Beattie, David, Bradley, Michelle, Brearley, Andrew, Charlton, Steven J, Cuenoud, Bernard M, Fairhurst, Robin A, Gedeck, Peter, Gosling, Martin, Janus, Diana, Jones, Darryl, Lewis, Christine, McCarthy, Clive, Oakman, Helen, Stringer, Rowan, Taylor, Roger J and Tuffnell, Andrew (2010) A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of β2-adrenoceptor agonists as inhaled long-acting bronchodilators. Bioorganic and Medicinal Chemistry Letters, 20 (17). pp. 5302-5307. ISSN 0960-894X

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Abstract

The chiral synthesis of a 4-hydroxybenzothiazolone based series of β2-adrenoceptor agonists is described. Using this methodology a library of N-substituted analogues were prepared for the rapid identification of leads with the potential to be fast onset and long-acting inhaled bronchodilators with improved therapeutic margins. The design of the library to achieve the targeted profile was based upon lipophilicity and metabolism based hypotheses. This approach identified β-phenethyl, α-substituted cyclopentyl and monoterpene N-substituents to be of particular interest for further evaluation, as exemplified by structures 19, 29 and 33, respectively. © 2010 Elsevier Ltd. All rights reserved.

Item Type:	Article
Schools and Departments:	School of Life Sciences > Chemistry
Subjects:	Q Science > QD Chemistry
Depositing User:	Tom Gittoes
Date Deposited:	27 Jan 2015 09:33
Last Modified:	27 Jan 2015 09:33
URI:	http://srodev.sussex.ac.uk/id/eprint/52456

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