Dual beta2-adrenoceptor agonists-PDE4 inhibitors for the treatment of asthma and COPD.

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Shan WJ, Huang L, Zhou Q, Jiang HL, Luo ZH, Lai KF, Li XS

Dual beta2-adrenoceptor agonists-PDE4 inhibitors for the treatment of asthma and COPD.

Bioorg Med Chem Lett. 2012 Feb 15;22(4):1523-6. doi: 10.1016/j.bmcl.2012.01.013. Epub 2012 Jan 14.

PubMed ID

22297114 [ View in PubMed

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Abstract

We designed and synthesized a novel class of dual pharmacology bronchodilators targeting both beta(2)-adrenoceptor and PDE4 by applying a multivalent approach. The most potent dual pharmacology molecule, compound 29, possessed good inhibitory activity on PDE4B2 (IC(50)=0.278 muM, which was more potent than phthalazinone, IC(50)=0.520 muM) and possessed excellent relaxant effects on tracheal rings precontracted by histamine (pEC(50)=9.3).

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
(R)-Rolipram	cAMP-specific 3',5'-cyclic phosphodiesterase 4B	IC 50 (nM)	500	N/A	N/A	Details