Literature DB >> 26372652

Pentafluorosulfanyl-containing flufenamic acid analogs: Syntheses, properties and biological activities.

Christine M M Hendriks1, Trevor M Penning2, Tianzhu Zang2, Dominik Wiemuth3, Stefan Gründer3, Italo A Sanhueza1, Franziska Schoenebeck1, Carsten Bolm1.   

Abstract

Pentafluorosulfanyl-containing analogs of flufenamic acid have been synthesized in high yields. Computationally, pKa, LogP and LogD values have been determined. Initial bioactivity studies reveal effects as ion channel modulators and inhibitory activities on aldo-keto reductase 1C3 (AKR1C3) as well as COX-1 and COX-2.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  AKR1C3 inhibitor; Bile acid-sensitive ion channel; Computational conformational analyses; Flufenamic acid; Ion channel modulator; Pentafluorosulfanyl group

Mesh：

Substances：

Year:  2015        PMID： 26372652      PMCID： PMC4599580          DOI： 10.1016/j.bmcl.2015.09.012

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


  25 in total

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7.  Synthesis of insecticidal fluorinated anthranilic diamides.

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Review 8.  Fluorine in pharmaceutical industry: fluorine-containing drugs introduced to the market in the last decade (2001-2011).

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Journal:  Chem Rev       Date:  2013-12-03       Impact factor: 60.622

9.  Crystal structures of prostaglandin D(2) 11-ketoreductase (AKR1C3) in complex with the nonsteroidal anti-inflammatory drugs flufenamic acid and indomethacin.

Authors:  Andrew L Lovering; Jon P Ride; Christopher M Bunce; Julian C Desmond; Stephen M Cummings; Scott A White
Journal:  Cancer Res       Date:  2004-03-01       Impact factor: 12.701

10.  Synthesis and biological evaluation of the first pentafluorosulfanyl analogs of mefloquine.

Authors:  Peter Wipf; Tingting Mo; Steven J Geib; Diana Caridha; Geoffrey S Dow; Lucia Gerena; Norma Roncal; Erin E Milner
Journal:  Org Biomol Chem       Date:  2009-08-07       Impact factor: 3.876
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  1 in total

1.  Structure-Activity Study of Bioisosteric Trifluoromethyl and Pentafluorosulfanyl Indole Inhibitors of the AAA ATPase p97.

Authors:  Celeste Alverez; Michelle R Arkin; Stacie L Bulfer; Raffaele Colombo; Marina Kovaliov; Matthew G LaPorte; Chaemin Lim; Mary Liang; William J Moore; R Jeffrey Neitz; Yongzhao Yan; Zhizhou Yue; Donna M Huryn; Peter Wipf
Journal:  ACS Med Chem Lett       Date:  2015-10-23       Impact factor: 4.345
  1 in total

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