357980-82-6

Upstream product

• 439660-78-3 2-[1-(3,4-dimethoxy-phenyl)-methanoyl]-cyclohexanecarboxylic acid 
• 85-42-7 1,2-Cyclohexanedicarboxylic acid-anhydride 
• 91-16-7 1,2-dimethoxybenzene 
• 439660-85-2 6-(3,4-dimethoxy-benzoyl)-cyclohex-3-enecarboxylic acid 
• 935-79-5 cis-1,2,3,6-tetrahydrophthalic anhydride 
• 89980-69-8 3,4-dimethoxyphenylmagnesium bromide 

Downstream Products

• 1116690-31-3 2-(2-bromopentyl)-4-(3,4-dimethoxyphenyl)-4a,5,6,7,8,8a-hexahydrophthalazin-1(2H)-one 
• 878663-15-1 C₃₇H₄₂F₃N₃O₄ 
• 878663-14-0 C₃₇H₄₂F₃N₃O₄ 

Relevant academic research and scientific papers

Design, synthesis and evaluation of dual pharmacology β2- adrenoceptor agonists and PDE4 inhibitors

A novel series of formoterol-phthalazinone hybrids were synthesised and evaluated as dual pharmacology β2-adrenoceptor agonists and PDE4 inhibitors. Most of the hybrids displayed high β2-adrenoceptor agonist and moderate PDE4 inhibitory activities. The most potent compound, (R,R)-11c, exhibited agonist (EC50 = 1.05 nM, pEC50 = 9.0) and potent PDE4B2 inhibitory activities (IC50 = 0.092 μM).

Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression

Multi-target compounds where more than one functional activity is incorporated into the same molecule may have advantages in treating disease states. Selective serotonin re-uptake inhibitors (SSRIs)a (i.e., (R)- and (S)-norfluoxetine) were chemically linked to a PDE4 inhibitor via a five carbon bridge. The new dual PDE4 inhibitor/SSRIs (i.e., (R)-8 and (S)-8) showed moderately potent but highly selective serotonin re-uptake inhibition (IC50 values of 173 and 42 nM, respectively) in vitro. The dual PDE4 inhibitor/SSRIs (R)-8 and (S)-8 also inhibited PDE4D2 (i.e., Ki values of 106 and 253 nM, respectively). Due to the synergistic functional activity, PDE4 inhibitor/SSRIs may be effective in treating diseases such as depression.