Literature DB >> 17502143

Design and synthesis of benzoazepinone-derived cyclic malonamides and aminoamides as potent gamma-secretase inhibitors.

Michael G Yang1, Jian-Liang Shi, Dilip P Modi, Jennifer Wells, Brian M Cochran, Mark A Wolf, Lorin A Thompson, Mercy M Ramanjulu, Arthur H Roach, Robert Zaczek, David W Robertson, Ruth R Wexler, Richard E Olson.   

Abstract

We report the synthesis of benzoazepine-derived cyclic malonamides (2) and aminoamides (3) as gamma-secretase inhibitors for the potential treatment of Alzheimer's disease. The in vitro structure-activity relationships of 2 and 3 along with dog pharmacokinetic results are described.

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Year:  2007        PMID： 17502143     DOI： 10.1016/j.bmcl.2007.04.102

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  3 in total

1.  The amide linker in nonpeptide neurotensin receptor ligands plays a key role in calcium signaling at the neurotensin receptor type 2.

Authors:  James B Thomas; Angela M Giddings; Srinivas Olepu; Robert W Wiethe; Keith R Warner; Philippe Sarret; Jean-Michel Longpre; Scott P Runyon; Brian P Gilmour
Journal:  Bioorg Med Chem Lett       Date:  2015-04-03       Impact factor: 2.823

Review 2.  Tumor microenvironment pathways: Cross regulation in breast cancer metastasis.

Authors:  Rama Rao Malla; P Kiran
Journal:  Genes Dis       Date:  2020-12-01

3.  Metal-bio functionalized bismuthmagnetite [Fe3-x Bi x O4/SiO2@l-ArgEt3 +I-/Zn(ii)]: a novel bionanocomposite for the synthesis of 1,2,4,5-tetrahydro-2,4-dioxobenzo[b][1,4]diazepine malononitriles and malonamides at room temperature and under sonication.

Authors:  Fatemeh Molaei Yielzoleh; Kobra Nikoofar
Journal:  RSC Adv       Date:  2022-04-01       Impact factor: 3.361
  3 in total

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