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

Publication date: Available online 19 March 2018
Source:Bioorganic & Medicinal Chemistry
Author(s): Anjali Sairaman, Fernanda Caldas Cardoso, Anjie Bispat, Richard J. Lewis, Peter J. Duggan, Kellie L. Tuck
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.

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