Synthesis and evaluation of aminobenzothiazoles as blockers of N- and T-type calcium channels. Issue 11 (15th July 2018)

• Record Type: Journal Article
• Authors: Sairaman, Anjali; Cardoso, Fernanda Caldas; Bispat, Anjie; Lewis, Richard J.; Duggan, Peter J.; Tuck, Kellie L.
• Is Part Of: Bioorganic & medicinal chemistry. Volume 26:Issue 11(2018)
• Page Start: 3046
• Page End: 3059
• Publication Date: 2018-07-15
• Subjects: Pain -- Benzothiazole -- CaV2.2 -- N-type calcium channel -- CaV3.2 -- T-type calcium channel; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2018.03.031
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: 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 CaV 2.2 and CaV 3.2 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 CaV 2.2 and CaV 3.2 channels.