56309-59-2Relevant academic research and scientific papers
Design, Synthesis and Discovery of N,N’-Carbazoyl-aryl-urea Inhibitors of Zika NS5 Methyltransferase and Virus Replication
Spizzichino, Sharon,Mattedi, Giulio,Lauder, Kate,Valle, Coralie,Aouadi, Wahiba,Canard, Bruno,Decroly, Etienne,Kaptein, Suzanne J. F.,Neyts, Johan,Graham, Carl,Sule, Zakary,Barlow, David J.,Silvestri, Romano,Castagnolo, Daniele
supporting information, p. 385 - 390 (2020/01/24)
The recent outbreaks of Zika virus (ZIKV) infection worldwide make the discovery of novel antivirals against flaviviruses a research priority. This work describes the identification of novel inhibitors of ZIKV through a structure-based virtual screening approach using the ZIKV NS5-MTase. A novel series of molecules with a carbazoyl-aryl-urea structure has been discovered and a library of analogues has been synthesized. The new compounds inhibit ZIKV MTase with IC50 between 23–48 μM. In addition, carbazoyl-aryl-ureas also proved to inhibit ZIKV replication activity at micromolar concentration.
Method to produce hyperpolarised carboxylates
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Page/Page column 18;19, (2016/03/19)
The invention relates to a dynamic nuclear polarisation method for producing hyperpolarised carboxylates of organic amines and amino compounds and compositions for use in that method. The DNP agent preferably is a stable oxygen-based, sulphur-based or car
Imidazolidine Derivatives, Uses Therefor, Preparation Thereof and Compositions Comprising Such
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Page/Page column 56, (2010/04/23)
Compounds of formula (I): wherein X is O or S, R1 is acyl, aldehyde, cycloalkyl, an optionally substituted alkyl, alkenyl or alkynyl, R2 is H. alkyl, hydroxyalkyl, haloalkyl, alkenyl, or alkynyl; substituted alkyl; alkylcarbonyl; R3 and R4 are H, halogen, alkyl, alkenyl, alkynyl, alkoxyl, alkylthio, hydroxyalkyl, haloalkyl, haloalkenyl, or haloalkynyl; or R3 and R4 form an, optionally aromatic or heterocyclic, optionally substituted ring, R5 is H, halogen, trifluoromethyl, —CN, or —NO2; not all of R3, R4, and R5 being H, R6 and R9 are H, halogen, OH; alkyl. hydroxyalkyl, alkoxyl, thioalkyl, haloalkyl, alkenyl, or alkynyl; R7 and R8 are H, halogen, OH, SH; alkoxyl or alkylthio optionally substituted by OH and/or halogen; one of R7 and R8 not being H or halogen; or one of R7 and R8 is a pharmaceutically acceptable ester or thioester grouping, or R6 is C1-3-alkyl or, together with either R1 or R2, represents C1-3 alkylene or alkenylene linking group, optionally substituted by methyl, trifluoromethyl, OH, or halogen, and pharmaceutically acceptable salts and esters thereof, are useful as selective androgen modulators.
METHOD TO PRODUCE HYPERPOLARISED CARBOXYLATES AND SULPHONATES
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, (2010/09/18)
The invention relates to a dynamic nuclear polarisation method for producing hyperpolarised carboxylates or sulphonates or mixtures thereof wherein the carboxylate or sulphonate used in the method of the invention comprises certain inorganic cations. The
Method of Dynamic Nuclear Polarisation DNP
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Page/Page column 9, (2008/12/04)
The invention relates to a method of dynamic nuclear polarisation (DNP) using a combination of a trityl radical and a paramagnetic metal ion as the polarising agent leading to enhanced levels of polarisation in the sample to be polarised and to compositio
Method to Produce Hyperpolarised Carboxylates
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, (2009/01/20)
The invention relates to a dynamic nuclear polarisation method for producing hyperpolarised carboxylates of organic amines and amino compounds and compositions for use in that method. The DNP agent preferably is a stable oxygen-based, sulphur-based or car
MULTIMERIC MAGENTIC RESONANCE CONTRAST AGENTS
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Page/Page column 28; 40, (2008/06/13)
The present invention relates to novel compounds of formula (I) and (II), compositions comprising compounds of formula (II) and their use as contrast agents in magnetic resonance (MR) imaging (MRI) and MR spectroscopy (MRS).
NOVEL SUBSTITUTED THIOPHENECARBOXAMIDES, THEIR PRODUCTION AND THEIR USE AS MEDICAMENTS
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Page/Page column 228, (2008/06/13)
The invention relates to novel substituted thiophene-2-carboxamides of general formula (I), in which A, and R1 to R8c are defined as cited in claim 1. The invention also relates to the tautomers, enantiomers, diastereomers, mixtures and salts, in particular the physiologically compatible salts of said compounds containing inorganic or organic acids or bases, which exhibit valuable properties.
