Design driven HtL: The discovery and synthesis of new high efficacy β 2 -agonists

Bioorganic & Medicinal Chemistry Letters
2011.0

Abstract

The design and synthesis of a new series of high efficacy β(2)-agonists devoid of the key benzylic alcohol present in previously described highly efficacious β(2)-agonists is reported. A hypothesis for the unprecedented level of efficacy is proposed based on considerations of β(2)-adrenoceptor crystal structure, other biophysical data and modeling studies.

Knowledge Graph

Similar Paper

Design driven HtL: The discovery and synthesis of new high efficacy β 2 -agonists
Bioorganic & Medicinal Chemistry Letters 2011.0
A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of β2-adrenoceptor agonists as inhaled long-acting bronchodilators
Bioorganic & Medicinal Chemistry Letters 2010.0
Design, synthesis and biological evaluation of 5-(2-amino-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one derivatives as potent β2-adrenoceptor agonists
Bioorganic & Medicinal Chemistry 2019.0
Synthesis and Structure−Activity Relationships of Long-acting β<sub>2</sub>Adrenergic Receptor Agonists Incorporating Arylsulfonamide Groups
Journal of Medicinal Chemistry 2009.0
Insights on the role of boron containing moieties in the design of new potent and efficient agonists targeting the β2 adrenoceptor
Bioorganic &amp; Medicinal Chemistry Letters 2015.0
Discovery of highly potent and selective biphenylacylsulfonamide-based β3-adrenergic receptor agonists and molecular modeling based on the solved X-ray structure of the β2-adrenergic receptor: Part 6
Bioorganic &amp; Medicinal Chemistry Letters 2009.0
Synthesis and Structure−Activity Relationships of Long-acting β<sub>2</sub>Adrenergic Receptor Agonists Incorporating Metabolic Inactivation: An Antedrug Approach
Journal of Medicinal Chemistry 2010.0
Discovery of a Highly Selective β<sub>2</sub>-Adrenoceptor Agonist with a 2-Amino-2-phenylethanol Scaffold as an Oral Antiasthmatic Agent
Journal of Medicinal Chemistry 2022.0
Synthesis, pharmacological and in silico evaluation of 1-(4-di-hydroxy-3,5-dioxa-4-borabicyclo[4.4.0]deca-7,9,11-trien-9-yl)-2-(tert-butylamino)ethanol, a compound designed to act as a β2 adrenoceptor agonist
European Journal of Medicinal Chemistry 2009.0
Synthesis and biological evaluation of β2-adrenoceptor agonists bearing the 2-amino-2-phenylethanol scaffold
European Journal of Medicinal Chemistry 2018.0