Literature DB >> 10360745

Piperidine-renin inhibitors compounds with improved physicochemical properties.

R Güller1, A Binggeli, V Breu, D Bur, W Fischli, G Hirth, C Jenny, M Kansy, F Montavon, M Müller, C Oefner, H Stadler, E Vieira, M Wilhelm, W Wostl, H P Märki.   

Abstract

Piperidine renin inhibitors with heterocyclic core modifications or hydrophilic attachments show improved physical properties (lower lipophilicity, improved solubility). Tetrahydroquinoline derivative rac-30 with a molecular weight of 517 and a log D(pH 7.4) of 1.9 displays potent and long lasting blood pressure lowering effects after oral administration to sodium depleted conscious marmosets.

Entities:  

Mesh:

Substances:

Year:  1999        PMID: 10360745     DOI: 10.1016/s0960-894x(99)00196-1

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


  4 in total

Review 1.  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

2.  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

Review 3.  Recent syntheses of 1,2,3,4-tetrahydroquinolines, 2,3-dihydro-4(1H)-quinolinones and 4(1H)-quinolinones using domino reactions.

Authors:  Baskar Nammalwar; Richard A Bunce
Journal:  Molecules       Date:  2013-12-24       Impact factor: 4.411

Review 4.  Decades-old renin inhibitors are still struggling to find a niche in antihypertensive therapy. A fleeting look at the old and the promising new molecules.

Authors:  Krishnappa Ramya; Ramalingam Suresh; Honnavalli Yogish Kumar; B R Prashantha Kumar; N B Sridhara Murthy
Journal:  Bioorg Med Chem       Date:  2020-03-28       Impact factor: 3.641

  4 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.