2-Phenylimidazo[1,2- b]pyridazine derivatives highly active against Haemonchus contortus

A series of 2-phenylimidazo[1,2- b]pyridazine derivatives were synthesized and evaluated for their in vitro anthelmintic activity against Haemonchus contortus. The most active compounds had in vitro LD 99 values comparable to that of the benchmark commercial nematocide, Ivermectin. A series of 2-phe...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 21; no. 14; pp. 4160 - 4163
Main Authors:	Ali, Abdelselam, Cablewski, Teresa, Francis, Craig L., Ganguly, Ashit K., Sargent, Roger M., Sawutz, David G., Winzenberg, Kevin N.
Format:	Journal Article
Language:	English
Published:	Amsterdam Elsevier Ltd 15-07-2011 Elsevier
Subjects:	Animals Anthelmintic Antibiotics. Antiinfectious agents. Antiparasitic agents Antinematodal Agents - chemical synthesis Antinematodal Agents - chemistry Antinematodal Agents - pharmacology Antiparasitic agents Biological and medical sciences chemistry Haemonchus - drug effects Haemonchus - growth & development Haemonchus contortus Imidazo[1,2- b]pyridazine ivermectin Ivermectin - chemistry Ivermectin - pharmacology Larva - drug effects Medical sciences nematicides Pharmacology. Drug treatments Pyridazines - chemical synthesis Pyridazines - chemistry Pyridazines - pharmacology Structure-Activity Relationship Imidazo[1,2- b]pyridazine Haemonchus contortus Anthelmintic Ether Angular nitrogen heterocycle Benzene derivatives In vitro Structure activity relation Imidazo[ 1,2-b]pyridazine Helmintha Bicyclic compound Parasiticide Nemathelminthia Diether Invertebrata Chemical synthesis Nematoda
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Summary:	A series of 2-phenylimidazo[1,2- b]pyridazine derivatives were synthesized and evaluated for their in vitro anthelmintic activity against Haemonchus contortus. The most active compounds had in vitro LD 99 values comparable to that of the benchmark commercial nematocide, Ivermectin. A series of 2-phenylimidazo[1,2- b]pyridazine derivatives were synthesized and evaluated for their in vitro anthelmintic activity against Haemonchus contortus. The most active compounds had in vitro LD 99 values of 30 nM, which is comparable to that of the benchmark commercial nematocide, Ivermectin.
Bibliography:	http://dx.doi.org/10.1016/j.bmcl.2011.05.096 ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 ObjectType-Article-2 ObjectType-Feature-1
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.05.096