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Synthesis and biological activity of anthelmintic thiadiazoles using an AF-2 receptor binding assay
B H Lee1, F E Dutton, M F Clothier
1Animal Health Discovery Research, Pharmacia & Upjohn, Inc., Kalamazoo, MI 49001, USA.
Bioorganic & Medicinal Chemistry Letters
|July 9, 1999
Abstract:
Following our discovery of the strong binding of thiadiazole 1 to the AF-2 neuropeptide receptor of gastrointestinal nematodes (e.g., Ascaris suum), we prepared two series of analogs. Only the series containing the thiadiazole ring had potencies comparable to that of compound 1. Analog 50 exhibited an apparent potency in the AF-2 binding assay 300 times that of compound 1.