N-Sulfonylphenoxazines as neuronal calcium ion channel blockers

Author:

Schmit Matthieu12ORCID,Hasan Md. Mahadhi3,Dongol Yashad3ORCID,Cardoso Fernanda C.3,Kuiper Michael J.4,Lewis Richard J.3,Duggan Peter J.25ORCID,Tuck Kellie L.1ORCID

Affiliation:

1. School of Chemistry, Monash University, Victoria 3800, Australia

2. CSIRO Manufacturing, Research Way, Clayton, Victoria 3168, Australia

3. Institute for Molecular Bioscience, The University of Queensland, St. Lucia, QLD 4072, Australia

4. CSIRO Data 61, Clunies Ross Street, Acton ACT 2601, Australia

5. College of Science and Engineering, Flinders University, Adelaide, South Australia 5042, Australia

Abstract

A series of N-sulfonylphenoxazines were synthesised and tested for CaV2.2 and CaV3.2 ion channel inhibition. Compounds with low micromolar activity for CaV2.2 had good plasma stability and liver microsomal stability, and favourable CNS MPO scores.

Funder

Monash University

Commonwealth Scientific and Industrial Research Organisation

National Health and Medical Research Council

Publisher

Royal Society of Chemistry (RSC)

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