Dual metalloprotease inhibitors. I. constrained peptidomimetics of mercaptoacyl dipeptides
A series of benzo-fused lactams were incorporated as conformationally restricted dipeptide mimetics of Ala-Pro in angiotensin converting (ACE)/neutral endopeptidase (NEP) inhibitors.
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2017, Tetrahedron LettersCitation Excerpt :During our drug discovery efforts, (S)-3-amino-benzo[b][1,4]oxazepin-4-one (1) (Fig. 1) was identified as an important pharmacophore as part of a RIP1 kinase inhibitor series.5 This benzoxazepinone template 1 has also been employed to treat other biological targets like β-secretase,6 angiotensin converting enzyme (ACE)7 and inhibitor of apoptosis proteins (IAPs).8 Lead optimization of this series led to identification of GSK2982772 (Fig. 1), a first-in-class RIP1 kinase inhibitor currently undergoing phase 2 clinical trials for the treatment of psoriasis, ulcerative colitis and rheumatoid arthritis.9
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