Design, synthesis, and systematic evaluation of 4-arylpiperazine- and 4-benzylpiperidine napthyl ethers as inhibitors of monoamine neurotransmitters reuptake. Issue 20 (1st November 2018)

• Record Type: Journal Article
• Authors: Paudel, Suresh; Min, Xiao; Acharya, Srijan; Khadka, Daulat Bikram; Yoon, Goon; Kim, Kyeong-Man; Cheon, Seung Hoon
• Is Part Of: Bioorganic & medicinal chemistry. Volume 26:Issue 20(2018)
• Page Start: 5538
• Page End: 5546
• Publication Date: 2018-11-01
• Subjects: Depression -- 4-Arylpiperazine -- 4-Benzylpiperidine -- Naphthyl ether -- 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.2018.09.033
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: Abstract: Two series of 4-arylpiperazine- and 4-benzylpiperidine naphthyl ethers were designed based on structure-activity relationship (SAR) and docking model of reported monoamine neurotransmitters reuptake inhibitors. The compounds were synthesized in 3-simple steps and their biological activities were evaluated. Several compounds were proven to be potent inhibitors of serotonin and norepinephrine reuptake. Computer docking was performed to study the interaction of the most potent compound35 with human serotonin transporter. The results of the analyses suggest that 4-arylpiperazine- and 4-benzylpiperidine naphthyl ethers might be promising antidepressants worthy of further studies.