Literature DB >> 10360744

Substituted piperidines--highly potent renin inhibitors due to induced fit adaptation of the active site.

E Vieira1, A Binggeli, V Breu, D Bur, W Fischli, R Güller, G Hirth, H P Märki, M Müller, C Oefner, M Scalone, H Stadler, M Wilhelm, W Wostl.   

Abstract

The identification, synthesis and activity of a novel class of piperidine renin inhibitors is presented. The most active compounds show activities in the picomolar range and are among the most potent renin inhibitors ever identified.

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Year:  1999        PMID： 10360744     DOI： 10.1016/s0960-894x(99)00195-x

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


  4 in total

1.  Discovery of Novel 2-Carbamoyl Morpholine Derivatives as Highly Potent and Orally Active Direct Renin Inhibitors.

Authors:  Daisuke Iijima; Hiroshi Sugama; Nobumasa Awai; Yoichi Takahashi; Yuko Togashi; Tohru Takebe; Jianshu Xie; Jingkang Shen; Ying Ke; Hidenori Akatsuka; Takayuki Kawaguchi; Kei Takedomi; Akiko Kashima; Masashi Nishio; Yosuke Inui; Hikaru Yoneda; Guangxin Xia; Toru Iijima
Journal:  ACS Med Chem Lett       Date:  2022-08-01       Impact factor: 4.632

2.  Development, evaluation and application of 3D QSAR Pharmacophore model in the discovery of potential human renin inhibitors.

Authors:  Shalini John; Sundarapandian Thangapandian; Mahreen Arooj; Jong Chan Hong; Kwang Dong Kim; Keun Woo Lee
Journal:  BMC Bioinformatics       Date:  2011-12-14       Impact factor: 3.169

Review 3.  In silico pharmacology for drug discovery: applications to targets and beyond.

Authors:  S Ekins; J Mestres; B Testa
Journal:  Br J Pharmacol       Date:  2007-06-04       Impact factor: 8.739

4.  Renin and angiotensinogen expression and functions in growth and apoptosis of human glioblastoma.

Authors:  L Juillerat-Jeanneret; J Celerier; C Chapuis Bernasconi; G Nguyen; W Wostl; H P Maerki; R-C Janzer; P Corvol; J-M Gasc
Journal:  Br J Cancer       Date:  2004-03-08       Impact factor: 7.640
  4 in total

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