Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1364981 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
SAR exploration of the central diamine, benzyl, and terminal aminoalkoxy regions of the N-cyclic azaalkyl benzamide series led to the identification of very potent human urotensin-II receptor antagonists such as 1a with a Ki of 4 nM. The synthesis and structure–activity relationships (SAR) of N-cyclic azaalkyl benzamides are described.
Graphical abstractSAR exploration of the central diamine, benzyl, and terminal aminoalkoxy regions of the N-cyclic azaalkyl benzamide series led to the identification of very potent human urotensin-II receptor antagonists such as 1a with a Ki of 4 nM. The synthesis and structure–activity relationships (SAR) of N-cyclic azaalkyl benzamides are described.Figure optionsDownload full-size imageDownload as PowerPoint slide