40288-36-6Relevant 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.
Ph3P/I2-mediated synthesis of N,N′,N″-substituted guanidines and 2-iminoimidazolin-4-ones from aryl isothiocyanates
Wangngae, Sirilak,Pattarawarapan, Mookda,Phakhodee, Wong
, p. 10331 - 10340 (2018/05/31)
A convenient one-pot procedure for the synthesis of acyclic and cyclic guanidines mediated by the Ph3P/I2 system is described. Sequential condensation of aryl isothiocyanates with amines followed by dehydrosulfurization and guanylation could lead to both symmetric and unsymmetric N,N′,N″-substituted derivatives. Through a tandem guanylation-cyclization, a series of 2-iminoimidazolin-4-ones could also be prepared in good yields from the reaction of aryl isothiocyanates with amino acid methyl esters.
Powerful approach to heterocyclic skeletal diversity by sequential three-component reaction of amines, isothiocyanates, and 1,2-diaza-1,3-dienes
Attanasi, Orazio A.,Bartoccini, Silvia,Favi, Gianfranco,Giorgi, Gianluca,Perrulli, Francesca Romana,Santeusanio, Stefania
experimental part, p. 1161 - 1167 (2012/03/12)
By highly efficient, one-pot, three-component reactions, combining one set of 1,2-diaza-1,3-dienes (DDs), primary amines, and isothiocyanates in a different sequential order of addition, heterocyclic skeletal diversity can be achieved. The key feature dis
