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Design, Synthesis, and Functional Evaluation of 1, 5-Disubstituted Tetrazoles as Monoamine Neurotransmitter Reuptake Inhibitors

Paudel S, Wang S, Kim E, Kundu D, Min X, Shin CY, Kim KM

Tetrazoles were designed and synthesized as potential inhibitors of triple monoamine neurotransmitters (dopamine, norepinephrine, serotonin) reuptake based on the functional and docking simulation of compound 6 which were performed in...
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Structural Requirements for Modulating 4-Benzylpiperidine Carboxamides from Serotonin/Norepinephrine Reuptake Inhibitors to Triple Reuptake Inhibitors

Paudel S, Kim E, Zhu A, Acharya S, Min X, Cheon SH, Kim KM

In this study, we determined the effect of 24 different synthetic 4-benzylpiperidine carboxamides on the reuptake of serotonin, norepinephrine, and dopamine (DA), and characterized their structure–activity relationship. The compounds with...
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Comparative Pre-clinical Efficacy of Chinese and Indian Cultivars of Bitter Melon (Momordica charantia) against Pancreatic Cancer

Kandhari K, Paudel S, Raina K, Agarwal C, Kant R, Wempe MF, Bryant CO, Agarwal R

Given the high rates of incidence and mortality associated with pancreatic cancer (PanC), there is a need to develop alternative strategies to target PanC. Recent studies have demonstrated that fruits...
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Structure–Activity Relationship and Evaluation of Phenethylamine and Tryptamine Derivatives for Affinity towards 5-Hydroxytryptamine Type 2A Receptor

Wang S, Zhu A, Paudel S, Jang CG, Lee YS, Kim KM

Among 14 subtypes of serotonin receptors (5-HTRs), 5-HT 2AR plays important roles in drug addiction and various psychiatric disorders. Agonists for 5-HT 2AR have been classified into three structural groups:...
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Novel GPR43 Agonists Exert an Anti-Inflammatory Effect in a Colitis Model

Park BO, Kang JS, Paudel S, Park SG, Park BC, Han SB, Kwak YS, Kim JH, Kim S

GPR43 (also known as FFAR2), a metabolite-sensing G-protein-coupled receptor stimulated by short-chain fatty acid (SCFA) ligands is involved in innate immunity and metabolism. GPR43 couples with Gα i/o and Gα...
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Potential Functional Role of Phenethylamine Derivatives in Inhibiting Dopamine Reuptake: Structure–Activity Relationship

Kundu D, Zhu A, Kim E, Paudel S, Jang CG, Lee YS, Kim KM

Numerous psychotropic and addictive substances possess structural features similar to those of β-phenethylamine (β-PEA). In this study, we selected 29 β-PEA derivatives and determined their structure–activity relationship (SAR) to their...
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