4.5 Article

Design-driven LO: The discovery of new ultra long acting dibasic β2-adrenoceptor agonists

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 15, 页码 4612-4616

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.05.097

关键词

LABA; beta(2)-Agonist; Adrenoceptor agonist; Asthma; COPD; Inhaled; Duration

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Starting with the molecular scaffold of the DA(2)/beta(2) dual agonist sibenadet ( Viozan (TM)), a number of molecular changes were incorporated, which were designed to increase the potency and selectivity of the target molecule, and improve its pharmacokinetics. Through this process a novel, high potency, full beta(2)-agonist with high selectivity and long duration capable of being dosed once daily has been discovered. (C) 2011 Published by Elsevier Ltd.

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