A novel class of dual pharmacology bronchodilators targeting both β2-adrenoceptor and PDE4 was designed and synthesised by combining the pharmacophores of salmeterol and roflumilast or phthalazinone. All the compounds exhibited better β2-adrenoceptor agonist activities (pEC50 = 8.47–9.20) than the reference compound salmeterol (pEC50 = 8.3) and good inhibitory activity on PDE4B2 (IC50 = 0.235–1.093 μM).A novel class of dual pharmacology bronchodilators targeting both β2-adrenoceptor and PDE4 was designed and synthesised by combining the pharmacophores of salmeterol and roflumilast or phthalazinone. All the compounds exhibited better β2-adrenoceptor agonist activities (pEC50 = 8.47–9.20) than the reference compound salmeterol (pEC50 = 8.3) and good inhibitory activities on PDE4B2 (IC50 = 0.235–1.093 μM).

We designed and synthesized a novel class of dual pharmacology bronchodilators targeting both β2-adrenoceptor and PDE4 by applying a multivalent approach. The most potent dual pharmacology molecule, compound 29, possessed good inhibitory activity on PDE4B2 (IC50 = 0.278 μM, which was more potent than phthalazinone, IC50 = 0.520 μM) and possessed excellent relaxant effects on tracheal rings precontracted by histamine (pEC50 = 9.3).We designed and synthesized a novel class of dual pharmacology bronchodilators targeting both β2-adrenoceptor and PDE4 by applying a multivalent approach. The most potent dual pharmacology molecule, compound 29, possessed good inhibitory activity on PDE4B2 (IC50 = 0.278 μM, which was more potent than phthalazinone, IC50 = 0.520 μM) and possessed excellent relaxant effects on tracheal rings precontracted by histamine (pEC50 = 9.3).

A series of novel indanone derivatives was designed, synthesised and evaluated as potential agents for Alzheimer’s disease. Among them, compound 6a, with a piperidine group linked to indone by a two-carbon spacer, exhibited the most potent inhibitor activity, with an IC50 of 0.0018 μM for AChE; the inhibitory activity of this compound was 14-fold more potent than that of donepezil. Furthermore, these compounds also exhibited good metal-chelating ability.A series of novel indanone derivatives was designed, synthesised and evaluated as potential agents for Alzheimer’s disease. Among them, compound 6a, with a piperidine group linked to indone by a two-carbon spacer, exhibited the most potent inhibitor activity, with an IC50 of 0.0018 μM for AChE; the inhibitory activity of this compound was 14-fold more potent than that of donepezil. Furthermore, these compounds also exhibited good metal-chelating ability.