Discovery of a Novel Series of Imipridone Compounds as Homo sapiens Caseinolytic Protease P Agonists with Potent Antitumor Activities In Vitro and In Vivo
Presumed pharmacophoric groups of melanocortin peptides (naphthalene, amino or guanidine, and indole moieties) were combined in mimetics molecules looking for their favorable location for activity at melanocortin (MC) receptors. Twenty-two compounds were prepared and tested. The best of these displayed micromolar affinities for the MC receptors. (C) 2002 Elsevier Science Ltd. All rights reserved.
Lukasiewicz; Eckstein, Bulletin de l'Academie Polonaise des Sciences, Serie des Sciences Chimiques, 1959, vol. 7, p. 797,799
作者:Lukasiewicz、Eckstein
DOI:——
日期:——
US6512000B1
申请人:——
公开号:US6512000B1
公开(公告)日:2003-01-28
[EN] NOVEL AROMATIC AMINES AND AMIDES ACTING ON THE MELANOCORTIN RECEPTORS<br/>[FR] NOUVEAUX AMINES ET AMIDES AROMATIQUES AGISSANT SUR LES RECEPTEURS DE LA MELANOCORTINE
申请人:MELACURE THERAPEUTICS AB
公开号:WO2001055107A2
公开(公告)日:2001-08-02
The present invention relates to novel aromatic amines and amides of general formula (I) and to the use of these amines and amides for the treatment of obesity, anorexia, inflammation, mental disorders and other diseases associated with the melanocortin receptors or related systems, e.g. the melanocyte stimulating hormones.