Bioorganic & Medicinal Chemistry 26 (2018) 3046–3059 Contents lists available at ScienceDirect Bioorganic & Medicinal Chemistry journal homepage: www.elsevier.com/locate/bmc Synthesis and evaluation of aminobenzothiazoles as blockers of N- and T-type calcium channels a,b,c,d e c,d e c,f,⇑ Anjali Sairaman , Fernanda Caldas Cardoso , Anjie Bispat , Richard J. Lewis , Peter J. Duggan , d,⇑ Kellie L. Tuck IITB-Monash Research Academy, Powai, Mumbai 400076, India Department of Chemistry, IIT Bombay, Mumbai 400076, India CSIRO Manufacturing, Bag 10, Victoria 3169, Australia School of Chemistry, Monash University, Victoria 3800, Australia Institute for Molecular Bioscience, The University of Queensland, St Lucia, QLD 4072, Australia School of Chemical and Physical Sciences, Flinders University, South Australia 5042, Australia ar ti c l e i nf o ab stra ct Article history: Both N- and T-type calcium ion channels have been implicated in pain transmission and the N-type chan- Received 15 February 2018 nel is a well-validated target for the treatment of neuropathic pain. An SAR investigation of a series of Revised 15 March 2018 substituted aminobenzothiazoles identiﬁed a subset of ﬁve compounds with comparable activity to Accepted 18 March 2018 the positive control Z160 in a FLIPR-based intracellular calcium response assay measuring potency
Bioorganic & Medicinal Chemistry – Elsevier
Published: Jul 15, 2018
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