16173-52-7

• Article title
• Article abstract
• Author
• Journal number and time
• Download

• Mesogens based on cholesterol derivatives: Synthesis and characterization
• A new series of liquid crystals involving cholesterol based mesogenic units and Schiff base moiety interlinked through ester linkage were designed and synthesized. The target compounds were obtained by the reaction of 4-(3-cholesteryl oxy carbonyl)benzald
• Pandey, Ashwini,Singh, Bachcha

• p. 166 - 176

  (2012)
• Read Online

• Spontaneous formation of a chiral structure in an achiral banana-shaped molecular system
• We have synthesized a new banana-shaped compound, having naphthalene as a center of molecule. This compound exhibited an unconventional smectic texture by optical microscopy where the growth of small-fractal domains was observed. Moreover, two different chiral domains were found to form in the smectic phase as well as in the Smblue phase which can be considered to possess a helical structure. The details will be discussed.
• Thisayukta, Jirakorn,Kamee, Hiroyuki,Kawauchi, Susumu,Watanabe, Junji

• p. 63 - 75

  (2000)
• Read Online

• Synthetic and structural study on some new porphyrin or metalloporphyrin macrocycle-containing model complexes for the active site of [FeFe]-hydrogenases
• To mimick the natural enzymes [FeFe]-hydrogenases, some new porphyrin and metalloporphyrin moiety-containing model complexes, namely 5-[p-Fe 2(CO)6(μ-SCH2)2CHO 2CC6H4],10,15,20-t
• Song, Li-Cheng,Wang, Liang-Xing,Li, Chang-Gong,Li, Fengyu,Chen, Zhongfang

• p. 120 - 128

  (2014)
• Read Online

• Sequestering ability to Cu2?+ of a new bodipy-based dye and its behavior as in vitro fluorescent sensor
• A Bodipy (4,4-difluoro-4-bora-3a,4a-diaza-s-indacene) derivative has been conceived and synthesized starting from L-aspartic acid, as a selective turn-off sensor of Cu2?+ ions. Its acid–base properties were determined to study the formation of
• Papalia, Teresa,Barattucci, Anna,Barreca, Davide,Bellocco, Ersilia,Bonaccorsi, Paola,Minuti, Lucio,Nicolò, Marco Sebastiano,Temperini, Andrea,Foti, Claudia

• p. 116 - 123

  (2017)
• Read Online

• Scale-up of the synthesis of a pyrimidine derivative directly on solid support
• The solid-phase synthesis of 4-(2-amino-6-phenylpyrimidin-4-yl)benzamide, a compound obtained through combinatorial chemistry and parallel synthesis, can be scaled up directly on solid support in excellent yields and high purity. By applying highly loaded aminomethyl polystyrene as solid support, a good ratio between the product and the starting resin is achieved. For comparison, the synthesis was also performed in solution. The solid-phase synthesis approach has the advantage that the desired compound is easily and quickly accessible in sufficient quantities for early development demands.
• Meisenbach, Mark,Allmendinger, Thomas,Mak, Ching-Pong

• p. 553 - 558

  (2003)
• Read Online

• BODIPY derivatives bearing borneol moieties: Enhancing cell membrane permeability for living cell imaging
• Three novel boron-dipyrromethene (BODIPY) dyes bearing borneol moieties have been designed, synthesized and characterized. The single-crystal structure of the compound 3 was also elucidated for the first time. Their photophysical properties and confocal f
• Yang, Jian,Fan, Yunshi,Cai, Fangjian,Xu, Xu,Fu, Bo,Wang, Shifa,Shen, Zhen,Tian, Jiangwei,Xu, Haijun

• p. 105 - 111

  (2019)
• Read Online

• Distinct formation of a chiral smectic phase in achiral banana-shaped molecules with a central core based on a 2,7-dihydroxynaphthalene unit
• We have prepared a novel series of banana-shaped molecules with a central bent core based on a 2,7-dihydroxynaphthalene group, the side wings containing a Schiff's based moiety, and alkoxy flexible tails with carbon numbers n = 6, 8, 10, 12, 14, and 16. Among these, the molecules with n = 8-16 formed a novel smectic phase. Its smectic layer possessed a liquidlike association of the molecules similar to the SmA or SmC phase, although the texture that developed from the isotropic melt was unconventional. Small fractal domains initially grew and then coalesced into several large domains. Very weak birefringence and fine structure without any anisotropy are characteristic of this phase. It is interesting to note that two different domains exist showing the opposite sign of optical rotation. Strong circular dichroism (CD) with a peak at 430 nm was also observed for each domain with the opposite sign. The results suggest a natural occurrence of the helix in these materials. The right-handed and left-handed helices were formed with equal probabilities, but the left-handed helix was selectively formed by the introduction of a chiral dopant. The molecule with n = 6 formed a frustrated smectic phase, which exhibited a simple fan-shaped texture.
• Thisayukta, Jirakorn,Nakayama, Yusuke,Kawauchi, Susumu,Takezoe, Hideo,Watanabe, Junji

• p. 7441 - 7448

  (2000)
• Read Online

• Bisulfite addition reaction as the basis for a hydrogensulfite bulk optode
• The reversible addition of hydrogensulfite to benzaldehydes was employed as the basic reaction type for the construction of a new kind of hydrogensulfite sensor. The membrane of the sensor consists of plasticized PVC, electrically neutral, lipophilized be
• Kuratli, Matthias,Badertscher, Martin,Rusterholz, Bruno,Simon, Wilhelm

• p. 3473 - 3479

  (1993)
• Read Online

• Prato reaction derived polythiophene/C60donor-acceptor double cable polymer, fabrication of photodetectors and evaluation of photocurrent generation
• Herein, a side chain engineered polythiophene copolymer based organic semiconductor polymer (OSP) with pendant aldehyde groups was synthesized by a combination of Grignard Metathesis (GRIM) polymerization and post-synthetic modifications. The pendant alde
• Iftikhar, Sunniya,Aslam, Saba,Butt, Nauman Zafar,Ashraf, Raja Shahid,Yameen, Basit

• p. 17365 - 17373

  (2020)
• Read Online

• A Synthetic Replicator Drives a Propagating Reaction-Diffusion Front
• A simple synthetic autocatalytic replicator is capable of establishing and driving the propagation of a reaction-diffusion front within a 50 μL syringe. This replicator templates its own synthesis through a 1,3-dipolar cycloaddition reaction between a nit
• Bottero, Ilaria,Huck, Jürgen,Kosikova, Tamara,Philp, Douglas

• p. 6723 - 6726

  (2016)
• Read Online

• Catalytic hydroamination of unactivated olefins using a Co catalyst for complex molecule synthesis
• Functional group tolerance is one of the important requirements for chemical reactions, especially for the synthesis of complex molecules. Herein, we report a mild, general, and functional group tolerant intramolecular hydroamination of unactivated olefins using a Co(salen) complex, an N-fluoropyridinium salt, and a disiloxane reagent. This method, which was carried out at room temperature (or 0 °C), afforded three-, five-, six-, and seven-membered ring nitrogen-containing heterocyclic compounds and was compatible with diverse functional groups.
• Shigehisa, Hiroki,Koseki, Natsumi,Shimizu, Nao,Fujisawa, Mayu,Niitsu, Makoto,Hiroya, Kou

• p. 13534 - 13537

  (2014)
• Read Online

• A Molecular Replication Process Drives Supramolecular Polymerization
• Supramolecular polymers are materials in which the connections between monomers in the polymer main chain are non-covalent bonds. This area has seen rapid expansion in the last two decades and has been exploited in several applications. However, suitable
• Feng, Yuanning,Philp, Douglas
• supporting information

  p. 17029 - 17039

  (2021/10/25)
• 

• C2 symmetric borneol-porphyrin hybrids: Synthesis, characterization, electronic structure and their anti-cancer behaviors
• A series of five C2 Symmetric A2B2 type borneol-porphyrin hybrids have been synthesized and characterized. Moreover, a detailed analysis of their optical and redox properties was carried out by comparing the results obtained via optical spectroscopy and electrochemistry. The current results demonstrated that the meso borneol-substitutions excitation coupled strongly with porphyrin core that leads to significant CD signals in the Soret band region, and molecular anti-cancer behaviors were also investigated.
• Dong, Xinyi,Fang, Xianying,Fu, Bo,Liang, Xu,Xu, Haijun,Yu, Xiaoxiao,Zhang, Zhen,Zhu, Weihua

• (2020/09/17)
• 

• Nickel-Catalyzed Carboalkenylation of 1,3-Dienes with Aldehydes and Alkenylzirconium Reagents: Access to Skipped Dienes
• A regio- and stereoselective nickel-catalyzed three-component coupling reaction of aldehydes, 1,3-dienes, and alkenylzirconium reagents was realized. The ligand- and additive-free protocol afforded a convenient approach to the synthesis of skipped diene compounds bearing various functionals (e.g., hydroxyl, carbonyl, halide) and heterocyclic groups. The products were readily transformed into structurally diverse polyenes. The utility of this reaction was also demonstrated by the one-pot operation and scale-up preparation.
• Wang, Cheng-Gang,Zhang, Yunxing,Wang, Simin,Chen, Bin,Li, Yang,Ni, Hai-Liang,Gao, Yuanji,Hu, Ping,Wang, Bi-Qin,Cao, Peng
• supporting information

  p. 535 - 541

  (2021/01/26)
• 

• Discovery of N-(3,4-Dimethylphenyl)-4-(4-isobutyrylphenyl)-2,3,3a,4,5,9b-hexahydrofuro[3,2- c]quinoline-8-sulfonamide as a Potent Dual MDM2/XIAP Inhibitor
• Murine double minute 2 (MDM2) and X-linked inhibitor of apoptosis protein (XIAP) are important cell survival proteins in tumor cells. As a dual MDM2/XIAP inhibitor reported previously, compound MX69 has low potency with an IC50 value of 7.5 μM against an acute lymphoblastic leukemia cell line EU-1. Herein, we report the structural optimization based on the MX69 scaffold, leading to the discovery of a 25-fold more potent analogue 14 (IC50 = 0.3 μM against EU-1). We demonstrate that 14 maintains its mode of action by dual targeting of MDM2 and XIAP through inducing MDM2 protein degradation and inhibiting XIAP mRNA translation, respectively, which resulted in cancer cell growth inhibition and cell death. The results strongly suggest that the scaffold based on 14 is promising for further optimization to develop a new therapeutic agent for leukemia and possibly other cancers where MDM2 and XIAP are dysregulated.
• Wu, Zhongzhi,Gu, Lubing,Zhang, Sicheng,Liu, Tao,Lukka, Pradeep B.,Meibohm, Bernd,Bollinger, John C.,Zhou, Muxiang,Li, Wei

• p. 1930 - 1950

  (2021/03/01)
• 

• COMPOUNDS AND METHODS OF USE
• This present disclosure relates to compounds with ferroptosis inducing activity, a method of treating a subject with cancer with the compounds, and combination treatments with a second therapeutic agent.
• -
• Page/Page column 82; 83

  (2021/03/05)
• 

• Preparation methods of revefenacin intermediate and revefenacin
• The invention relates to a synthesis method of a revefenacin intermediate, which specifically comprises the following steps: in a solvent, enabling piperidin-4-yl [1,1-biphenyl]-2-carbamate to react with methyl(2-oxyethyl) tert-butyl carbamate in the pres
• -
• Paragraph 0060-0065

  (2021/05/26)
• 

• NO Donor compound as well as preparation method and application thereof
• The invention discloses NO donor compounds and a preparation method and application thereof, wherein the compound is a drug active component formed by splicing 5 - monoisosorbide mononitrate and NIT type nitroxide radicals, and the structure is shown I. A
• -
• Paragraph 0090; 0091

  (2021/11/26)
• 

• (E)-4-(pyridine formylhydrazino)-N-phenylbenzamide anti-tumor compounds
• The invention belongs to the technical field of medicines, and relates to a compound with antitumor activity and a specific chemical structure, in particular to (E)-4-(pyridine formylhydrazino)-N-phenylbenzamide antitumor compounds and a preparation metho
• -
• Paragraph 0049-0051

  (2020/05/30)
• 

• Design, synthesis and biological evaluation of novel (E)-N-phenyl-4-(pyridine-acylhydrazone) benzamide derivatives as potential antitumor agents for the treatment of multiple myeloma (MM)
• A series of novel (E)-N-phenyl-4-(pyridine-acylhydrazone) benzamide derivatives were designed, synthesized, and evaluated for their anti-proliferative activity against two different human cancer cell lines and one human normal cell line. Compound 8b had t
• Li, Xin-yang,Li, Shuai,Lu, Guo-qing,Wang, De-pu,Liu, Kai-li,Qian, Xin-hua,Xue, Wen-han,Meng, Fan-hao

• (2020/09/04)
• 

• Pesticide for cucumbers and control method of cucumber pests (by machine translation)
• The invention relates to the technical field of plant insecticides, and particularly discloses a pesticide and a control method for cucumber pests. The main active ingredient of the insecticide is shown in formula (1). Oxazoline-substituted benzamide comp
• -
• Paragraph 0090-0094

  (2020/12/02)
• 

• Chalcone derivative, preparation method and application thereof in medicine
• The invention relates to a chalcone derivative, its preparation method and an application of the chalcone derivative in medicine, specifically to a chalcone derivative as shown in the general formula (I), its preparation method, a pharmaceutical compositi
• -
• Paragraph 0099-0101

  (2019/07/24)
• 

• COMPOUNDS AND METHOD OF USE
• This present disclosure relates to compounds with ferroptosis inducing activity, a method of treating a subject with cancer with the compounds, and combination treatments with a second therapeutic agent.
• -
• Paragraph 0975

  (2019/09/06)
• 

• Metathesis-active ligands enable a catalytic functional group metathesis between aroyl chlorides and aryl iodides
• Current methods for functional group interconversion have, for the most part, relied on relatively strong driving forces which often require highly reactive reagents to generate irreversibly a desired product in high yield and selectivity. These approaches generally prevent the use of the same catalytic strategy to perform the reverse reaction. Here we describe a catalytic functional group metathesis approach to interconvert, under CO-free conditions, two synthetically important classes of electrophiles that are often employed in the preparation of pharmaceuticals and agrochemicals—aroyl chlorides (ArCOCl) and aryl iodides (ArI). Our reaction design relies on the implementation of a key reversible ligand C–P bond cleavage event, which enables a non-innocent, metathesis-active phosphine ligand to mediate a rapid aryl group transfer between the two different electrophiles. Beyond enabling a practical and safer approach to the interconversion of ArCOCl and ArI, this type of ligand non-innocence provides a blueprint for the development of a broad range of functional group metathesis reactions employing synthetically relevant aryl electrophiles.
• Lee, Yong Ho,Morandi, Bill

• p. 1016 - 1022

  (2018/09/06)
• 

• Tecarfarin preparation method
• The invention provides a new Tecarfarin preparation method, which comprises: carrying out acyl chlorination on 4-carboxybenzaldehyde, carrying out condensation with 1,1,1,3,3,3-hexafluoro-2-methylpropan-2-ol to form an ester, and carrying out a reaction o
• -
• Paragraph 0029; 0030; 0031

  (2018/10/26)
• 

• Functional Group Transposition: A Palladium-Catalyzed Metathesis of Ar-X σ-Bonds and Acid Chloride Synthesis
• We describe the development of a new method to use palladium catalysis to form functionalized aromatics: via the metathesis of covalent σ-bonds between Ar-X fragments. This transformation demonstrates the dynamic nature of palladium-based oxidative addition/reductive elimination and offers a straightforward approach to incorporate reactive functional groups into aryl halides through exchange reactions. The reaction has been exploited to assemble acid chlorides without the use of high energy halogenating or toxic reagents and, instead, via the metathesis of aryl iodides with other acid chlorides.
• De La Higuera Macias, Maximiliano,Arndtsen, Bruce A.
• supporting information

  p. 10140 - 10144

  (2018/08/23)
• 

• GLUCOCORTICOID RECEPTOR AGONIST AND IMMUNOCONJUGATES THEREOF
• Provided herein are glucocorticoid receptor agonist immunoconjugates, glucocorticoid receptor agonists, and methods of using the same, e.g., to treat autoimmune or inflammatory diseases.
• -
• Paragraph 001106; 001107

  (2018/01/17)
• 

• Silylated Imine And Carbamate Polymeric Benzoate Compounds, Uses, And Compositions Thereof
• The present invention relates to organosilicon polymers containing benzoic acid esters in form of particles, process for their preparation, cosmetic or dermatological composition comprising them, as well as their use for protecting a human or animal livin
• -
• Paragraph 0212; 0220; 0228; 0236; 0242; 00248

  (2017/04/18)
• 

• Irreversible Cysteine-Selective Protein Labeling Employing Modular Electrophilic Tetrafluoroethylation Reagents
• Fluoroalkylation reagents based on hypervalent iodine are widely used to transfer fluoroalkyl moieties to various nucleophiles. However, the transferred groups have so far been limited to simple structural motifs. We herein report a reagent featuring a secondary amine that can be converted to amide, sulfonamide, and tertiary amine derivatives in one step. The resulting reagents bear manifold functional groups, many of which would not be compatible with the original synthetic pathway. Exploiting this structural versatility and the known high reactivity toward thiols, the new-generation reagents were used in bioconjugation with an artificial retro-aldolase, containing an exposed cysteine and a reactive catalytic lysine. Whereas commercial reagents based on maleimide and iodoacetamide labeled both sites, the iodanes exclusively modified the cysteine residue. The study thus demonstrates that modular fluoroalkylation reagents can be used as tools for cysteine-selective bioconjugation.
• Václavík, Ji?í,Zschoche, Reinhard,Klimánková, Iveta,Matou?ek, Václav,Beier, Petr,Hilvert, Donald,Togni, Antonio
• supporting information

  p. 6490 - 6494

  (2017/05/15)
• 

• BICYCLIC HYDROXAMIC ACIDS USEFUL AS INHIBITORS OF MAMMALIAN HISTONE DEACETYLASE ACTIVITY
• A compound of formula (Ia) or (Ib) or a pharmaceutically acceptable salt thereof. The compound is an inhibitor of a histone deacetylase, and as such is useful in terepy, e.g. in the treatment of autoimmune disorders, mental disorders, neurodegenerative disorders, and hyperproliferative disorders.
• -
• Page/Page column 125; 126

  (2017/07/14)
• 

• Merging gold catalysis, organocatalytic oxidation, and Lewis acid catalysis for chemodivergent synthesis of functionalized oxazoles from: N -propargylamides
• Novel catalytic systems consisting of cationic gold complexes, N-hydroxyphthalimide (NHPI), and transition-metal-based Lewis acids have been developed for the one-pot synthesis of functionalized oxazoles from N-propargylamides with excellent functional group tolerance. These transformations demonstrated the excellent compatibility of homogeneous gold catalysis with organocatalytic oxidative carbon-nitrogen bond formations using tert-butyl nitrite as the terminal oxidant. Moreover, oxazolecarbonitriles or carboxamides can be easily synthesized in a one-pot protocol according to the different synthetic requirements.
• Mai, Shaoyu,Rao, Changqing,Chen, Ming,Su, Jihu,Du, Jiangfeng,Song, Qiuling
• supporting information

  p. 10366 - 10369

  (2017/09/25)
• 

• NOVEL CLOSTRIDIUM DIFFICILE TOXIN INHIBITORS
• The present invention relates to benzodiazepine derivative compounds of formula (I), or pharmaceutically acceptable salts thereof. The present benzodiazepine compounds are useful Clostridium difficile inhibitors in the treatment of Clostridium difficile infection in humans. The present invention provides a pharmaceutical composition containing benzodiazepine compounds of formula (I) and a method of making as well as a method of using the same in treating patients infected with Clostridium difficile infection by administering the same. The compounds of the present invention may be used in combination with additional antibiotics or anti-toxin antibody drugs.
• -
• Page/Page column 89

  (2018/01/17)
• 

• Probing the Limits of Selectivity in a Recognition-Mediated Reaction Network Embedded within a Dynamic Covalent Library
• Two recognition-mediated reaction processes operating through reactive binary complexes drive resolution of a 24-component dynamic covalent library, assembled from individual aldehydes and nucleophiles. The effectiveness of the library resolution and sele
• Kosikova, Tamara,MacKenzie, Harry,Philp, Douglas
• supporting information

  p. 1831 - 1839

  (2016/02/20)
• 

• Transition-Metal-Free Synthesis of N-Aryl Hydroxamic Acids via Insertion of Arynes
• An efficient and transition-metal-free N-arylation of amides via the insertion of arynes into the N-H bonds in the N-alkoxy amides is described. A variety of the reactive functional groups including the reactive aldehyde carbonyl group, furan ring, carbon-carbon double bonds, and free N-H bond of indole are found to be compatible with this process. In particular, the protocol is applicable in the synthesis of structurally diverse N-aryl hydroxamates and hydroxamic acids derived from N-protecting amino acids and peptides. In the presence of multiple amide N-H bonds, the N-arylation reaction can proceed selectively in the N-H bonds of terminal N-OBn amides giving rise to the desired N-aryl hydroxamates.
• Zhang, Lanlan,Geng, Yu,Jin, Zhong

• p. 3542 - 3552

  (2016/05/24)
• 

• Novel benzamide-based histamine H3 receptor antagonists: The identification of two candidates for clinical development
• The preclinical characterization of novel phenyl(piperazin-1-yl)methanones that are histamine H3 receptor antagonists is described. The compounds described are high affinity histamine H3 antagonists. Optimization of the physical properties of these histamine H3 antagonists led to the discovery of several promising lead compounds, and extensive preclinical profiling aided in the identification of compounds with optimal duration of action for wake promoting activity. This led to the discovery of two development candidates for Phase I and Phase II clinical trials.
• Letavic, Michael A.,Aluisio, Leah,Apodaca, Richard,Bajpai, Manoj,Barbier, Ann J.,Bonneville, Anne,Bonaventure, Pascal,Carruthers, Nicholas I.,Dugovic, Christine,Fraser, Ian C.,Kramer, Michelle L.,Lord, Brian,Lovenberg, Timothy W.,Li, Lilian Y.,Ly, Kiev S.,McAllister, Heather,Mani, Neelakandha S.,Morton, Kirsten L.,Ndifor, Anthony,Nepomuceno, S. Diane,Pandit, Chennagiri R.,Sands, Steven B.,Shah, Chandra R.,Shelton, Jonathan E.,Snook, Sandra S.,Swanson, Devin M.,Xiao, Wei

• p. 450 - 454

  (2015/04/27)
• 

• Acid Chloride Synthesis by the Palladium-Catalyzed Chlorocarbonylation of Aryl Bromides
• We report a palladium-catalyzed method to synthesize acid chlorides by the chlorocarbonylation of aryl bromides. Mechanistic studies suggest the combination of sterically encumbered PtBu3 and CO coordination to palladium can rapidly equilibrate the oxidative addition/reductive elimination of carbon-halogen bonds. This provides a useful method to assemble highly reactive acid chlorides from stable and available reagents, and can be coupled with subsequent nucleophilic reactions to generate new classes of carbonylated products. The Good, the Bad and the Bulky! By employing a sterically encumbered phosphine ligand, tri-tert-butyl phosphine, under palladium catalysis inert aryl bromides are chlorocarbonylated to create reactive acid chlorides by reversible carbon-halogen bond reductive elimination. This general platform allows for an expanded scope of the Heck carbonylation reaction to include previously incompatible nucleophiles.
• Quesnel, Jeffrey S.,Kayser, Laure V.,Fabrikant, Alexander,Arndtsen, Bruce A.
• supporting information

  p. 9550 - 9555

  (2015/06/30)
• 

• Metal-free trifluoromethylation of aromatic and heteroaromatic aldehydes and ketones
• The ability to convert simple and common substrates into fluoroalkyl derivatives under mild conditions remains an important goal for medicinal and agricultural chemists. One representative example of a desirable transformation involves the conversion of aromatic and heteroaromatic ketones and aldehydes into aryl and heteroaryl β,β,β-trifluoroethylarenes and -heteroarenes. The traditional approach for this net transformation involves stoichiometric metals and/or multistep reaction sequences that consume excessive time, material, and labor resources while providing low yields of products. To complement these traditional strategies, we report a one-pot metal-free decarboxylative procedure for accessing β,β,β- trifluoroethylarenes and -heteroarenes from readily available ketones and aldehydes. This method features several benefits, including ease of operation, readily available reagents, mild reaction conditions, high functional-group compatibility, and scalability.
• Qiao, Yupu,Si, Tuda,Yang, Ming-Hsiu,Altman, Ryan A.

• p. 7122 - 7131

  (2014/08/18)
• 

• Degradable hybrid materials based on cationic acylhydrazone dynamic covalent polymers promote dna complexation through multivalent interactions
• The design of smart nonviral vectors for gene delivery is of prime importance for the successful implementation of gene therapies. In particular, degradable analogues of macromolecules represent promising targets as they would combine the multivalent pres
• Bouillon, Camille,Paolantoni, Delphine,Rote, Jennifer C.,Bessin, Yannick,Peterson, Larryn W.,Dumy, Pascal,Ulrich, Sbastien

• p. 14705 - 14714

  (2015/03/18)
• 

• Benzothiazinones: A novel class of adenosine receptor antagonists structurally unrelated to xanthine and adenine derivatives
• 2-(Acyl)amino-4H-3,1-benzothiazin-4-ones and related thienothiazinones were identified as structurally novel antagonists at adenosine receptors (ARs). 6-Methyl-2-benzoylamino-4H-3,1-benzothiazin-4-one (10d) was found to be a balanced AR antagonist with affinity for all human (h) subtypes (Ki hA1 65.6 nM; hA2A 120 nM; hA2B 360 nM; hA 3 30.4 nM), while in rat (r), 10d was a highly potent A 1-selective antagonist (rA1 7.7 nM; rA2A 546 nM; rA2B 679 nM, rA3 >10000 nM). 2-(4- Methylbenzoylamino)-4H-3,1-benzothiazin-4-one (10g) was found to be a potent antagonist at human A2A (68.8 nM) and A3 ARs (23.0 nM) with high selectivity versus the other human AR subtypes. In contrast to A 1 and A3 ARs, A2A and A2B ARs tolerated bulky 2-acyl substituents. tert-Butyl (4-oxo-4H-3,1-benzothiazin-2- ylcarbamoyl)benzylcarbamate (15g, Ki hA2B 186 nM; hA 2A 603 nM) and 4-(4-benzylpiperazine-1-carbonyl)-N-(4-oxo-4H-3,1- benzothiazin-2-yl)benzamide (15k, hA2A 69.5 nM; hA2B 178 nM) were highly selective versus the other AR subtypes. 2-Acylamino-3,1- benzothiazin-4-ones represent novel scaffolds suitable for the development of potent and selective AR antagonists for each of the four receptor subtypes.
• Gütschow, Michael,Schlenk, Miriam,G?b, Jürgen,Paskaleva, Minka,Alnouri, Mohamad Wessam,Scolari, Silvia,Iqbal, Jamshed,Müller, Christa E.
• supporting information; experimental part

  p. 3331 - 3341

  (2012/06/04)
• 

• A small molecule sensor for fluoride based on an autoinductive, colorimetric signal amplification reaction
• This article describes a small molecule reagent that is capable of detecting fluoride down to 0.12 mM (2.3 ppm) in water. The reagent reveals this level of fluoride through a novel autoinductive signal amplification reaction that produces an unambiguous colorimetric readout.
• Baker, Matthew S.,Phillips, Scott T.
• supporting information; experimental part

  p. 3595 - 3599

  (2012/06/18)
• 

• Acid-responsive organogel mediated by arene-perfluoroarene and hydrogen bonding interactions
• A phenyl and a 2,3,5,6-tetrafluorophenyl ring, each bearing a tris(n-dodecyloxy)benzylamine moiety via an amide bond, were tethered together through an imine linkage to give a non-covalent synthon (imine 1) with a strong capacity of supramolecular self-as
• Wu, Huixian,Ni, Ben-Bo,Wang, Chong,Zhai, Feng,Ma, Yuguo
• experimental part

  p. 5486 - 5492

  (2012/08/14)
• 

• Structure-based design of novel boronic acid-based inhibitors of autotaxin
• Autotaxin (ATX) is a secreted phosphodiesterase that hydrolyzes the abundant phospholipid lysophosphatidylcholine (LPC) to produce lysophosphatidic acid (LPA). The ATX-LPA signaling axis has been implicated in inflammation, fibrosis, and tumor progression
• Albers, Harald M. H. G.,Hendrickx, Loes J. D.,Van Tol, Rob J. P.,Hausmann, Jens,Perrakis, Anastassis,Ovaa, Huib
• supporting information; experimental part

  p. 4619 - 4626

  (2011/09/14)
• 

• The chiral pool as valuable natural source: New chiral mesogens made from lactic acid
• Twenty new enantiopure chiral materials have been synthesized, showing liquid crystalline phases of smectic (SmA*), twisted grain boundary (TGB) and cholesteric (N*) type. The central ester-linkage as well as the length of the attached alkyl-chains were varied in a systematic way and the effects of these structural changes on the liquid crystalline properties have been studied. The liquid crystalline phases were characterized by means of differential scanning calorimetry, polarisation microscopy as well as small angle X-ray diffraction (SAXS). Copyright Taylor & Francis Group, LLC.
• Brombach,Neudoerfl,Blunk
• body text

  p. 62 - 74

  (2012/01/06)
• 

• Synthesis and mesogenic property of new bent-core molecules with semifluorinated alkanes
• -
• Choi, E-Joon,Sim, Hoo-Sik,Chien, Liang-Chy,Lee, Soo-Min
• scheme or table

  p. 725 - 727

  (2012/01/12)
• 

• Anhydrotetracycline-peptide conjugates as representatives for ligand-based transactivating systems
• Bioconjugates of anhydrotetracycline and minimal activation sequences (VP1, VP2) derived from the Herpes simplex virus protein VP16 were synthesized. Different ligation strategies were applied and the resulting molecules tested in HeLa cells expressing the reverse transactivator rtTA-S3 for activity. The data clearly demonstrate that the atc-peptide conjugates are able to penetrate the cell membrane. Furthermore, binding to and induction of rtTA-S3 were detected. Structure-activity relationships indicated that the biological activity of the atc-peptide strongly depends on the specific linker used. The N-terminally linked oxime derivative 10 proved excellent activity when the increase of luciferace activity indicated a transcriptional activation substantially exceeding the inducing properties of anhydrotetracycline.
• Lochner, Susanne,Einsiedel, Juergen,Schaefer, Gesa,Berens, Christian,Hillen, Wolfgang,Gmeiner, Peter
• experimental part

  p. 6127 - 6133

  (2010/09/18)
• 

• Controlled and chemoselective reduction of secondary amides
• This communication describes a metal-free methodology involving an efficient and controlled reduction of secondary amides to imines, aldehydes, and amines in good to excellent yields under ambient pressure and temperature. The process includes a chemoselective activation of a secondary amide with triflic anhydride in the presence of 2-fluoropyridine. The electrophilic activated amide can then be reduced to the corresponding iminium using triethylsilane, a cheap, rather inert, and commercially available reagent. Imines can be isolated after a basic workup or readily transformed to the aldehydes following an acidic workup. The amine moiety can be accessed via a sequential reductive amination by the addition of silane and Hantzsch ester hydride in a one-pot reaction. Moreover, this reduction tolerates various functional groups that are usually reactive under reductive conditions and is very selective to secondary amides.
• Pelletier, Guillaume,Bechara, William S.,Charette, Andre B.
• supporting information; experimental part

  p. 12817 - 12819

  (2010/11/05)
• 

• METHOD FOR CONVERTING AROMATIC ALDEHYDES TO AROMATIC ACYL HALIDES
• The invention relates to a method for converting an aromatic aldehyde or a mixture of aromatic aldehydes to a reaction product which is an aromatic acyl halide or a mixture of aromatic acyl halides in a reaction medium which is free from xylene, comprising bringing the aromatic aldehyde or mixture of aromatic aldehydes in contact with a halogen to obtain the reaction product, wherein the reaction medium optionally comprises a co-solvent selected from the group consisting of any aromatic acyl halide and mixtures thereof. Particularly, the aromatic aldehyde is terephthaldehyde, the aromatic acyl halide is terephthaloyldichloride, and the halogen is chlorine.
• -
• Page/Page column 7

  (2010/10/03)
• 

• Amide analogs of antifungal dioxane-triazole derivatives: Synthesis and in vitro activities
• A new series of triazole compounds possessing an amide-part were efficiently synthesized and their in vitro antifungal activities were investigated. The amide analogs showed excellent in vitro activity against Candida, Cryptococcus and Aspergillus species
• Uchida, Takuya,Kagoshima, Yoshiko,Konosu, Toshiyuki
• scheme or table

  p. 2013 - 2017

  (2009/11/30)
• 

• Effect of alkylthio tail on phase behaviors of bent-shaped molecules based on naphthalene core
• New bent-shaped molecules with naphthalene central core and alkylthio tail are prepared, and their banana phase structures and properties are discussed in comparison with those of conventional alkoxy molecules. Copyright
• Li, Xiaodong,Lee, Seng Kue,Kang, Sungmin,Tokita, Masatoshi,Kawauchi, Susumu,Watanabe, Junji
• supporting information; scheme or table

  p. 424 - 425

  (2010/03/04)
• 

• Development of 2,6-carboxy-substituted boron dipyrromethene (BODIPY) as a novel scaffold of ratiometric fluorescent probes for live cell imaging
• Ratiometric fluorescent probes based on boron dipyrromethene (BODIPY) were developed based on a novel design strategy, in which a change of the electron-withdrawing character of the 2,6-substituents resulting from reaction with a target molecule generates a fluorescence wavelength change. The Royal Society of Chemistry 2009.
• Komatsu, Toru,Urano, Yasuteru,Fujikawa, Yuuta,Kobayashi, Tomonori,Kojima, Hirotatsu,Terai, Takuya,Hanaoka, Kenjiro,Nagano, Tetsuo
• supporting information; experimental part

  p. 7015 - 7017

  (2010/04/25)
• 

• SUBSTITUTED BENZAMIDE MODULATORS OF THE HISTAMINE H3 RECEPTOR
• Certain substituted benzamide compounds are histamine H3receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
• -
• Page/Page column 23; 27-28; 32; 35-36; 39-40; 42

  (2008/06/13)
• 

• Modulators of calcitonin and amylin receptor activity
• In various aspects, the present invention relates to non-peptidic compounds, which modulate calcitonin and amylin receptor activity; to processes for the preparation of some such compounds; and to pharmaceutical compositions including such compounds. Compounds of the invention are useful as calcitonin and/or amylin agonists and in the treatment of bone diseases and metabolic diseases.
• -
• Page/Page column 24

  (2008/12/06)
• 

• Discovery of brain penetrant, soluble, pyrazole amide EP1 receptor antagonists
• We describe the discovery of a series of pyrazole amide EP1 receptor antagonists with good aqueous solubility and CNS penetration. In order to achieve solubility we investigated the incorporation of a basic group in the region of the molecule p
• Hall, Adrian,Billinton, Andy,Bristow, Alan K.,Brown, Susan H.,Chowdhury, Anita,Cutler, Leanne,Giblin, Gerard M.P.,Goldsmith, Paul,Hayhow, Thomas G.,Kilford, Ian R.,Naylor, Alan,Passingham, Barry,Rawlings, D. Anthony
• scheme or table

  p. 4027 - 4032

  (2009/04/10)
• 

• CYCLOPROPYL AMINES AS MODULATORS OF THE HISTAMINE H3 RECEPTOR
• Certain cyclopropyl amines are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases.
• -
• Page/Page column 8; 9

  (2010/11/26)
•