711-82-0Relevant articles and documents
Pseudorotaxane capped mesoporous silica nanoparticles for 3,4-methylenedioxymethamphetamine (MDMA) detection in water
Lozano-Torres, Beatriz,Pascual, Lluís,Bernardos, Andrea,Marcos, María D.,Jeppesen, Jan O.,Salinas, Yolanda,Martínez-Má?ez, Ramón,Sancenón, Félix
, p. 3559 - 3562 (2017)
Mesoporous silica nanoparticles loaded with fluorescein and capped by a pseudorotaxane, formed between a naphthalene derivative and cyclobis(paraquat-p-phenylene) (CBPQT4+), were used for the selective and sensitive fluorogenic detection of 3,4-methylenedioxymethamphetamine (MDMA).
Indane derivative and synthetic method and medicinal application thereof
-
Paragraph 0056; 0057; 0058, (2017/09/02)
The invention discloses an indane derivative and a synthetic method and medicinal application thereof. The structural general formula is as shown in the specification. The indane derivative disclosed by the invention has excellent inhibitory activity and high selectivity on MAO-B.
Synthesis and inhibitory evaluation of 3-linked imipramines for the exploration of the S2 site of the human serotonin transporter
Brink?, Anne,Larsen, Maja T.,Kolds?, Heidi,Besenbacher, Louise,Kolind, Anders,Schi?tt, Birgit,Sinning, Steffen,Jensen, Henrik H.
supporting information, p. 2725 - 2738 (2016/06/08)
The human serotonin transporter is the primary target of several antidepressant drugs, and the importance of a primary, high affinity binding site (S1) for antidepressant binding is well documented. The existence of a lower affinity, secondary binding site (S2) has, however, been debated. Herein we report the synthesis of 3-position coupled imipramine ligands from clomipramine using a copper free Sonogashira reaction. Ligand design was inspired by results from docking and steered molecular dynamics simulations, and the ligands were utilized in a structure-activity relationship study of the positional relationship between the S1 and S2 sites. The computer simulations suggested that the S2 site does indeed exist although with lower affinity for imipramine than observed within the S1 site. Additionally, it was possible to dock the 3-linked imipramine analogs into positions which occupy the S1 and the S2 site simultaneously. The structure activity relationship study showed that the shortest ligands were the most potent, and mutations enlarging the proposed S2 site were found to affect the larger ligands positively, while the smaller ligands were mostly unaffected.