- Mycosamine orientation of amphotericin B controlling interaction with ergosterol: Sterol-dependent activity of conformation-restricted derivatives with an amino-carbonyl bridge
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Amphotericin B (AmB 1) is known to assemble together and form an ion channel across biomembranes. The antibiotic consists of mycosamine and macrolactone moieties, whose relative geometry is speculated to be determinant for the drug's channel activity and
- Matsumori, Nobuaki,Sawada, Yuri,Murata, Michio
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Read Online
- Novel BQCA- and TBPB-Derived M1 Receptor Hybrid Ligands: Orthosteric Carbachol Differentially Regulates Partial Agonism
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Recently, investigations of the complex mechanisms of allostery have led to a deeper understanding of G protein-coupled receptor (GPCR) activation and signaling processes. In this context, muscarinic acetylcholine receptors (mAChRs) are highly relevant due to their exemplary role in the study of allosteric modulation. In this work, we compare and discuss two sets of putatively dualsteric ligands, which were designed to connect carbachol to different types of allosteric ligands. We chose derivatives of TBPB [1-(1′-(2-tolyl)-1,4′-bipiperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one] as M1-selective putative bitopic ligands, and derivatives of benzyl quinolone carboxylic acid (BQCA) as an M1 positive allosteric modulator, varying the distance between the allosteric and orthosteric building blocks. Luciferase protein complementation assays demonstrated that linker length must be carefully chosen to yield either agonist or antagonist behavior. These findings may help to design biased signaling and/or different extents of efficacy.
- Schramm, Simon,Agnetta, Luca,Bermudez, Marcel,Gerwe, Hubert,Irmen, Matthias,Holze, Janine,Littmann, Timo,Wolber, Gerhard,Tr?nkle, Christian,Decker, Michael
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Read Online
- Amphiphilic dendrimer, synthesis method thereof, and application of amphiphilic dendrimer as drug delivery system
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The invention relates to a microenvironment response type amphiphilic dendrimer, a synthesis method thereof, and application of the microenvironment response type amphiphilic dendrimer as a drug delivery system. The microenvironment response type amphiphilic dendrimer is a compound with a structure as shown in a formula (I), a formula (II) or a formula (III) or pharmaceutically acceptable salt of the compound. The compound disclosed by the invention can be used as the nano delivery system based on tumor microenvironment specific response, has good solubility in an aqueous solution, can be self-assembled with a drug in the aqueous solution to form a relatively stable nano compound, can effectively deliver the loaded drug to a tumor site; and can responsively disassembl the nano-drug delivery carrier under corresponding stimulation to achieve the purpose of accurate drug release, so that the drug can be released to the focus part to the greatest extent, and the compound is a novel nano-delivery carrier.
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Paragraph 0096-0101
(2021/08/07)
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- An Intramolecular Iodine-Catalyzed C(sp3)?H Oxidation as a Versatile Tool for the Synthesis of Tetrahydrofurans
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The formation of ubiquitous occurring tetrahydrofuran patterns has been extensively investigated in the 1960s as it was one of the first examples of a non-directed remote C?H activation. These approaches suffer from the use of toxic transition metals in overstoichiometric amounts. An attractive metal-free solution for transforming carbon-hydrogen bonds into carbon-oxygen bonds lies in applying economically and ecologically favorable iodine reagents. The presented method involves an intertwined catalytic cycle of a radical chain reaction and an iodine(I/III) redox couple by selectively activating a remote C(sp3)?H bond under visible-light irradiation. The reaction proceeds under mild reaction conditions, is operationally simple and tolerates many functional groups giving fast and easy access to different substituted tetrahydrofurans.
- Br?se, Stefan,Koch, Vanessa
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supporting information
p. 3478 - 3483
(2021/07/22)
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- IRAK DEGRADERS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same.
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Paragraph 2529; 2530
(2019/07/10)
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- Controlling the self-assembly of cationic bolaamphiphiles: Counterion-directed transitions from 0D/1D to exclusively 2D planar structures
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Self-assembly of cationic bolaamphiphiles is usually reported to form one-dimensional (1D) or zero-dimensional (0D), rather than two-dimensional (2D) structures. Here we have found a facile counterion-directed structure switch for such amphiphilic moietie
- Wu, Guanglu,Verwilst, Peter,Liu, Kai,Smet, Mario,Faul, Charl F. J.,Zhang, Xi
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p. 4486 - 4493
(2013/11/19)
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- Elaboration of the ether cleaving ability and selectivity of the classical Pearlman's catalyst [Pd(OH)2/C]: Concise synthesis of a precursor for a myo-inositol pyrophosphate
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The cleavage of propargyl, allyl, benzyl, and PMB ethers by Pd(OH) 2/C can be tuned in that order, by varying the reaction conditions. Other moieties such as C-C double bonds, esters, trityl ether, p-bromo and p-nitrobenzyl ethers are stable to these reaction conditions. Cleavage of allyl ethers can be made catalytic by using 1:1 mixture of Pd(OH)2/C and Pd/C. The synthetic potential of the selective ether cleaving ability of Pd(OH)2/C, essentially under neutral conditions, has been demonstrated by an efficient synthesis of a precursor for the preparation of an inositol pyrophosphate derivative.
- Mart, Alson,Shashidhar, Mysore S.
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p. 9769 - 9776,8
(2012/12/11)
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- Elaboration of the ether cleaving ability and selectivity of the classical Pearlman's catalyst [Pd(OH)2/C]: Concise synthesis of a precursor for a myo-inositol pyrophosphate
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The cleavage of propargyl, allyl, benzyl, and PMB ethers by Pd(OH) 2/C can be tuned in that order, by varying the reaction conditions. Other moieties such as C-C double bonds, esters, trityl ether, p-bromo and p-nitrobenzyl ethers are stable to these reaction conditions. Cleavage of allyl ethers can be made catalytic by using 1:1 mixture of Pd(OH)2/C and Pd/C. The synthetic potential of the selective ether cleaving ability of Pd(OH)2/C, essentially under neutral conditions, has been demonstrated by an efficient synthesis of a precursor for the preparation of an inositol pyrophosphate derivative.
- Mart, Alson,Shashidhar, Mysore S.
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p. 9769 - 9776
(2013/01/13)
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- EPR spectroscopic characterization of local nanoscopic heterogeneities during the thermal collapse of thermoresponsive dendronized polymers
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(Figure Presented) The collapse transition of thermoresponsive dendronized polymers was characterized on a molecular scale by CW EPR spectroscopy. Aggregation of the polymer is triggered by dynamic structural inhomogeneities of a few nanometers, and the dehydration of the polymer chains proceeds, despite the sharp phase transition, over a temperature interval of at least 30°C (see picture).
- Junk, Matthias J. N.,Li, Wen,Schlueter, A.Dieter,Wegner, Gerhard,Spiess, Hans W.,Zhang, Afang,Hinderberger, Dariush
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supporting information; experimental part
p. 5683 - 5687
(2010/11/02)
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- Light-driven rotary molecular motors on gold nanoparticles
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We report the synthesis of unidirectional light-driven rotary molecular motors based on chiral overcrowded alkenes and their immobilisation on the surface of gold nanoparticles through two anchors. Using a combination of 1H and 13C N
- Pollard, Michael M.,Ter Wiel, Matthijs K. J.,Van Delden, Richard A.,Vicario, Javier,Koumura, Nagatoshi,Van Den Brom, Coenraad R.,Meetsma, Auke,Feringa, Ben L.
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supporting information; experimental part
p. 11610 - 11622
(2009/12/09)
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- SULFAMOYL-CONTAINING DERIVATIVES AND USES THEREOF
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Sulfamoyl-containing compounds are disclosed, having utility as inhibitors of disease-related targets, such as Heat Shock Protein 90 (HSP90), and which are useful for treating disorders, e.g., proliferative disorders, including HSP90-mediated disorders. Methods for preparing and using the disclosed compounds are also described.
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Page/Page column 23
(2008/06/13)
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- Ti(III) chloride: A novel reagent for the chemoselective deprotection of tetrahydropyranyl ethers
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Ti(III) chloride was found to be an effective catalyst for the deprotection of tetrahydropyranyl ethers of alcohols and phenols at an ambient temperature. Allyl ether, benzyl ether, tert-butyl-diphenylsilyl (TBDPS) ether, p-toluenesulfonate ester and isomerizable double bond were found to be compatible under the reaction conditions.
- Semwal, Abha,Nayak, Sandip K.
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- A facile route to the deprotection of sulfonate esters and sulfonamides with low valent titanium reagents
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A novel method for the cleavage of N/O-tosyl bonds by low-valent titanium is reported. TBDPS ether, THP ether, and olefin are found to be compatible under the reaction conditions.
- Nayak
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p. 1575 - 1578
(2007/10/03)
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