66628-99-7Relevant academic research and scientific papers
Bioinspired Design Provides High-Strength Benzoxazine Structural Adhesives
Higginson, Cody J.,Malollari, Katerina G.,Xu, Yunqi,Kelleghan, Andrew V.,Ricapito, Nicole G.,Messersmith, Phillip B.
supporting information, p. 12271 - 12279 (2019/08/01)
A synthetic strategy to incorporate catechol functional groups into benzoxazine thermoset monomers was developed, leading to a family of bioinspired small-molecule resins and main-chain polybenzoxazines derived from biologically available phenols. Lap-she
Revisiting Arene C(sp2)?H Amidation by Intramolecular Transfer of Iridium Nitrenoids: Evidence for a Spirocyclization Pathway
Hwang, Yeongyu,Park, Yoonsu,Kim, Yeong Bum,Kim, Dongwook,Chang, Sukbok
supporting information, p. 13565 - 13569 (2018/09/25)
Two mechanistic pathways, that is, electrocyclization and electrophilic aromatic substitution, are operative in most intramolecular C?H amination reactions proceeding by metal nitrenoid catalysis. Reported here is an alternative mechanistic scaffold leading to benzofused δ-lactams selectively. Integrated experimental and computational analysis revealed that the reaction proceeds by a key spirocyclization step followed by a skeletal rearrangement. Based on this mechanistic insight, a new synthetic route to spirolactams has been developed.
1,2,4-Triazole-3-thione Compounds as Inhibitors of Dizinc Metallo-β-lactamases
Sevaille, Laurent,Gavara, Laurent,Bebrone, Carine,De Luca, Filomena,Nauton, Lionel,Achard, Maud,Mercuri, Paola,Tanfoni, Silvia,Borgianni, Luisa,Guyon, Carole,Lonjon, Pauline,Turan-Zitouni, Gülhan,Dzieciolowski, Julia,Becker, Katja,Bénard, Lionel,Condon, Ciaran,Maillard, Ludovic,Martinez, Jean,Frère, Jean-Marie,Dideberg, Otto,Galleni, Moreno,Docquier, Jean-Denis,Hernandez, Jean-Fran?ois
, p. 972 - 985 (2017/06/27)
Metallo-β-lactamases (MBLs) cause resistance of Gram-negative bacteria to β-lactam antibiotics and are of serious concern, because they can inactivate the last-resort carbapenems and because MBL inhibitors of clinical value are still lacking. We previously identified the original binding mode of 4-amino-2,4-dihydro-5-(2-methylphenyl)-3H-1,2,4-triazole-3-thione (compound IIIA) within the dizinc active site of the L1 MBL. Herein we present the crystallographic structure of a complex of L1 with the corresponding non-amino compound IIIB (1,2-dihydro-5-(2-methylphenyl)-3H-1,2,4-triazole-3-thione). Unexpectedly, the binding mode of IIIB was similar but reverse to that of IIIA. The 3 D structures suggested that the triazole–thione scaffold was suitable to bind to the catalytic site of dizinc metalloenzymes. On the basis of these results, we synthesized 54 analogues of IIIA or IIIB. Nineteen showed IC50 values in the micromolar range toward at least one of five representative MBLs (i.e., L1, VIM-4, VIM-2, NDM-1, and IMP-1). Five of these exhibited a significant inhibition of at least four enzymes, including NDM-1, VIM-2, and IMP-1. Active compounds mainly featured either halogen or bulky bicyclic aryl substituents. Finally, some compounds were also tested on several microbial dinuclear zinc-dependent hydrolases belonging to the MBL-fold superfamily (i.e., endonucleases and glyoxalase II) to explore their activity toward structurally similar but functionally distinct enzymes. Whereas the bacterial tRNases were not inhibited, the best IC50 values toward plasmodial glyoxalase II were in the 10 μm range.
A dihydro oats acyl anthranilic acid D synthesis method
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Paragraph 0031-0033; 0035-0044, (2018/11/03)
The invention provides a method for synthesizing 4-hydroxy benzenepropionamido benzoic acid. The method comprises the following steps: carrying out a thermal insulation reaction between p-hydroxybenzene propanoic acid and thionyl chloride in a cold bath a
N-substituted benzenepropanamide or benzenepropenamide derivatives for use in the treatment of pain and inflammation
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Page/Page column 9; 10, (2015/12/17)
Compounds for use in the treatment or prophylaxis of pain, including acute and chronic pain (e.g., nociceptive pain, neuropathic pain, headaches, migraine), represented by general formula (I) in which: the dotted line represents a single or a double bond; and R5 and R5′ are independently —H, —OH or —OR6, where R6 is a linear or branched C1-C4 alkyl; X is -0-, —CH2O—, —CH2CH2O—, —CH(CH3)CH2O— or —CH2CH(CH3)O—; Z is —CH2CH2O—, —CH(CH3)CH2O— or —CH2CH(CH3)O—; m is an integer of O or 1; and n is an integer of 0-50. The compounds of the invention are also effective for reducing inflammation and may be used alone or in combination with other analgesics.
Use of Syk Tyrosine Kinase Inhibitors for the Treatment of Cell Proliferative Disorders
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Page/Page column 7, (2009/12/24)
The invention relates to polyalkylene glycol compounds and their use in treating cell proliferative disorders, more specifically Syk tyrosine kinase-mediated disorders.
IMPROVEMENTS IN OR RELATING TO COMPOUNDS FOR USE IN THE TREATMENT OF AIDS AND OTHER VIRAL DISEASES AND HIV-RELATED INFECTIONS AND COMPOSITIONS CONTAINING SUCH COMPOUNDS, METHODS OF TREATING SUCH DISEASES AND INFECTIONS AND METHODS OF MAKING SUCH COMPOUNDS AND COMPOSITIONS
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Page/Page column 22, (2008/06/13)
The present invention provides methods for treating Acquired Immunodeficiency Syndrome (AIDS) and other viral diseases and Human Immunodeficiency Virus (HIV) related infections by administering one or more compounds of formula I: wherein: the dotted line represents a single or a double bond; and R1 and R2 are the same or different and independently of each other represent - CH2OH, -CH2OR4, -CH(OH)CH3, -CH(OR4)CH3 or a group represented by the formula: or salts or hydrates thereof in a carrier which minimizes micellar formation or van der Waals attraction of molecules of said compound. The invention also provides S enantiomeric forms of such compounds which possess the ability to inhibit cell growth whilst being of low toxicity to such cells and methods of making such compounds.
2-(Arylpropionylamino)- and 2-(arylacryloylamino)benzophenones: Farnesyltransferase inhibition and antimalarial activity
Fucik,Kettler,Wiesner,Ortmann,Unterreitmeier,Krauss,Bracher,Jomaa,Schlitzer, Martin
, p. 744 - 752 (2007/10/03)
Structural variation of the 2-acylamino moiety of some benzophenone farnesyltransferase inhibitors led to the para-trifluoromethylphenylpropionyl derivative with relatively low farnesyltransferase inhibition but considerable antimalarial activity and no c
NOVEL COMPOUNDS FOR USE IN THE TREATMENT OF AUTOIMMUNE DISEASES, IMMUNO-ALLERGICAL DISEASES AND ORGAN OR TISSUE TRANSPLANTATION REJECTION
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Example 1, (2010/02/06)
The present invention provides compounds, pharmaceutical compositions and methods for treating, immuno-allergical diseases, autoimmune diseases, and organ or tissue rejection following transplantation.
Efficient synthesis of resin-bound α-TMSdiazoketones and their use in solid-phase organic synthesis
Iso, Yasuyoshi,Shindo, Hirohisa,Hamana, Hiroshi
, p. 5353 - 5361 (2007/10/03)
α-TMSdiazoketones on a solid support could be simply and efficiently prepared by reaction of the corresponding resin-bound acid chlorides with excess TMSdiazomethane, without any bases. These α-TMSdiazoketones were used via carbenes or carbenoids for a variety of solid-phase reactions. These useful solid-phase reactions allow efficient construction of diverse compound libraries by use of combinatorial chemistry, due to the high reactivity and wide applications of the carbenes or carbenoids. (C) 2000 Elsevier Science Ltd.
