- 1,4-Dihydropyridines: discovery of minimal AIEEgens and their mitochondrial imaging applications
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Typical aggregation-induced emission enhancement fluorogens (AIEEgens) generally are designed as propeller-shaped molecules with multiple aromatic rotors. Described herein are 1,4-dihydropyridines, which have the minimum size necessary for AIEE, containing only a single ring, synthesized through a facile biocatalysis procedure. Owing to the AIEE property, intramolecular motion can be restrained by the surrounding environment, causing the radiative channel to open up. Both the fluorescence intensities and the lifetimes of the 1,4-dihydropyridine representatives increased with increasing viscosity, and high sensitivities were observed. On the basis of the single crystal X-ray structures, density functional theory (DFT) calculations were performed to explain the mechanism of the single-ring AIEE behaviour. Moreover, a few of the neutral AIEEgens were found to possess a high specificity towards mitochondria. As an example, one of the AIEEgens exhibited superior photostability and excellent storage tolerance, allowing for real-time imaging, viscosity mapping, and long-term tracking of the dynamics of the mitochondrial morphology.
- Zhang, Wei,Wang, Na,Liu, Yan-Hong,Jiao, Shu-Yan,Zhang, Wei-Wei,Pu, Xue-Mei,Yu, Xiao-Qi
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supporting information
p. 464 - 469
(2017/01/24)
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- Synthesis of some new 1,4-dihydropyridine derivatives through a facile one-pot Hantzsch condensation catalyzed by triethylamine
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A facile and efficient synthesis of new 1,4-dihydropyridine derivatives was reported via Hantzsch three-component condensation reaction of aldehydes or formylphenylboronic acids, ethyl acetoacetate, and ammonium acetate in the presence of a catalytic amount of triethylamine under solvent-free conditions. The method described here offers several advantages including high yields, short reaction times, and simple work-up procedure.
- Ghalem, Wassima,Boulcina, Raouf,Debache, Abdelmadjid
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experimental part
p. 733 - 737
(2012/05/20)
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- COMPOUNDS AND COMBINATIONS THEREOF FOR INHIBITING BETA-AMYLOID PRODUCTION AND METHODS OF USE THEREOF
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Provided are compounds which can be used in combination for treating diseases associated with a condition associated with cerebral accumulation of Alzheimer’s amyloid, such as Alzheimer’s disease. Also provided are methods of treating or reducing the risk of developing β-amyloid production, β-amyloid deposition, β-amyloid neurotoxicity (including abnormal hyperphosphorylation of tau) and microgliosis associated with cerebral accumulation of Alzheimer’s amyloid by administering therapeutically effective amounts of compounds which in combination can decrease β-amyloid production and capacitative calcium entry in cells. Further provided are methods for diagnosing diseases associated with cerebral accumulation of Alzheimer’s amyloid in animals or humans by administering diagnostically effective amounts of the compounds.
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Page/Page column 138-139
(2010/11/29)
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- PROCESS FOR THE PREPARATION OF 1,4-DIHYDROPYRIDINES AND NOVEL 1,4-DIHYDROPYRIDINES USEFUL AS THERAPEUTIC AGENTS
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The present invention provides a process for the preparation of 1,4-dihydropyridines of the formula (1), wherein R1 is H, NO2, Cl, OAc, OH, R2 is H, NO2, Cl, -O-CH2-O-, OMe, OAc, OEt, OH, R3 is H, NO2, Cl, N(Me)2, -O- CH2 -O-, OMe, OAc, OH, R4 is H, OMe, OAc, OH, R5 is H, Cl, I, and R6 and R7 are either methyl, ethyl or both by preparing a mixture of an aromatic aldehyde, alkyl acetoacetate and a source of ammonia, adsorbing the prepared mixture and adsorbent till adsorbent becomes free flowing, heating the material so obtained under microwave irradiation, cooling the reaction mixture and recovering the compound of formula (1). The present invention also relates to novel 1,4-dihydropyridines with cardiovascular activity.
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