Discovery of amino-acetonitrile derivatives, a new class of synthetic anthelmintic compounds.
A new series of amino-acetonitrile derivatives (AAD) have been discovered that exhibit high anthelmintic activity against parasitic nematode species such as Haemonchus contortus and Trichostrongylus colubriformis. Significantly, these compounds also demonstrate activity against nematode strains resistant to the currently available broad-spectrum anthelmintics. The discovery, synthesis, structure-activity relationship and biological results are presented.
Ducray
Pierre
P
Novartis Animal Health Inc., Chemistry and Bioactives, Schwarzwaldallee 215, CH-4002 Basel, Switzerland.
Gauvry
Noëlle
N
Pautrat
François
F
Goebel
Thomas
T
Fruechtel
Joerg
J
Desaules
Yves
Y
Weber
Sandra Schorderet
SS
Bouvier
Jacques
J
Wagner
Trixie
T
Froelich
Olivier
O
Kaminsky
Ronald
R
D000607:Aminoacetonitrile / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D000871:Anthelmintics / Q000138:chemical synthesis / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006189:Haemonchus / Q000187:drug effects*; D008956:Models, Chemical; D021261:Parasitic Sensitivity Tests; D013329:Structure-Activity Relationship; D014254:Trichostrongylus / Q000187:drug effects*
D000871:Anthelmintics; D000607:Aminoacetonitrile