874766-64-0Relevant articles and documents
Synthesis and antimalarial activity of (S)-methyl-(7-chloroquinolin-4-ylthio)acetamidoalquilate derivatives
Colmenarez, Custodiana,Acosta, María,Rodríguez, Miguel,Charris, Jaime
, p. 161 - 166 (2020/01/09)
The synthesis of five new (S)-methyl-(7-chloroquinolin-4-ylthio)acetamidoalquilate derivatives is carried out under a modified version of the Steglich esterification reaction between different l-amino acid methyl esters and 2-(7-chloroquinolin-4-ylthio)acetic acid. Two of the compounds showed significant inhibition (>50%) of β-hematin formation. The two active structures were tested in vivo as potential antimalarials in mice infected with Plasmodium berghei ANKA, a chloroquine susceptible strain. Compounds 6b and 6e exhibited antimalarial activity comparable to that of chloroquine.
N-Acylhydrazones as inhibitors of PDE10A
Gage, Jennifer L.,Onrust, Rene,Johnston, Derek,Osnowski, Andrew,MacDonald, Wendy,Mitchell, Lee,ür?gdi, László,Rohde, Alex,Harbol, Kevin,Gragerov, Sasha,Dormán, Gy?rgy,Wheeler, Tom,Florio, Vince,Cutshall, Neil S.
scheme or table, p. 4155 - 4159 (2011/08/10)
Cyclic nucleotide phosphodiesterases (PDEs) are represented by a large superfamily of enzymes. A series of hydrazone-based inhibitors was synthesized and shown to be novel, potent, and selective against PDE10A. Optimized compounds of this class were efficacious in animal models of schizophrenia and may be useful for the treatment of this disease.
