32263-70-0Relevant articles and documents
The evaluation of 1-tetralone and 4-chromanone derivatives as inhibitors of monoamine oxidase
Cloete, Stephanus J.,N’Da, Clarina I.,Legoabe, Lesetja J.,Petzer, Anél,Petzer, Jacobus P.
, p. 491 - 507 (2020/10/02)
Abstract: Monoamine oxidase (MAO) is of much clinical relevance, and inhibitors of this enzyme are used in the treatment for neuropsychiatric and neurodegenerative disorders such as depression and Parkinson’s disease. The present study synthesises and evaluates the MAO inhibition properties of a series of 33 1-tetralone and 4-chromanone derivatives in an attempt to discover high-potency compounds and to expand on the structure–activity relationships of MAO inhibition by these classes. Among these series, eight submicromolar MAO-A inhibitors and 28 submicromolar MAO-B inhibitors are reported, with all compounds acting as specific inhibitors of the MAO-B isoform. The most potent inhibitor was a 1-tetralone derivative (1h) with IC50 values of 0.036 and 0.0011?μM for MAO-A and MAO-B, respectively. Interestingly, with the reduction of 1-tetralones to the corresponding alcohols, a decrease in MAO inhibition potency is observed. Among these 1-tetralol derivatives, 1p (IC50 = 0.785?μM) and 1o (IC50 = 0.0075?μM) were identified as particularly potent inhibitors of MAO-A and MAO-B, respectively. Potent compounds such as those reported here may act as leads for the future development of MAO-B specific inhibitors. Graphic abstract: The present study describes the MAO inhibitory activities of a series of 1-tetralone and 4-chromanone derivatives. Numerous high-potency MAO-B specific inhibitors were identified.[Figure not available: see fulltext.].
COMPOUND HAVING S1P5 RECEPTOR AGONIST ACTIVITY
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Paragraph 0155, (2021/01/14)
Provided is a compound in which the balance of the agonist activity against the S1P5 receptor relative to the S1P1 receptor has been improved in order to develop a pharmaceutical useful for the treatment of SIPs-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases. A compound represented by the general formula (V) (wherein, all the symbols are as defined in the specification) has an improved balance of the agonist activity against the S1P5 receptor relative to the S1P1 receptor, and can thus serve as a therapeutic agent for S1P5-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases.
TETRAHYDRONAPHTHALENE ESTROGEN RECEPTOR MODULATORS AND USES THEREOF
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Paragraph 0243, (2017/06/06)
Described herein are tetrahydronaphthalene compounds with estrogen receptor modulation activity or function having the Formula I structure: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structura