- Design, synthesis, and structure–activity relationship study of potent mapk11 inhibitors
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Huntington’s disease (HD) is a rare single-gene neurodegenerative disease, which can only be treated symptomatically. Currently, there are no approved drugs for HD on the market. Studies have found that MAPK11 can serve as a potential therapeutic target f
- Gong, Mengdie,Li, Honglin,Li, Lu,Li, Shiliang,Sun, Hongxia,Tu, Mingyan,Zhao, Zhenjiang,Zhu, Lili
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- Synthesis of 3-Benzylphthalide Derivatives by Using a TDAE Strategy
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A one-pot synthesis of new 3-benzylphthalide derivatives was developed by using a strategy based on tetrakis(dimethylamino)ethylene (TDAE). The reactions in the presence of TDAE of substituted benzyl chlorides with methyl 2-formylbenzoate or of substitute
- Ibrahimi, Maroua,Khoumeri, Omar,Abderrahim, Raoudha,Terme, Thierry,Vanelle, Patrice
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p. 283 - 286
(2020/11/23)
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- Indium-Catalyzed C?F Bond Transformation through Oxymetalation/β-Fluorine Elimination to Access Fluorinated Isocoumarins
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Fluorinated heterocycles have attracted much attention in the pharmaceutical and agrochemical industries. Many strategies have already been developed to achieve the synthesis of fluorinated heterocycles. Formidable challenges remain, however, in the synthesis of fluorinated isocoumarin derivatives that are among the most alluring structural motifs. Herein, the indium-catalyzed C?F bond transformation of 2-(2,2-difluorovinyl) benzoates is reported, which are readily accessible compounds, to give a diverse array of fluorinated isocoumarins. The present reaction proceeds smoothly using inexpensive reagents: a catalytic amount of indium salt in the presence of zinc salt. A theoretical calculation of potential energy profiles showed that the reaction consists of oxymetalation with the elimination of alkyl halide and the β-fluorine elimination.
- Yata, Tetsuji,Nishimoto, Yoshihiro,Chiba, Kouji,Yasuda, Makoto
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supporting information
p. 8288 - 8294
(2021/05/21)
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- Engineering a highly selective probe for ratiometric imaging of H2S: N and revealing its signaling pathway in fatty liver disease
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Hydrogen polysulfides (H2Sn, n > 1) have continuously been proved to act as important signal mediators in many physiological processes. However, the physiological role of H2Sn and their signaling pathways in complex diseases, such as the most common liver
- Lai, Huanhua,Li, Wei,Wang, Lu,Yin, Shulu,Yuan, Lin,Zhang, Xiaobing
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p. 7991 - 7999
(2020/08/14)
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- Bioorthogonal double-fluorogenic siliconrhodamine probes for intracellular super-resolution microscopy
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A series of double-fluorogenic siliconrhodamine probes were synthesized. These tetrazine-functionalized, membrane-permeable labels allowed site-specific bioorthogonal tagging of genetically manipulated intracellular proteins and subsequent imaging using s
- Kozma,Estrada Girona,Paci,Lemke,Kele
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supporting information
p. 6696 - 6699
(2017/07/10)
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- Efficient Heterogeneous CO2 to CO Conversion with a Phosphonic Acid Fabricated Cofacial Iron Porphyrin Dimer
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For developing renewable fuels and controlling global warming, catalyst promoted conversion of CO2 to CO is essential. Numerous CO2 to CO conversion molecular catalysts have shown very high activity and stability. For large-scale con
- Mohamed, Eman A.,Zahran, Zaki N.,Naruta, Yoshinori
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p. 7140 - 7150
(2017/09/19)
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- Isomerically Pure Tetramethylrhodamine Voltage Reporters
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We present the design, synthesis, and application of a new family of fluorescent voltage indicators based on isomerically pure tetramethylrhodamines. These new Rhodamine Voltage Reporters, or RhoVRs, use photoinduced electron transfer (PeT) as a trigger for voltage sensing, display excitation and emission profiles in the green to orange region of the visible spectrum, demonstrate high sensitivity to membrane potential changes (up to 47% ΔF/F per 100 mV), and employ a tertiary amide derived from sarcosine, which aids in membrane localization and simultaneously simplifies the synthetic route to the voltage sensors. The most sensitive of the RhoVR dyes, RhoVR 1, features a methoxy-substituted diethylaniline donor and phenylenevinylene molecular wire at the 5′-position of the rhodamine aryl ring, exhibits the highest voltage sensitivity to date for red-shifted PeT-based voltage sensors, and is compatible with simultaneous imaging alongside green fluorescent protein-based indicators. The discoveries that sarcosine-based tertiary amides in the context of molecular-wire voltage indicators prevent dye internalization and 5′-substituted voltage indicators exhibit improved voltage sensitivity should be broadly applicable to other types of PeT-based voltage-sensitive fluorophores.
- Deal, Parker E.,Kulkarni, Rishikesh U.,Al-Abdullatif, Sarah H.,Miller, Evan W.
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p. 9085 - 9088
(2016/08/05)
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- Facile construction of pyrrolo[1,2-: B] isoquinolin-10(5 H)-ones via a redox-amination-aromatization-Friedel-Crafts acylation cascade reaction and discovery of novel topoisomerase inhibitors
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An efficient redox-amination-aromatization-Friedel-Crafts acylation cascade process from trans-4-hydroxyproline and 2-formylbenzoic acids has been developed for the synthesis of pyrrolo[1,2-b]isoquinolin-10(5H)-ones. Compound 3h was identified as a new potent dual topoisomerase I/II inhibitor.
- Wu, Shanchao,Liu, Na,Dong, Guoqiang,Ma, Lin,Wang, Shengzheng,Shi, Wencai,Fang, Kun,Chen, Shuqiang,Li, Jian,Zhang, Wannian,Sheng, Chunquan,Wang, Wei
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p. 9593 - 9596
(2016/08/01)
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- Asymmetric Organocatalytic Synthesis of 4-Aminoisochromanones via a Direct One-Pot Intramolecular Mannich Reaction
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A highly stereoselective one-pot intramolecular Mannich reaction using 2-oxopropyl-2-formylbenzoates and anilines as substrates, catalyzed by a secondary amine, has been developed. The procedure leads to a new class of 4-aminoisochromanones bearing two ad
- Vetica, Fabrizio,Fronert, Jeanne,Puttreddy, Rakesh,Rissanen, Kari,Enders, Dieter
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p. 4451 - 4458
(2016/12/14)
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- An Efficient Entry to syn- and anti-Selective Isoindolinones via an Organocatalytic Direct Mannich/Lactamization Sequence
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(Chemical Equation Presented) An organocatalytic direct Mannich-lactamization sequence for the syntheses of pharmacologically important enantioenriched isoindolinones is reported. The method utilizes simple α-amino acids to deliver syn- and anti- selectiv
- Bisai, Vishnumaya,Unhale, Rajshekhar A.,Suneja, Arun,Dhanasekaran, Sivasankaran,Singh, Vinod K.
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supporting information
p. 2102 - 2105
(2015/05/13)
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- Enantioselective addition of arylboronic acids to methyl 2-formylbenzoates by using a ruthenium/Me-BIPAM catalyst for synthesis of chiral 3-aryl-isobenzofuranones
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Ruthenium/Me-BIPAM-catalyzed asymmetric addition of arylboronic acids to methyl 2-formylbenzoates afforded chiral 3-aryl-isobenzofuranones. [RuCl2(p-cymene)]2/Me-BIPAM and RuCl2(PPh3)3/Me-BIPAM catalyst systems tolerate a variety of functional groups and give high yields with high enantioselectivities.
- Yohda, Masaaki,Yamamoto, Yasunori
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p. 10874 - 10880
(2015/11/17)
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- A general approach to spirolactonized Si-rhodamines
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A general approach has been developed for the synthesis of spirolactonized Si-rhodamines (SiRBs). The alternative synthetic route provides a facile opportunity to access various SiRBs bearing ring-expanded scaffolds and substituents for conjugation. By click reaction, a near-infrared (NIR) mitochondrial tracker was prepared, displaying specific mitochondrial staining in cells. This journal is
- Wang, Baogang,Chai, Xiaoyun,Zhu, Weiwei,Wang, Ting,Wu, Qiuye
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p. 14374 - 14377
(2014/12/11)
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- Highly enantioselective synthesis of 2,3-dihydro-1 H-imidazo[2,1-a isoindol-5(9b H)-ones via catalytic asymmetric intramolecular cascade imidization-nucleophilic addition-lactamization
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Highly enantioselective catalytic asymmetric intramolecular cascade imidization-nucleophilic addition-lactamization of N1-alkylethane-1,2-diamine with methyl 2-formylbenzoate catalyzed by a chiral phosphoric acid represents the first efficient method for the preparation of medicinally interesting chiral 2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-ones with high yields and excellent enantioselectivities. This strategy has been shown to be quite general toward various methyl 2-formylbenzoates.
- He, Yuwei,Cheng, Chuyu,Chen, Bin,Duan, Kun,Zhuang, Yue,Yuan, Bo,Zhang, Meisan,Zhou, Yougui,Zhou, Zihong,Su, Yu-Jun,Cao, Rihui,Qiu, Liqin
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supporting information
p. 6366 - 6369
(2015/01/16)
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- SUBSTITUTED BENZOYLAMINO-INDAN-2-CARBOXYLIC ACIDS AND RELATED COMPOUNDS
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The present invention relates to A compound of the formula Ia wherein in any of its stereoisomers forms or a mixture of stereoisomeric forms in any ratio, or a physiologically acceptable salt thereof, wherein the substituents are as described herein. The inventive compounds have CXCR5 inhibitory activity are particularly useful in treating or preventing various inflammatory diseases, such as rheumatoid arthritis, multiple sclerosis, lupus, Crohn's Disease, associated with the modulation of the human CXCR5 receptor.
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- NEW COMPOUNDS I/418
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There is provided compounds of formula I, wherein R1 to R7 have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.
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Page/Page column 33
(2008/06/13)
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- Furan ring opening - Isocoumarine ring closure: A recyclization reaction of 2-carboxyaryldifurylmethanes
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A general method for the synthesis of isocoumarine derivatives has been developed. Bis(5-R-2-furyl)methylbenzoic acids (R = methyl, ethyl) underwent recyclization and subsequent cyclization into tetracyclic isochromene-1-one derivatives under treatment with hydrogen chloride in methanol. It has been shown that intermediate 4-(5-R-furan-2-yl)-3-(3-oxo-3-R-propyl)-isochromene-1- ones can be obtained selectively by varying a concentration of the hydrogen chloride and reaction times. In the case of R = tert-butyl only corresponding 4-[5-(tert-butyl)-2-furyl]-3-(4,4-dimethyl-3-oxopentyl)-1-isochromenones were isolated regardless of the reaction conditions.
- Abaev, Vladimir T.,Dmitriev, Artem S.,Gutnov, Andrey V.,Podelyakin, Sergey A.,Butin, Alexander V.
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p. 1195 - 1204
(2007/10/03)
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