Literature DB >> 12668017

Phenylbutyrates as potent, orally bioavailable vitronectin receptor (integrin alphavbeta3) antagonists.

William H Miller1, Peter J Manley, Russell D Cousins, Karl F Erhard, Dirk A Heerding, Chet Kwon, Stephen T Ross, James M Samanen, Dennis T Takata, Irene N Uzinskas, Catherine C K Yuan, R Curtis Haltiwanger, Catherine J Gress, Michael W Lark, Shing Mei Hwang, Ian E James, David J Rieman, Robert N Willette, Tian Li Yue, Leonard M Azzarano, Kevin L Salyers, Brian R Smith, Keith W Ward, Kyung O Johanson, William F Huffman.   

Abstract

In our continuing efforts to identify small molecule vitronectin receptor antagonists, we have discovered a series of phenylbutyrate derivatives, exemplified by 16, which have good potency and excellent oral bioavailability (approximately 100% in rats). This new series is derived conceptually from opening of the seven-membered ring of SB-265123.

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Year:  2003        PMID: 12668017     DOI: 10.1016/s0960-894x(03)00102-1

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


  4 in total

1.  Methylene C(sp3)-H Arylation of Aliphatic Ketones Using a Transient Directing Group.

Authors:  Kai Hong; Hojoon Park; Jin-Quan Yu
Journal:  ACS Catal       Date:  2017-09-13       Impact factor: 13.084

2.  Palladium-Catalyzed Enantioselective Redox-Relay Heck Arylation of 1,1-Disubstituted Homoallylic Alcohols.

Authors:  Zhi-Min Chen; Margaret J Hilton; Matthew S Sigman
Journal:  J Am Chem Soc       Date:  2016-09-01       Impact factor: 15.419

3.  Facile synthesis of 7-alkyl-1,2,3,4-tetrahydro-1,8-naphthyridines as arginine mimetics using a Horner-Wadsworth-Emmons-based approach.

Authors:  Rhys A Lippa; John A Murphy; Tim N Barrett
Journal:  Beilstein J Org Chem       Date:  2020-07-08       Impact factor: 2.883

4.  Three-component vicinal-diarylation of alkenes via direct transmetalation of arylboronic acids.

Authors:  Yun Zhang; Gong Chen; Dongbing Zhao
Journal:  Chem Sci       Date:  2019-07-03       Impact factor: 9.825

  4 in total

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