1224939-47-2

Upstream product

• 109-70-6 1.3-chlorobromopropane 
• 6843-49-8 5-methyl-5-phenylimidazolidin-2,4-dione 

Downstream Products

• 1224939-51-8 5-methyl-5-phenyl-3-[3-(4-phenylpiperazin-1-yl)propyl]-imidazolidine-2,4-dione 
• 1224939-52-9 5-methyl-5-phenyl-3-{3-[4-(2-methoxyphenyl)piperazin-1-yl]propyl}-imidazolidine-2,4-dione 
• 1224939-53-0 5-methyl-5-phenyl-3-{3-[4-(3-chlorophenyl)piperazin-1-yl]-propyl}-imidazolidine-2,4-dione 

Relevant academic research and scientific papers

AMIDOALKYLPIPERAZINYL DERIVATIVES FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISEASES

The invention relates to novel amidoalkylpiperazinyl derivatives of tricyclic heterocyclic systems of general formula (I), wherein Z represents -NH- and X represents -S-, or Z represents -S- and X represents >C=C1 represents H or -CH3, R6 and R7 both represent H, n is an integer from 0 to 4 inclusive, G represents a cyclic amide or imide moiety, and optical isomers, geometric isomers, and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of the central nervous system disorders.

Synthesis and pharmacological evaluation of new 5-(cyclo)alkyl-5-phenyl- and 5-spiroimidazolidine-2,4-dione derivatives. Novel 5-HT1A receptor agonist with potential antidepressant and anxiolytic activity

The synthesis of 5-(cyclo)alkyl-5-phenyl- and 5-spiroimidazolidine-2,4-dione derivatives with an arylpiperazinylpropyl moiety (12-23) and their in vitro and in vivo pharmacological properties and molecular characteristics were described. The investigated compounds exhibited high affinity for 5-HT1A (13-22) and 5-HT2A (18, 20, 21, 23) receptors and diversified pharmacological profile. Compounds 17, 20 and 22 showed antagonistic, partial agonistic and agonistic activity, respectively, toward 5-HT1A receptor and they were investigated as potential antidepressants and/or anxiolytics. The most interesting compound 22 (1-[3-(4-(2-methoxyphenyl)piperazin-1-yl)propyl]-3′,4′-dihydro-2′H-spiro[imidazolidine-4,1′-naphthalene]-2,5-dione), a pre- and postsynaptic 5-HT1A receptor agonist produced an antidepressant-like effect, which was more pronounced than that of imipramine in the forced swim test in mice, without affecting locomotor activity. Moreover, compound 22 produced a weak anxiolytic-like effect in the four-plate test in mice. Molecular docking studies of compound 22 to the homology model of the 5-HT1A receptor showed that a 3′,4′-dihydro-2′H-spiro[imidazolidine-4,1′-naphthalene]-2,5-dione moiety played an important role in stabilizing the ligand-receptor complex.