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

Synthesis and evaluation of aminobenzothiazoles as blockers of N- and T-type calcium channels 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 http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Bioorganic & Medicinal Chemistry Elsevier

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

Loading next page...
 
/lp/elsevier/synthesis-and-evaluation-of-aminobenzothiazoles-as-blockers-of-n-and-t-IOqua87iJ7
Publisher
Elsevier
Copyright
Copyright © 2018 Elsevier Ltd
ISSN
0968-0896
D.O.I.
10.1016/j.bmc.2018.03.031
Publisher site
See Article on Publisher Site

Abstract

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

Journal

Bioorganic & Medicinal ChemistryElsevier

Published: Jul 15, 2018

References

You’re reading a free preview. Subscribe to read the entire article.


DeepDyve is your
personal research library

It’s your single place to instantly
discover and read the research
that matters to you.

Enjoy affordable access to
over 18 million articles from more than
15,000 peer-reviewed journals.

All for just $49/month

Explore the DeepDyve Library

Search

Query the DeepDyve database, plus search all of PubMed and Google Scholar seamlessly

Organize

Save any article or search result from DeepDyve, PubMed, and Google Scholar... all in one place.

Access

Get unlimited, online access to over 18 million full-text articles from more than 15,000 scientific journals.

Your journals are on DeepDyve

Read from thousands of the leading scholarly journals from SpringerNature, Elsevier, Wiley-Blackwell, Oxford University Press and more.

All the latest content is available, no embargo periods.

See the journals in your area

DeepDyve

Freelancer

DeepDyve

Pro

Price

FREE

$49/month
$360/year

Save searches from
Google Scholar,
PubMed

Create lists to
organize your research

Export lists, citations

Read DeepDyve articles

Abstract access only

Unlimited access to over
18 million full-text articles

Print

20 pages / month

PDF Discount

20% off