15258-05-6Relevant articles and documents
Deuterium-substituted 3-(methylsulfonyl)-L-phenylalanine derivative and medicine composition, medicine preparation and application thereof
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Paragraph 0034; 0079; 0080, (2017/08/31)
The invention provides a deuterium-substituted 3-(methylsulfonyl)-L-phenylalanine derivative and a medicine composition, a medicine preparation and application thereof. The deuterium-substituted 3-(methylsulfonyl)-L-phenylalanine derivative has a structure shown in a formula I. A compound provided by the invention and the derivative thereof have good LFA-1 antagonistic activity, excellent pharmacodynamics property and lower toxicity. The formula I is shown in the description, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20 and R21 are respectively and independently hydrogen or deuterium, and at least contain one deuterium; R is hydrogen.
Design and synthesis of 4-benzylpiperidine carboxamides as dual serotonin and norepinephrine reuptake inhibitors
Paudel, Suresh,Cao, Yongkai,Guo, Shuohan,An, Byeongkwan,Kim, Kyeong-Man,Cheon, Seung Hoon
, p. 6418 - 6426 (2015/10/05)
A series of 4-benzylpiperidine carboxamides were designed and synthesized, and tested for their dual (serotonin and norepinephrine) reuptake inhibition. The synthesis of 4-benzylpiperidine carboxamides involved two main steps: amidation and substitution. Derivatives with 3 carbon linker displayed better activity than with 2 carbon linker. 4-Biphenyl- and 2-naphthyl-substituted derivatives 7e and 7j showed greater dual reuptake inhibition than standard drug venlafaxine HCl.