- Design, synthesis, and mechanistic investigations of phenylalanine derivatives containing a benzothiazole moiety as HIV-1 capsid inhibitors with improved metabolic stability
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Further clinical development of PF74, a lead compound targeting HIV-1 capsid, is impeded by low antiviral activity and inferior metabolic stability. By modifying the benzene (region I) and indole of PF74, we identified two potent compounds (7m and 7u) wit
- Cherukupalli, Srinivasulu,Cocklin, Simon,De Clercq, Erik,Dick, Alexej,Ding, Dang,Ding, Xiao,Gao, Shenghua,Huang, Tianguang,Jiang, Xiangyi,Kang, Dongwei,Liu, Xinyong,Meuser, Megan E.,Pannecouque, Christophe,Sun, Lin,Tao, Yucen,Xu, Shujing,Zalloum, Waleed A.,Zhan, Peng,Zhang, Xujie
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- Phenylalanine derivative containing benzothiazole, and preparation method and application thereof
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The invention provides a phenylalanine derivative containing benzothiazole and a preparation method and application thereof. The derivative has the structure shown in the general formula I below. The invention also relates to a preparation method of the d
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Paragraph 0068-0074; 0155-0159
(2021/10/05)
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- Synthesis of polyaramids in γ-valerolactone-based organic electrolyte solutions
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The current synthetic procedures for polyaramids mainly involve the use of amide solvents such asN-methylpyrrolidone andN,N-dimethylacetamide. However, these solvents are suspected to be teratogenic and are considered ‘Substances of Very High Concern’ by the European Commission. Here we propose a benign alternative solvent system: an Organic Electrolyte Solution (OES) consisting of γ-valerolactone (GVL) and a small amount of the ionic liquid 1-methyl-3-octylimidazolium chloride, [C8MIm][Cl]. Three commercially relevant polyaramids were synthesized: poly-p-phenylene terephthalamide (PPTA), poly-m-phenylene isophthalamide (PMIA) and copoly(p-phenylene/3,4′-diphenylether terephthalamide) (ODA/PPTA). PMIA was successfully synthesized in the OES containing [C8MIm][Cl] in a molar fraction ofxIL= 0.043, achieving an inherent viscosity ofηinh= 1.94 ± 0.064 dL g?1, which is on par with the current industrial standard and the benchmark lab scale synthesis. The reaction mixture could also be directly used for the wet spinning of polyaramid fibers, and all components of the solvent could be recycled in good yields by a series of evaporation and distillation steps. ODA/PPTA could be synthesized, but only rather low inherent viscosities were achieved. The reaction mixture was too viscoelastic to be spun by our small-scale spinning setup. PPTA always instantly precipitated and could not be synthesized from a [C8MIm][Cl]/GVL OES. α-Picoline, the organic base which was added to capture the released HCl during the reaction, was found to play a pivotal role in the polymerization reaction. By undergoing an acid-base reaction with HCl, it forms a protic ionic liquidin situwhich increases the solubility of the polymer.
- Winters, Jonas,Bolia, Raheed,Dehaen, Wim,Binnemans, Koen
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p. 1228 - 1239
(2021/02/26)
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- Aromatic Amide Compound
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An aromatic amide compound having the following general formula (I) is provided: wherein, X1 and X2 are independently C(O)HN or NHC(O);G1, G2 and G3 are independently hydrogen, C(O)HN-phenyl, or NHC(O)-phenyl, wherein at least one of G1, G2 and G3 is C(O)HN-phenyl or NHC(O)-phenyl;Q1, Q2, and Q3 are independently hydrogen, C(O)HN-phenyl, or NHC(O)-phenyl, wherein at least one of Q1, Q2, and Q3 is C(O)HN-phenyl or NHC(O)-phenyl;R5 is halo, haloalkyl, alkyl, alkenyl, aryl, heteroaryl, cycloalkyl, or heterocyclyl; andm is from 0 to 4.
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Paragraph 0071; 0072
(2013/03/26)
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- Meta-Substituted benzamide oligomers that complex mono-, di- and tricarboxylates: Folding-induced selectivity and chirality
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meta-Substituted arylamide trimer, pentamer and heptamer have been prepared from simple benzene-1,3-diamine, benzene-1,3-dicarboxylic acid, and 3-aminobenzoic acid units. 2D NOESY 1H NMR experiments reveal that these flexible oligomers form fol
- Shi, Zhu-Ming,Chen, Shi-Gui,Zhao, Xin,Jiang, Xi-Kui,Li, Zhan-Ting
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experimental part
p. 8122 - 8129
(2012/01/04)
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- Foldamers as cross-links for tuning the dynamic mechanical property of methacrylate copolymers
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This paper reports a foldamer-based approach to modulating the thermal and mechanical properties of cross-linked n-butyl methacrylate copolymers. Intramolecularly hydrogen-bonding-induced folded aromatic amide segments were designed and prepared, which reacted with a salicylaldehyde-bearing prepolymer to form cross-linked copolymers. As a control, analogous aromatic cross-links incapable of forming discrete folded structures due to lack of specific intramolecular H-bonding were also prepared and incorporated into copolymers. From the two series of cross-linked copolymers, 18 films were prepared and characterized by dynamic mechanical analysis (DMA) as well as creep/recovery experiments. We show that, compared to the control, the discrete folded cross-links substantially improve the mechanical properties of the copolymers. We attribute this enhancement to the ability of the folded cross-links to reversibly reveal the hidden length on extension via dissipative cleavage of the intramolecular H-bonds.
- Shi, Zhu-Ming,Huang, Jin,Ma, Zhi,Zhao, Xin,Guan, Zhibin,Li, Zhan-Ting
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experimental part
p. 6185 - 6192
(2011/11/12)
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- Ring-chain interconversion in high-performance polymer systems. 3. Cyclodepolymerization of poly(m-phenylene isophthalamide) (nomex) and entropically driven ring-opening polymerization of the macrocyclic oligomers so produced
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A homologous series of macrocyclic oligoamides has been prepared in high yield by reaction of isophthaloyl chloride with m-phenylenediamine under pseudo-high-dilution conditions. The products were characterized by infrared and 1H NMR spectrosco
- Ben-Haida, Abderrazak,Hodge, Philip,Colquhoun, Howard M.
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p. 722 - 729
(2007/10/03)
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- Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use
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Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
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