Further optimization of novel pyrrole 3-carboxamides for targeting serotonin 5-HT2A, 5-HT2C, and the serotonin transporter as a potential antidepressant
- Further optimization of novel pyrrole 3-carboxamides for targeting serotonin 5-HT2A, 5-HT2C, and the serotonin transporter as a potential antidepressant
- 강석연; 박은정; 박우규; 김현정; 최길돈; 정명은; 서희정; 김민주; 배애님; 김정민; 이진화
- serotonin; 5-Ht2a; 5-Ht2c; depression; Antidepressant; Piperazine; Pyrrole
- Issue Date
- Bioorganic & medicinal chemistry
- VOL 18, 6156-6169
- In the continuing search for novel compounds targeting serotonin 5-HT2A, 5-HT2C, and serotonin
transporter, new arylpiperazine-containing pyrrole 3-carboxamide derivatives were synthesized and
evaluated. Based on the lead reported previously, structural modifications regarding N-(3-(4-(2,3-dichlorophenyl)
piperazin-1-yl)propyl)-1,2-dimethyl-5-phenyl-1H-pyrrole-3-carboxamide 5, were accomplished
for improvements in not only binding affinity against serotonin receptors and transporter, but
also in hERG channel inhibition. Along the line, both the forced swimming tests and spontaneous locomotor
activity tests were performed to distinguish between antidepressant activity and false positive
results. As potential antidepressant agents, both 2,4-dimethyl-5-phenyl-1H-pyrrole-3-carboxamide and
5-tert-butyl-2-methyl-1H-pyrrole-3-carboxamide derivatives exhibited favorable in vitro and in vivo
activities, warranting further investigation around these scaffolds.
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