Synthesis and biological activity of anthelmintic thiadiazoles using an AF-2 receptor binding assay

Authors
Lee, BH Dutton, FE Clothier, MF Bowman, JW Davis, JP Johnson, SS Thomas, EM Zantello, MR Zinser, EW McGuire, JC Thompson, DP Geary, TG
Citation
Bh. Lee et al., Synthesis and biological activity of anthelmintic thiadiazoles using an AF-2 receptor binding assay, BIOORG MED, 9(12), 1999, pp. 1727-1732
Citations number
16
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
12
Year of publication
1999
Pages
1727 - 1732
Database
ISI
SICI code
0960-894X(19990621)9:12<1727:SABAOA>2.0.ZU;2-H
Abstract
Following our discovery of the strong binding of thiadiazole 1 to the AF-2 neuropeptide receptor of gastrointestinal nematodes (e.g., Ascaris suum), w e prepared two series of analogs. Only the series containing the thiadiazol e 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. (C) 1999 Elsevier Science Ltd. All rights reserved.