Literature DB >> 21944381

Steroidal C-21 mercapto derivatives as dissociated steroids: discovery of an inhaled dissociated steroid.

Purakkattle Biju1, Kevin McCormick, Robert Aslanian, Michael Berlin, Daniel Solomon, Richard Chapman, Robbie McLeod, Daniel Prelusky, Stephen Eckel, George Kelly, Michelle Natiello, Aileen House, Xiomara Fernandez, Rema Bitar, Jonathan Phillips, John Anthes.   

Abstract

A series of C-21 mercapto derivatives of hydrocortisone have been synthesized and evaluated in cell based transrepression and transactivation assays. The benzothiazole derivative, compound 6 not only showed a dissociated profile in vitro functional assays but also a pharmacological profile in a Brown-Norway rat therapeutic index model of asthma that dissociated side effects (thymolysis) while maintaining efficacy against pulmonary inflammation and lung function.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21944381     DOI: 10.1016/j.bmcl.2011.08.108

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


  5 in total

1.  Thiobenzothiazole-modified Hydrocortisones Display Anti-inflammatory Activity with Reduced Impact on Islet β-Cell Function.

Authors:  Susan J Burke; Amanda L May; Robert C Noland; Danhong Lu; Marcela Brissova; Alvin C Powers; Elizabeth M Sherrill; Michael D Karlstad; Shawn R Campagna; Jacqueline M Stephens; J Jason Collier
Journal:  J Biol Chem       Date:  2015-04-07       Impact factor: 5.157

2.  Btk Inhibitor RN983 Delivered by Dry Powder Nose-only Aerosol Inhalation Inhibits Bronchoconstriction and Pulmonary Inflammation in the Ovalbumin Allergic Mouse Model of Asthma.

Authors:  Jonathan E Phillips; Lorena Renteria; Lisa Burns; Paul Harris; Ruoqi Peng; Carla M T Bauer; Dramane Laine; Christopher S Stevenson
Journal:  J Aerosol Med Pulm Drug Deliv       Date:  2016-04-25       Impact factor: 2.849

3.  Dry Powder and Nebulized Aerosol Inhalation of Pharmaceuticals Delivered to Mice Using a Nose-only Exposure System.

Authors:  Jonathan E Phillips; Xuxia Zhang; James A Johnston
Journal:  J Vis Exp       Date:  2017-04-06       Impact factor: 1.355

4.  Synthesis of budesonide conjugates and their anti-inflammatory effects: a preliminary study.

Authors:  Yan Yan; Pengchong Wang; Ruiying Li; Ying Sun; Rui Zhang; Chuanchuan Huo; Jianfeng Xing; Yalin Dong
Journal:  Drug Des Devel Ther       Date:  2019-02-19       Impact factor: 4.162

5.  Biological activities of 2-mercaptobenzothiazole derivatives: a review.

Authors:  Mohammed Afzal Azam; Bhojraj Suresh
Journal:  Sci Pharm       Date:  2012-06-18
  5 in total

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