39802-78-3Relevant articles and documents
KDS2010, a Newly Developed Reversible MAO-B Inhibitor, as an Effective Therapeutic Candidate for Parkinson’s Disease
An, Heeyoung,Cho, Doo-Wan,Choi, Ji Won,Han, Su-Cheol,Heo, Jun Young,Jang, Bo Ko,Jeon, Sang Ryong,Kim, Hyeon Jeong,Kim, Sangwook,Kim, Siwon,Lee, C. Justin,Lee, Hyowon,Nam, Min-Ho,Oh, Soo-Jin,Park, Jong-Hyun,Park, Ki Duk,Park, Sun Jun,Song, Hyo Jung,Yang, Young-Su,Yoon, Hyung Ho
, p. 1729 - 1747 (2021/10/08)
Monoamine oxidase-B (MAO-B) is a well-established therapeutic target for Parkinson’s disease (PD); however, previous clinical studies on currently available irreversible MAO-B inhibitors have yielded disappointing neuroprotective effects. Here, we tested the therapeutic potential of KDS2010, a recently synthesized potent, selective, and reversible MAO-B inhibitor in multiple animal models of PD. We designed and synthesized a series of α-aminoamide derivatives and found that derivative KDS2010 exhibited the highest potency, specificity, reversibility, and bioavailability (> 100%). In addition, KDS2010 demonstrated significant neuroprotective and anti-neuroinflammatory efficacy against nigrostriatal pathway destruction in the mouse MPTP model of parkinsonism. Treatment with KDS2010 also alleviated parkinsonian motor dysfunction in 6-hydroxydopamine-induced and A53T mutant α-synuclein overexpression rat models of PD. Moreover, KDS2010 showed virtually no toxicity or side effects in non-human primates. KDS2010 could be a next-generation therapeutic candidate for PD.
PIPERIDINES USEFUL FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS
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Page 39; 41, (2008/06/13)
The invention relates to compounds which are substituted chiral or achiral derivatives of 3- or 4- aminopiperidine of the general formula (I). The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more compounds of general formula I and especially their use as inhibitors of β-secretases.
Comparison of the Properties of Liquid Crystals Derived from Certain Lateral Halogeno-substituted Azomethines
Brown, John W.,Butcher, Jane L.,Byron, David J.,Gunn, Elaine S.,Rees, Mark,Wilson, Robert C.
, p. 255 - 266 (2007/10/02)
Twenty-eight 4-n-alkoxy-N-(2- and 2'-halogenobiphenyl-4-ylmethylene)anilines comprising 4,8,8,4, and 4 members derived , respectively, from 2-fluoro-, 2'-fluoro-, 2'-chloro-, 2'-bromo-, and 2'-iodo-biphenyl-4-carbaldehyde, together with six 4-p-n-alkoxy-2'-fluorobenzylideneaminobiphenyls have been prepared.The liquid crystal behaviour of these compounds has been compared with analogous azomethines with reversed CH=N linkage, previously reported.