Design, synthesis and docking study of 4-arylpiperazine carboxamides as monoamine neurotransmitters reuptake inhibitors. Issue 14 (7th August 2018)

• Record Type: Journal Article
• Authors: Paudel, Suresh; Sun, Ningning; Khadka, Daulat Bikram; Yoon, Goon; Kim, Kyeong-Man; Cheon, Seung Hoon
• Is Part Of: Bioorganic & medicinal chemistry. Volume 26:Issue 14(2018)
• Page Start: 4127
• Page End: 4135
• Publication Date: 2018-08-07
• Subjects: 4-Arylpiperazine carboxamide -- Serotonin reuptake inhibitor -- Norepinephrine reuptake inhibitor -- Docking; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2018.06.043
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: Abstract: Rational drug design method has been used to generate 4-arylpiperazine carboxamides in an effort to develop safer, more potent and effective monoamine neurotransmitters reuptake inhibitors. Out of twenty-seven synthesized compounds, compound 9 displayed potent monoamine neurotransmitter reuptake inhibitory activity against HEK cells transfected with hSERT or hNET. A Surflex-Dock docking model of 9 was also studied.