Styryl and azastyryl 1,3-benzazoles with antihelminthic activity.
New 2-benzylideneimino- and 2-styryl-1,3-benzimidazole and benzothiazole derivatives have been prepared and tested in vitro against Caenorhabditis elegans, and Heligmosomoides polygyrus, showing some of them, interesting properties as inhibitors, which were not observed in the complementary in vivo tests. In order to rationalize the activity, log P was measured for all compounds, and QSAR models were developed, allowing the optimisation of the in vitro activity.
Cuadro
A
A
Departamento de Quimica Organica, Universidad de Alcala, Alcala de Henares, Spain.
Perez-Butragueño
J
J
Pastor-Maeso
M
M
Alvarez-Builla
J
J
Martinez-Grueiro
M M
MM
Martinez-Fernandez
A R
AR
D000818:Animals; D000871:Anthelmintics / Q000138:chemical synthesis* / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D002107:Caenorhabditis / Q000187:drug effects; D051379:Mice; D008954:Models, Biological; D009348:Nematoda / Q000187:drug effects; D009349:Nematode Infections / Q000188:drug therapy / Q000469:parasitology; D013329:Structure-Activity Relationship; D013343:Styrenes / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use
D000871:Anthelmintics; D001562:Benzimidazoles; D013343:Styrenes