Synthesis and evaluation of aminobenzothiazoles as blockers of N- and T-type calcium channels

Anjali Sairaman, Fernanda Caldas Cardoso, Anjie Bispat, Richard J. Lewis, Peter J. Duggan, Kellie L. Tuck

    Research output: Contribution to journalArticlepeer-review

    7 Citations (Scopus)

    Abstract

    Both N- and T-type calcium ion channels have been implicated in pain transmission and the N-type channel is a well-validated target for the treatment of neuropathic pain. An SAR investigation of a series of substituted aminobenzothiazoles identified a subset of five compounds with comparable activity to the positive control Z160 in a FLIPR-based intracellular calcium response assay measuring potency at both CaV2.2 and CaV3.2 channels. These compounds may form the basis for the development of drug leads and tool compounds for assessing in vivo effects of variable modulation of CaV2.2 and CaV3.2 channels.

    Original languageEnglish
    Pages (from-to)3046-3059
    Number of pages14
    JournalBioorganic and Medicinal Chemistry
    Volume26
    Issue number11
    DOIs
    Publication statusPublished - 15 Jul 2018

    Keywords

    • Benzothiazole
    • Cav2.2
    • Cav3.2
    • N-type calcium channel
    • Pain
    • T-type calcium channel

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