Central Research Laboratories, Green Cross Corporation, 303 Bojeong-Dong, Giheung-Gu, Yongin 446-770, Republic of Korea.
Bioorg Med Chem Lett. 2010 Mar 1;20(5):1705-11. doi: 10.1016/j.bmcl.2010.01.093. Epub 2010 Jan 21.
Arylpiperzine-containing pyrrole 3-carboxamide derivatives were synthesized and evaluated as novel antidepressant compounds. The various analogues were efficiently prepared and bio-assayed for binding to 5-HT(2A), 5-HT(2C) receptor, and 5-HT transporter. Based on their in vitro and in vivo activities as well as selectivity over other neurotransmitter receptors and PK profiles, 33 and 34 were identified as lead compounds. Consequently, this pyrrole series of compounds appears to be promising enough to warrant further investigation.
含芳基哌嗪的吡咯-3-甲酰胺衍生物被合成并评估为新型抗抑郁化合物。各种类似物被有效地制备并进行了与 5-HT(2A)、5-HT(2C)受体和 5-HT 转运体结合的生物测定。根据它们在体外和体内的活性以及对其他神经递质受体的选择性和 PK 特征，33 和 34 被鉴定为先导化合物。因此，这个吡咯系列化合物具有足够的潜力，值得进一步研究。
