- Mechano-Sensitive Synthetic Ion Channels
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Mechanical stress is a ubiquitous stimulus sensed by membrane proteins, but rarely by synthetic molecules. Inspired by mechano-sensitive ion channels found in cell membranes, tension-responsive transmembrane multiblock amphiphiles were developed. In membranes, a single-transmembrane amphiphile responds to both expanding and contracting tensions to weaken and strengthen the stacking of membrane-spanning units, respectively, and ion transportation is triggered by expanding tension to form a supramolecular channel, while little transportation is observed under a tensionless condition. In contrast, a three-transmembrane amphiphile showed little spectroscopic response to tensions, likely due to weaker stacking of membrane-spanning units than in the single-transmembrane amphiphile. Nevertheless, the three-transmembrane amphiphile shows ion transportation by forming a unimolecular channel even under a tensionless condition, and the ion-transporting activity decreased with expanding tension. Interestingly, the estimated operating force of these synthetic systems was comparable to that of the mechano-sensitive proteins. This study opens the door toward new mechano-sensitive molecular devices.
- Muraoka, Takahiro,Umetsu, Kaori,Tabata, Kazuhito V.,Hamada, Tsutomu,Noji, Hiroyuki,Yamashita, Takashi,Kinbara, Kazushi
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Read Online
- BIARYL DERIVATIVE AND MEDICINE CONTAINING SAME
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Provided is a compound showing excellent antifungal activity against Trichophyton fungus, which is a major causative microorganism of superficial mycosis, and high effectiveness on diseases caused by Trichophyton fungi. A biaryl derivative represented by the formula (I) or a salt thereof: wherein ring A is an optionally substituted phenyl, or an optionally substituted 5- or 6-membered ring heteroaryl (ring A may be further condensed to form an optionally substituted fused ring); Q is CH2, C=O, NH, O, S or the like; X1, X2 and X3 are CR1 or N; Y is CH or N; Z is CR2b or N; R2a and R2b are each a hydrogen atom, a halogen atom, an optionally substituted C1-C6 alkyl group, a C1-C6 haloalkyl group or the like; R2a and R2b may form, together with carbon atoms bonded thereto, an optionally substituted carbocycle, or an optionally substituted heterocycle.
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Paragraph 0321; 0322
(2018/08/07)
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- PHARMACEUTICALS COMPRISING BIARYL DERIVATIVES OR SALTS THEREOF
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PROBLEM TO BE SOLVED: To provide compounds with excellent antimycotic activity against Trichophyton. SOLUTION: The invention provides pharmaceuticals comprising biaryl derivatives represented by general formula (I) or salts thereof, where ring A is optionally substituted phenyl or the like; Q is CH2 or the like; X1, X2 and X3 are CR1 or the like; and Y is CH or N. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
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Paragraph 0315; 0316; 0317
(2018/10/24)
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- Povarov reaction, scope and limitations: Preparation of diversely heterocyclic tetrahydro-1H-cyclopenta[c]quinolines
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Parallel synthesis of diverse heterocyclic-tetrahydro-1H-cyclopenta[c]quinolines in excellent yields and high endo diastereoselectivity has been described hereia These compounds are highly functionalized natural product-like tricyclic systems, which may be useful as biologically relevant targets. Fine tuning of the reaction conditions need to be performed depending on the nature and molecular structure of the heterocyclic aromatic carbaldehyde, as well as the choice of the Lewis acid catalyst. Synthesis of the heterocyclic aromatic aldehyde precursors of the Povarov Reaction is also described.
- Ni?o, Patricia,Caba, Marta,Aguilar, Nuria,Terricabras, Emma,Albericio, Fernando,Fernàndez, Joan-Carles
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p. 1117 - 1130
(2017/04/28)
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- SPIROCYCLIC ISOXAZOLINES AS ANTIPARASITIC AGENTS
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The invention recites spirocyclic isoxazoline derivatives of Formula (1) stereoisomers thereof, veterinary or pharmaceutical acceptable salts thereof, compositions thereof, processes for making, and their use as a parasiticide in an animal. The variables
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Page/Page column 40; 41
(2014/03/26)
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- SUBSTITUTED TRICYCLIC COMPOUNDS WITH ACTIVITY TOWARDS EP1 RECEPTORS
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The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.
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Page/Page column 98
(2013/10/22)
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- NOVEL COMPOUNDS AS ANTAGONISTS OR INVERSE AGONISTS FOR OPIOID RECEPTORS
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This invention relates to novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy.
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Page/Page column 97
(2010/09/07)
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- Synthesis of 5-bromopyridyl-2-magnesium chloride and its application in the synthesis of functionalized pyridines
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(Chemical Equation Presented) The 5-bromopyridyl-2-magnesium chloride (2), which was not accessible previously, was efficiently synthesized for the first time via an iodomagnesium exchange reaction with 5-bromo-2-iodopyridine (1). This reactive intermediate was allowed to react with a variety of electrophiles to afford a range of useful functionalized pyridine derivatives. Application of this methodology to 5-bromo-2-iodo-3-picoline provided a simple and economical synthesis of a key intermediate for the preparation of Lonafarnib, a potent anticancer agent.
- Song, Jinhua J.,Yee, Nathan K.,Tan, Zhulin,Xu, Jinghua,Kapadia, Suresh R.,Senanayake, Chris H.
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p. 4905 - 4907
(2007/10/03)
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- Synthesis of heteroarylamine intermediate compounds
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Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.
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- Synthesis of heteroarylamine intermediate compounds
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Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.
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- Novel synthesis of heteroarylamine intermediate compounds
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Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.
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