,6-dione derivatives as corticotropin-releasing factor1 receptor antagonists
Hartz, Richard A.,Nanda, Kausik K.,Ingalls, Charles L.,Ahuja, Vijay T.,Molski, Thaddeus F.,Zhang, Ge,Wong, Harvey,Peng, Yong,Kelley, Michelle,Lodge, Nicholas J.,Zaczek, Robert,Gilligan, Paul J.,Trainor, George L.
, p. 4741 - 4754 (2007/10/03)
A growing body of evidence suggests that CRF1 receptor antagonism offers considerable therapeutic potential in the treatment of diseases resulting from elevated levels of CRF, such as anxiety and depression. A series of novel 1,2,3,7-tetrahydro-6H-purin-6-one and 3,7-dihydro-1H-purine-2, 6-dione derivatives was synthesized and evaluated as corticotropin releasing factor-1 (CRF1) receptor antagonists. Compounds within this series, represented by compound 12d (IC50 = 5.4 nM), were found to be highly potent CRF1 receptor antagonists. In addition, compounds 12d and 12j were determined to be selective CRF1 antagonists. The synthesis, structure-activity relationships and pharmacokinetic properties of compounds within this series is presented.
