2015
DOI: 10.1002/ardp.201400455
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Synthesis of Carbamide Derivatives Bearing Tetrahydroisoquinoline Moieties and Biological Evaluation as Analgesia Drugs in Mice

Abstract: Transient receptor potential vanilloid 1 (TRPV1) is a ligand-gated non-selective cation channel that is considered to be an important pain integrator. Tetrahydroisoquinoline, the prototypical antagonist of TRPV1, has a clear therapeutic potential. Here, a series of carbamide derivatives of tetrahydroisoquinoline were designed and synthesized. Preliminary biological tests suggested that the compounds I 1, I 2, and I 9 had favorable TRPV1 antagonism activity. In further studies, I 1 exhibited better antinocicept… Show more

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Cited by 3 publications
(3 citation statements)
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“…1 H NMR (600 MHz, CDCl 3 ): δ 7.78 (q, J = 3.8, 2.9 Hz, 1H), 7.42–7.00 (m, 2H), 4.10 (s, 2H), 3.14 (q, J = 4.3, 2.8 Hz, 2H), 3.04 (t, J = 5.7 Hz, 2H), 1.93 (br s, 1H). Analytical data were identical to those reported in the literature …”
Section: Methodsmentioning
confidence: 51%
See 1 more Smart Citation
“…1 H NMR (600 MHz, CDCl 3 ): δ 7.78 (q, J = 3.8, 2.9 Hz, 1H), 7.42–7.00 (m, 2H), 4.10 (s, 2H), 3.14 (q, J = 4.3, 2.8 Hz, 2H), 3.04 (t, J = 5.7 Hz, 2H), 1.93 (br s, 1H). Analytical data were identical to those reported in the literature …”
Section: Methodsmentioning
confidence: 51%
“…Analytical data were identical to those reported in the literature. 43 5-Bromo-1,2,3,4-tetrahydroisoquinoline (2c). Colorless oil (80.2 mg, yield 76%).…”
Section: ■ Conclusionmentioning
confidence: 99%
“…Increase aromatic amino acid decarboxylase activity, catechol-Omethyl-transferase-inhibitro, methyl donor, methyl guanidine inhibitor. Antithrombotic activity [20], Free radical scavenger and inhibitor of glutamate induced excitotoxicity [21], analgesic [22], antihypertensive [23] and antiviral [24] 6.…”
Section: Discussionmentioning
confidence: 99%