197802-86-1Relevant academic research and scientific papers
Purin-8-ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists
Beck, James P.,Arvanitis, Argyrios G.,Curry, Matt A.,Rescinito, Joseph T.,Fitzgerald, Larry W.,Gilligan, Paul J.,Zaczek, Robert,Trainor, George L.
, p. 967 - 972 (2007/10/03)
A series of purin-8-ones was prepared and discovered to have excellent binding affinity to the CRH-R1 receptor. Structure-activity studies focused on amine side-chain optimization, urea substitution and pyridyl isostere incorporation. Thus, the highly potent purin-8-ones show promise as a new class of potential anxiolytics and/or antidepressants.
Synthesis, corticotropin-releasing factor receptor binding affinity, and pharmacokinetic properties of triazolo-, imidazo-, and pyrrolopyrimidines and -pyridines
Chorvat, Robert J.,Bakthavatchalam, Rajagopal,Beck, James P.,Gilligan, Paul J.,Wilde, Richard G.,Cocuzza, Anthony J.,Hobbs, Frank W.,Cheeseman, Robert S.,Curry, Matthew,Rescinito, Joseph P.,Krenitsky, Paul,Chidester, Dennis,Yarem, Jerry A.,Klaczkiewicz, John D.,Hodge, C. Nicholas,Aldrich, Paul E.,Wasserman, Zelda R.,Fernandez, Christine H.,Zaczek, Robert,Fitzgerald, Lawrence W.,Huang, Shiew-Mei,Shen, Helen L.,Wong, Y. Nancy,Chien, Ben M.,Quon, Check Y.,Arvanitis, Argyrios
, p. 833 - 848 (2007/10/03)
The synthesis and CRF receptor binding affinities of several new series of N-aryltriazolo- and -imidazopyrimidines and -pyridines are described. These cyclized systems were prepared from appropriately substituted diaminopyrimidines or -pyridines by nitrous acid, orthoester, or acyl halide treatment. Variations of amino (ether) pendants and aromatic substituents have defined the structure-activity relationships of these series and resulted in the identification of a variety of high-affinity agents (K(i)'s 1 has been selected for further pharmacological studies that will be reported in due course.
