60669-22-9Relevant academic research and scientific papers
Antiferroptotic Activity of Phenothiazine Analogues: A Novel Therapeutic Strategy for Oxidative Stress Related Disease
Liu, Jun,Bandyopadhyay, Indrajit,Zheng, Lei,Khdour, Omar M.,Hecht, Sidney M.
supporting information, p. 2165 - 2173 (2020/12/17)
Ferroptosis is an iron-catalyzed, nonapoptotic form of regulated necrosis that has been implicated in the pathological cell death associated with various disorders including neurodegenerative diseases (e.g., Friedreich's ataxia (FRDA), Alzheimer's disease, and Parkinson's disease), stroke, and traumatic brain injury. Recently, we showed that lipophilic methylene blue (MB) and methylene violet (MV) analogues both promoted increased frataxin levels and mitochondrial biogenesis, in addition to their antioxidant activity in cultured FRDA cells. Presently, we report the synthesis of series of lipophilic phenothiazine analogues that potently inhibit ferroptosis. The most promising compounds (1b-5b) exhibited an improved protection compared to the parent phenothiazine against erastin- and RSL3-induced ferroptotic cell death. These analogues have equivalent or better potency than ferrostatin-1 (Fer-1) and liproxstatin-1 (Lip-1), that are among the most potent inhibitors of this regulated cell death described so far. They represent novel lead compounds with therapeutic potential in relevant ferroptosis-driven disease models such as FRDA.
A yellow star longicorn pheromone preparation method (by machine translation)
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Paragraph 0101; 0102; 0103, (2018/09/21)
The present invention provides a preparation method of huang xing longicorn pheromone, the present invention relates to chiral compound compound 1 as the initial reactant, and selecting different quaternary phosphonium salt, can be efficient and rapid growth of the aliphatic, obtained with high stereo specific hued rectangle which bears longicorn pheromone. The present invention provides a preparation method of the operation is simple, short synthetic route, and the goal overall yield of the product is high, up to 20% (as the compound 1 is calculated as the initiator), is suitable for the large scale synthesis, the beetles of the pheromone huang xing active research, biological experiment, agricultural applications and pest control of important significance. (by machine translation)
NOVEL GLYCINE TRANSPORT INHIBITORS FOR THE TREATMENT OF PAIN
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Page/Page column 51; 52, (2018/08/12)
The present invention relates to novel glycine transport inhibitor compounds and their use for treating pain.
Development of sulfonamide AKT PH domain inhibitors
Ahad, Ali Md.,Zuohe, Song,Du-Cuny, Lei,Moses, Sylvestor A.,Zhou, Li Li,Zhang, Shuxing,Powis, Garth,Meuillet, Emmanuelle J.,Mash, Eugene A.
supporting information; experimental part, p. 2046 - 2054 (2011/05/05)
Disruption of the phosphatidylinositol 3-kinase/AKT signaling pathway can lead to apoptosis in cancer cells. Previously we identified a lead sulfonamide that selectively bound to the pleckstrin homology (PH) domain of AKT and induced apoptosis when present at low micromolar concentrations. To examine the effects of structural modification, a set of sulfonamides related to the lead compound was designed, synthesized, and tested for binding to the expressed PH domain of AKT using a surface plasmon resonance-based competitive binding assay. Cellular activity was determined by means of an assay for pAKT production and a cell killing assay using BxPC-3 cells. The most active compounds in the set are lipophilic and possess an aliphatic chain of the proper length. Results were interpreted with the aid of computational modeling. This paper represents the first structure-activity relationship (SAR) study of a large family of AKT PH domain inhibitors. Information obtained will be used in the design of the next generation of inhibitors of AKT PH domain function.
Syntheses of 5-hexadecanolide, 6-acetoxy-5-hexadecanolide and tanikolide
Chang, Meng-Yang,Lin, Chien-Lun,Chen, Shui-Tein
, p. 787 - 794 (2007/10/03)
Total syntheses of 5-hexadecanolide (1), 6-acetoxy-5-hexadecanolide (2) and tanikolide (3) are described. 1-Bromoundecane (4) and 5-benzyl-1-pentanal (5) were chosen as starting materials. Wittig olefination and Grignard addition 4 and 5 afforded the 16-carbon skeleton, which underwent a series of functional group transformations to give δ-lactone derivatives 1, 2 and 3.
Synthesis and biological activity of new diarylalkenes
Golebiewski, W. Marek,Cieniecka-Ros?onkiewicz,Szybinska
, p. 26 - 30 (2007/10/03)
Condensation of 5-nitro-, 3-chloro-, and 5-chlorosalicylic acid with formaldehyde afforded dimeric disalicylmethanes which were O-methylated with dimethyl sulfate and oxidized with chromium(VI) oxide to give the diarylketones 10, 11, 12. Wittig reaction with ylides obtained by deprotonation of alkyltriphenylphosphonium salts with sodium bis (trimethylsilyl)amide yielded a series of diarylalkenes. Some of the obtained compounds showed high antimicrobial activity in vitro against Bacillus subtilis and Mycobacterium smegmatis.
Stereoselective total syntheses of (-)-desoxoprosopinine and (-)-desoxoprosophylline: Palladium(0)-catalyzed intramolecular N-alkylation for the key piperidine ring formation
Takao,Nigawara,Nishino,Takagi,Maeda,Tadano,Ogawa
, p. 5681 - 5704 (2007/10/02)
Intramolecular N-alkylation of D-glucose-derived substrate 21E proceeded in an S(N)2' mode smoothly in the presence of a Pd(0) catalyst and n-Bu4NI. The major cyclization product, a 2,6-dialkylated piperidine 22t, was effectively converted into the title alkaloids.
Pyrrolealdehyde derivative
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, (2008/06/13)
A novel pyrrolealdehyde derivative represented by the following formula (I): STR1 wherein R represents C10 -C16 alkyl unsubstituted or substituted by at least one substituent selected from the group consisting of halo, hydroxy, amino, carbamoyl, C1 -C5 alkylamino, C2 -C6 dialkylamino, C2 -C6 acylamino, C1 -C5 alkylthio, mercapto, C2 -C6 acyloxy, carbamoyloxy, C6 -C12 aryl and C3 -C7 cycloalkyl; or C10 -C16 alkenyl having at least one vinyl, and a pharmaceutically acceptable salt thereof are provided. The compounds are highly effective in reducing the level of triglyceride and cholesterol in serum, and useful as an active ingredient of a pharmaceutical composition for treating hyperlipemia and arteriosclerosis.
OZONOLYSIS OF ALKENES AND INVESTIGATION OF THE REACTIONS OF POLYFUNCTIONAL COMPOUNDS. XXIII. A NEW SYNTHESIS OF DIASTEREOMERIC (+/-)-13,17,21-TRIMETHYLTRI-, (+/-)-13,17,21-TRIMETHYLPENTA-, AND (+/-)-13,17,21-TRIMETHYLHEPTATRIACONTANES
Odinokov, V. N.,Akhmetova, V. R.,Tolstikov, G. A.,Moiseenkov, A. M.,Semenovskii, A. V.
, p. 443 - 447 (2007/10/02)
A three-stage synthesis of the hydrocarbons 13,17,21-trimethyltri-, 13,17,21-trimethylpenta-, and 13,17,21-trimethylheptatriacontanes, isolated from the eggs of the tobacco worm (Manduc Sexta L.), was realized from (E,E)-4,8-dimethyl-1,12-dioxo-4,8-tridecadiene.
