- Synthesis and antimicrobial evaluation of novel N-substituted 4-ethylsulfanyl-2-pyridones and triazolopyridines
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The design and development of new methods for the synthesis of antimicrobial drugs is an important goal currently for medicinal chemistry. Sixteen novel N-substituted-amino-, N-arylsulfonylamino-, and N-aryl-4-ethylsulfanyl-2-pyridones were synthesized. A
- Azzam, Rasha A.,Elgemeie, Galal H.
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- Discovery and optimization of pyrazolopyrimidine sulfamates as ATG7 inhibitors
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Autophagy is postulated to be required by cancer cells to survive periods of metabolic and/or hypoxic stress. ATG7 is the E1 enzyme that is required for activation of Ubl conjugation pathways involved in autophagosome formation. This article describes the design and optimization of pyrazolopyrimidine sulfamate compounds as potent and selective inhibitors of ATG7. Cellular levels of the autophagy markers, LC3B and NBR1, are regulated following treatment with these compounds.
- Adhikari, Sharmila,Brownell, James E.,Calderwood, Emily F.,Chouitar, Jouhara,D'Amore, Natalie Roy,England, Dylan B.,Foley, Klaudia,Gould, Alexandra E.,Harrison, Sean J.,Huang, Shih-Chung,LeRoy, Patrick J.,Lok, David,Lublinsky, Anna,Ma, Li-Ting,Menon, Saurabh,Yang, Yu,Zhang, Ji
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- ATG7 INHIBITORS AND THE USES THEREOF
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Disclosed are chemical entities which are compounds of formula (I) : or a pharmaceutically acceptable salt thereof, wherein R1, R2, and Ra have the values described herein. Chemical entities according to the disclosure can be useful as inhibitors of ATG7. Further provided are pharmaceutical compositions comprising a chemical entity of the disclosure and methods of using the compositions in the treatment of cancer.
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Paragraph 00319
(2018/05/27)
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- An unprecedented trinuclear FeII triazole-based complex exhibiting a concerted and complete sharp spin transition above room temperature
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We report a triazole-based trinuclear complex as the first example that displays a complete one-step first-order [HS-HS-HS] ? [LS-LS-LS] spin transition at 318 K. The strong ferro-elastic interactions, between the three metal centers, have been identified as the source of the concerted spin transition in this trinuclear complex.
- Pittala, Narsimhulu,Thétiot, Franck,Charles, Catherine,Triki, Smail,Boukheddaden, Kamel,Chastanet, Guillaume,Marchivie, Mathieu
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supporting information
p. 8356 - 8359
(2017/07/26)
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- Synthesis of Pyrroles, a Diazepindione and Substituted 3-Aminoacrylonitriles by Reaction of Bisalkylthioacrylonitriles with α-Aminoacid Derivatives
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3,3-Bisalkylthioacrylonitriles (2), substituted by a cyano, carboxylate or amido group at position 2 react with derivatives 5 of α-aminoacids by monosubstitution under the formation of 3-carbonylmethylaminoacrylnitriles (6) or by substitution and cyclisation to 5-alkylthio-3-aminopyrrole-2-carboxylates (7) or the tetrahydro-1,4-diazepin-2,7-dione (8).
- Erdmann, Barbara,Knoll, A.,Liebscher, J.
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p. 1015 - 1021
(2007/10/02)
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- HETEROCYCLIC AND RELATED COMPOUNDS DERIVED FROM DIPOTASSIUM 1,1-DIMERCAPTO-2,2-DICYANOETHYLENE AND SODIUM 2-MERCAPTOPYRIDINE N-OXIDE
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The reaction of dipotassium 1,1-dimercapto-2,2-dicyanoethylene with certain halogen compounds furnished the expected dialkylation products (1)-(4).Replacing the halogen compound with 4-chloro-3,5-dinitrobenzotrifluoride afforded a novel heterocycle (5).The reaction of the potassium salt with phenyl or p-chlorophenylchlorothioformate gave 2,2-diphenyl or di-p-chlorophenylthio-2,2-dicyanoethylene (6) and (7).The reaction of 1 or 2 with excess hydrogen peroxide afforded substituted oxiranes (8) and (9).Depending on reaction conditions, the reaction of sodium 2-mercaptopyridine N-oxide with 4-chloro-3,5-dinitrobenzotrifluoride afforded either the expected sulfide (11) or the unexpected heterocycle (12).Possible mechanisms and supporting NMR, Ir and mass spectral data are discussed.
- D'Amico, J. J.,Ruminski, P. G.,Suba, L. A.,Freeman, J. J.,Dahl, W. E.
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p. 307 - 314
(2007/10/02)
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- 3-Alkylthio-, 3-alkylsulfinyl-, and 3-alkylsulfonylisothiazole derivatives as herbicides
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A new class of herbicidal compounds consisting of 1-alkyl- and 1,1-dialkyl-3-(3,4-substituted-5-isothiazolyl)ureas and N-(3,4-substituted-5-isothiazolyl)-alkanamides in which the 3-substituent consists of alkylthio, alkylsulfinyl, and alkylsulfonyl, and the 4-substituent consists of cyano, and carbamoyl, exhibits preemergence and postemergence herbicidal activity, controlling effectively the growth of a wide spectrum of grassy and broad-leaved plant species. The synthesis of members of this class is described in detail, and the utility of representative compounds is exemplified.
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