Literature DB >> 25532755

Design and synthesis of new tricyclic indoles as potent modulators of the S1P1 receptor.

Daniel J Buzard1, Thomas O Schrader1, Xiuwen Zhu1, Juerg Lehmann1, Ben Johnson1, Michelle Kasem1, Sun Hee Kim1, Andrew Kawasaki1, Luis Lopez1, Jeanne Moody1, Sangdon Han1, Yinghong Gao1, Jeff Edwards1, Jeremy Barden1, Jayant Thatte1, Joel Gatlin1, Robert M Jones1.   

Abstract

Modulators of S1P1 have proven utility for the treatment of autoimmune disease and efforts to identify new agents with improved safety and pharmacokinetic parameters are ongoing. Several new S1P1 chemotypes were designed and optimized for potency and oral bioavailability. These new agents are characterized by a 'tricyclic fused indole array' and are highly potent agonists of the S1P1 receptor.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Gilenya®; S1P(1); Sphingosine-1-phosphate

Mesh:

Substances:

Year:  2014        PMID: 25532755     DOI: 10.1016/j.bmcl.2014.11.089

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


  3 in total

1.  A simple and facile synthesis of tricyclic-fused pyrimido[4,5-b]indol-2-amines.

Authors:  Wentao Gao; Dongfang Wang; Yang Li
Journal:  Mol Divers       Date:  2017-06-19       Impact factor: 2.943

2.  Alignment independent 3D-QSAR studies and molecular dynamics simulations for the identification of potent and selective S1P1 receptor agonists.

Authors:  Ali Akbar Alizadeh; Behzad Jafari; Siavoush Dastmalchi
Journal:  J Mol Graph Model       Date:  2019-09-29       Impact factor: 2.518

3.  Regiodivergent synthesis of pyrazino-indolines vs. triazocines via α-imino carbenes addition to imidazolidines.

Authors:  Alejandro Guarnieri-Ibáñez; Adiran de Aguirre; Céline Besnard; Amalia I Poblador-Bahamonde; Jérôme Lacour
Journal:  Chem Sci       Date:  2020-11-23       Impact factor: 9.825

  3 in total

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