Synthesis and bioactivity of aripiprazole derivatives.
Ten aripirazole (CAS 129722-12-9) derivatives were prepared and examined for dopamine receptor antagonist activity. The structures of these newly synthesized compounds were confirmed by their elemental analyses and by IR, 1H-NMR and mass spectra. It was demonstrated that all the new compounds have dopamine receptor antagonist activity to a certain extent. Three compounds showed more potent activity than aripiprazole.
Ge
Hai-Xia
HX
Department of Organic Chemistry, China Pharmaceutical University, Nanjing, China.
Wang
Li-Chen
LC
Jiang
Zhen-Zhou
ZZ
Ni
Sheng-Liang
SL
D000818:Animals; D014150:Antipsychotic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001058:Apomorphine / Q000037:antagonists & inhibitors / Q000494:pharmacology; D000068180:Aripiprazole; D018491:Dopamine Agonists / Q000494:pharmacology; D018492:Dopamine Antagonists / Q000494:pharmacology; D005260:Female; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D013058:Mass Spectrometry; D051379:Mice; D008813:Mice, Inbred ICR; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D015363:Quinolones / Q000138:chemical synthesis* / Q000494:pharmacology*; D011954:Receptors, Dopamine / Q000187:drug effects; D012727:Sex Characteristics; D013055:Spectrophotometry, Infrared; D013239:Stereotyped Behavior / Q000187:drug effects
D014150:Antipsychotic Agents; D018491:Dopamine Agonists; D018492:Dopamine Antagonists; D007202:Indicators and Reagents; D010879:Piperazines; D015363:Quinolones; D011954:Receptors, Dopamine; D000068180:Aripiprazole; D001058:Apomorphine