From libraries to candidate: the discovery of new ultra long-acting dibasic beta(2)-adrenoceptor agonists.

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Alcaraz L, Bailey A, Cadogan E, Connolly S, Jewell R, Jordan S, Kindon N, Lister A, Lawson M, Mullen A, Dainty I, Nicholls D, Paine S, Pairaudeau G, Stocks MJ, Thorne P, Young A

From libraries to candidate: the discovery of new ultra long-acting dibasic beta(2)-adrenoceptor agonists.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):689-95. doi: 10.1016/j.bmcl.2011.10.049. Epub 2011 Oct 20.

PubMed ID

22079756 [ View in PubMed

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Abstract

Libraries of dibasic compounds designed around the molecular scaffold of the DA(2)/beta(2) dual agonist sibenadet (Viozan) have yielded a number of promising starting points that have been further optimised into novel potent and selective target molecules with required pharmacokinetic properties. From a shortlist, 31 was discovered as a novel, high potency, and highly efficacious beta(2)-agonist with high selectivity and a duration of action commensurable with once daily dosing.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Salmeterol	Beta-1 adrenergic receptor	IC 50 (nM)	501.19	N/A	N/A	Details