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 journalArticleResearchpeer-review

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 - 2018

Keywords

  • Benzothiazole
  • Ca2.2
  • Ca3.2
  • N-type calcium channel
  • Pain
  • T-type calcium channel

Cite this

Sairaman, Anjali ; Cardoso, Fernanda Caldas ; Bispat, Anjie ; Lewis, Richard J. ; Duggan, Peter J. ; Tuck, Kellie L. / Synthesis and evaluation of aminobenzothiazoles as blockers of N- and T-type calcium channels. In: Bioorganic and Medicinal Chemistry. 2018 ; Vol. 26, No. 11. pp. 3046-3059.
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Synthesis and evaluation of aminobenzothiazoles as blockers of N- and T-type calcium channels. / Sairaman, Anjali; Cardoso, Fernanda Caldas; Bispat, Anjie; Lewis, Richard J.; Duggan, Peter J.; Tuck, Kellie L.

In: Bioorganic and Medicinal Chemistry, Vol. 26, No. 11, 2018, p. 3046-3059.

Research output: Contribution to journalArticleResearchpeer-review

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