16982-21-1Relevant articles and documents
1,2,4-Triazine-Modified 2′-Deoxyuridine Triphosphate for Efficient Bioorthogonal Fluorescent Labeling of DNA
Peewasan, Krisana,Wagenknecht, Hans-Achim
, p. 1473 - 1476 (2017)
In order to establish the Diels–Alder reaction with inverse electron demand for postsynthetic DNA modification, a 1,2,4-triazine-modified 2′-deoxyuridine triphosphate was synthesized. The bioorthogonally reactive 1,2,4-triazine group was attached at the 5-position of 2′-deoxyuridine by a flexible alkyl linker to facilitate its acceptance by DNA polymerases. The screening of four DNA polymerases showed successful primer extensions, using a mixture of dATP, dGTP, dCTP, and the modified 2′-deoxyuridine triphosphate, by using KOD XL or Vent polymerase. The triazine moiety was stable under the conditions of primer extension, which was evidenced by labeling with a BCN-modified rhodamine at room temperature in yields of up to 82 %. Two or three modified bases could be incorporated in quantitative yields when the modification sites were separated by three base pairs. These results establish the 1,2,4-triazene group as a bioorthogonally reactive moiety in DNA, thereby replacing the problematic 1,2,4,5-tetrazine for postsynthetic labeling by the Diels–Alder reaction with inverse electron demand.
The crystal structure and vibrational spectra of potassium oxathioamidate
Hereygers, Marleen L.B.F.,Desseyn, Herman O.,Perlepes, Spyros P.,Verhulst, Koen A.F.,Lenstra, Albert T.H.
, p. 181 - 188 (1995)
The crystal and molecular structure determination of the title compound, K-SO2NC2H2, Mr = 143.21, (1) is part of a series of determinations of N-substituted oxathioamidates.The structure has been refined using single-crystal X-ray diffraction data measured at 295 K .The crystals are orthorhombic, space group Pn21a, Z = 8, with cell dimensions: a = 11.399(2) Angstroem, b = 22.131(2) Angstroem, c = 4.021(1) Angstroem, V = 1014.5(7) Angstroem3.Dcalc. = 1.875 mg m-3, Dobs = 1.600 mg m-3, F(000) = 576, μ = 13.14 cm-1.The final agreement factors for 1979 observed reflections 3?(I)> were: R = 0.062 and Rw = 0.067.The vibrational spectra confirm the geometrical differences between the two thiooxamidate molecules.KEY WORDS: Potassium oxathioamidate.
METHODS AND COMPOSITIONS FOR INHIBITING CNKSR1
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Paragraph 0154, (2014/07/07)
Embodiments include compositions and methods of inhibiting CNKSR1 and methods of identifying inhibitors of CNKSR1.
IMIDAZOTHIADIAZOLE AND IMIDAZOPYRAZINE DERIVATIVES AS PROTEASE ACTIVATED RECEPTOR 4 (PAR4) INHIBITORS FOR TREATING PLATELET AGGREGATION
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Paragraph 00147, (2013/11/18)
The present invention provides thiazole compounds of Formula I wherein W, Y, R0, R2, R4, R5, R6, R7, X1, X2, X3 and X4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.
PAR4 AGONIST PEPTIDES
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Page/Page column, (2013/11/06)
The present invention provides PAR4 agonist peptides. These peptides are useful for developing robust PAR4 receptor assays.
ARYLCYCLOPROPYLAMINE BASED DEMETHYLASE INHIBITORS OF LSD1 AND THEIR MEDICAL USE
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Page/Page column 107; 108, (2012/02/13)
The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).
Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants
Kazmierski, Wieslaw M.,Hamatake, Robert,Duan, Maosheng,Wright, Lois L.,Smith, Gary K.,Jarvest, Richard L.,Ji, Jing-Jing,Cooper, Joel P.,Tallant, Matthew D.,Crosby, Renae M.,Creech, Katrina,Wang, Amy,Li, Xianfeng,Zhang, Suoming,Zhang, Yong-Kang,Liu, Yang,Ding, Charles Z.,Zhou, Yasheen,Plattner, Jacob J.,Baker, Stephen J.,Bu, Wei,Liu, Liang
supporting information; experimental part, p. 3021 - 3026 (2012/06/01)
The macrocyclic urea 2, a byproduct in the synthesis of benzoxaborole 1, was identified to be a novel and potent HCV protease inhibitor. We further explored this motif by synthesizing additional urea-based inhibitors and by characterizing them in replicase HCV protease-resistant mutants assay. Several compounds, exemplified by 12, were found to be more potent in HCV replicon assays than leading second generation inhibitors such as danoprevir and TMC-435350. Additionally, following oral administration, inhibitor 12 was found in rat liver in significantly higher concentrations than those reported for both danoprevir and TMC-435350, suggesting that inhibitor 12 has the combination of anti-HCV and pharmacokinetic properties that warrants further development of this series.
AMINOTRIAZOLE DERIVATIVES AS ALX AGONISTS
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Page/Page column 80-81, (2009/07/18)
The invention relates to aminotriazole derivatives of formula (I), wherein A, E, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds. The compounds are useful for the prevention or treatment of diseases, which respond to the modulation of the ALX receptor such as inflammatory diseases.
SUBSTITUTED SULFONAMIDE DERIVATIVES
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Page/Page column 144, (2009/11/29)
The invention relates to substituted sulfonamide derivatives, processes for the preparation thereof, medicaments containing these compounds and the use of substituted sulfonamide derivatives for the preparation of medicaments.
THIAZOLE-2-CARBOXAMIDE DERIVATIVES FOR USE AS HPPAR AGONISTS IN THE TREATMENT OF I.A. DYSLIPIDEMIA
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Page/Page column 10, (2010/02/11)
A compound of formula (I) and pharmaceutically acceptable salts, solvates and hydrolysable esters thereof is claimed for use as a selective dual agonist of PPAR alpha and gamma.
