|
|||||
|
|
Synthesis and evaluation of aminobenzothiazoles as blockers of N- and T-type calcium channels |
|
| Authors: | Anjali Sairaman Fernanda Caldas Cardoso Anjie Bispat Richard J Lewis Peter J Duggan Kellie L Tuck |
| Institution: | 1. IITB-Monash Research Academy, Powai, Mumbai 400076, India;2. Department of Chemistry, IIT Bombay, Mumbai 400076, India;3. CSIRO Manufacturing, Bag 10, Victoria 3169, Australia;4. School of Chemistry, Monash University, Victoria 3800, Australia;5. Institute for Molecular Bioscience, The University of Queensland, St Lucia, QLD 4072, Australia;6. School of Chemical and Physical Sciences, Flinders University, South Australia 5042, Australia |
| 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. |
| Keywords: | Pain Benzothiazole N-type calcium channel T-type calcium channel |
| 本文献已被 ScienceDirect 等数据库收录！ | |