Literature DB >> 10397509

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

B H Lee1, F E Dutton, M F Clothier, J W Bowman, J P Davis, S S Johnson, E M Thomas, M R Zantello, E W Zinser, J C McGuire, D P Thompson, T G Geary.   

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.

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Year:  1999        PMID: 10397509     DOI: 10.1016/s0960-894x(99)00267-x

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  The nematode neuropeptide, AF2 (KHEYLRF-NH2), increases voltage-activated calcium currents in Ascaris suum muscle.

Authors:  S Verma; A P Robertson; R J Martin
Journal:  Br J Pharmacol       Date:  2007-05-21       Impact factor: 8.739

  1 in total

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