Document Report Card

ID: ALA1135413

Journal: J Med Chem

Title: Arylamidrazones as novel corticotropin releasing factor receptor antagonists.

Authors: Wilson DM, Termin AP, Mao L, Ramirez-Weinhouse MM, Molteni V, Grootenhuis PD, Miller K, Keim S, Wise G.

Abstract: The arylamidrazones have been found to be potent corticotropin releasing factor (CRF) receptor antagonists structurally distinct from previously reported CRF1 antagonists. Attempts to modify the arylamidrazone core suggested an important role for the anilino NH moiety. The right-hand-side 2-nitro feature in lead 1 could be replaced with substituents methyl, chloro, cyano, or trifluoromethyl with a 4- to 10-fold reduction in receptor binding. With appropriate left-hand-side modifications, this potency loss could be recovered.

CiteXplore: 12014949

DOI: 10.1021/jm025512y