Hybrids consisting of the pharmacophores of salmeterol and roflumilast or phthalazinone: dual beta(2)-adrenoceptor agonists-PDE4 inhibitors for the treatment of COPD.

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Liu A, Huang L, Wang Z, Luo Z, Mao F, Shan W, Xie J, Lai K, Li X

Hybrids consisting of the pharmacophores of salmeterol and roflumilast or phthalazinone: dual beta(2)-adrenoceptor agonists-PDE4 inhibitors for the treatment of COPD.

Bioorg Med Chem Lett. 2013 Mar 1;23(5):1548-52. doi: 10.1016/j.bmcl.2012.11.058. Epub 2012 Nov 29.

PubMed ID

23375225 [ View in PubMed

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Abstract

A novel class of dual pharmacology bronchodilators targeting both beta(2)-adrenoceptor and PDE4 was designed and synthesised by combining the pharmacophores of salmeterol and roflumilast or phthalazinone. All the compounds exhibited better beta(2)-adrenoceptor agonist activities (pEC(50)=8.47-9.20) than the reference compound salmeterol (pEC(50)=8.3) and good inhibitory activity on PDE4B2 (IC(50)=0.235-1.093 muM).

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