Potent, orally active corticotropin-releasing factor receptor-1 antagonists containing a tricyclic pyrrolopyridine or pyrazolopyridine core

…, M Haddach, D Marinkovic, JR McCarthy…

Index: Dyck, Brian; Grigoriadis, Dimitri E.; Gross, Raymond S.; Guo, Zhiqiang; Haddach, Mustapha; Marinkovic, Dragan; McCarthy, James R.; Moorjani, Manisha; Regan, Collin F.; Saunders, John; Schwaebe, Michael K.; Szabo, Tomas; Williams, John P.; Zhang, Xiaohu; Bozigian, Haig; Chen, Ta Rung Journal of Medicinal Chemistry, 2005 , vol. 48, # 12 p. 4100 - 4110

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Citation Number: 24

Abstract

Two new classes of tricyclic-based corticotropin-releasing factor (CRF1) receptor-1 antagonists were designed by constraining known 1 H-pyrrolo [2, 3-b] pyridine and 1 H- pyrazolo [3, 4-b] pyridine ligands. Pyrrole-and pyrazole-based molecules 19g and 22a, respectively, were discovered that potently bind the recombinant CRF1 receptor (K i= 3.5, 2.9 nM) and inhibit adrenocorticotropic hormone (ACTH) release from rat pituitary cell ...