56309-59-2Relevant articles and documents
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.
Imidazolidine Derivatives, Uses Therefor, Preparation Thereof and Compositions Comprising Such
-
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 of Dynamic Nuclear Polarisation DNP
-
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