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May 13-14, 2019 | Prague, Czech Republic
Chemistry and Medicinal Chemistry
9
th
World Congress on
Asian Journal of Biomedical and Pharmaceutical Sciences | Volume 9
ISSN: 2249-622X
Synthesis of Voltage Gated Sodium Channel Blockers (VGSCB)
Bölcskei H
1,2
1
Budapest University of Technology and Economics, Hungary
2
Gedeon Richter Plc., Hungary
V
oltage gated sodium channels play an important role
in the physiological processes of the central nervous
system. The main therapeutic areas are epilepsy, various
types of pain, migraine and spasticity. In this talk the
key aspects and difficulties (e.g. hERG activity) of the
development of the new compounds with VGSCB activity
will be demonstrated on three examples.
1) CompanyGedeonRICHTERdevelopedthecentrallyacting
muscle relaxant Mydeton. Searching its derivatives,
many aryloxy-alkyl-amines were synthetized, changing
the aromatic moiety, the spacer, the amine function.
2) An HTS was the starting point of the development of
NaV1.7 Subtype selective sodium channel blockers.
Various members of an aryl- and heteroarylsubstituted
benzyloxy-benzylamine compound family were prepared.
3) Targeting the obscessive compulsive disorder,
compounds were prepared with dual activity: VGSCB
and serotonin reuptake inhibitory activity. We focused
on dextormethorphan derivatives. The best compounds
were tested in vivo (marble burying test) too.
Speaker Biography
Bölcskei H has completed her MSc study as a chemical engineer from
University of Technology, Budapest, Hungary. She received her PhD
in 1979 at the same university, and her scientific degree “candidate of
sciences” in 1988 from the Hungarian Academy of Sciences. Between
1973-2013 she worked as a researcher at the Hungarian pharmaceutical
company Gedeon Richter Plc. Since 2009 she has been working as
the associate professor of University of Technology and Economics,
Budapest, Hungary. Her main research interest: alkaloid chemistry,
organic chemistry, medicinal chemistry. She has over 60 publications that
have been cited over 200 times.
e:
h.bolcskei@mail.bme.huBölcskei H, Asian J Biomed Pharmaceut Sci, Volume:9
DOI: 10.4066/2249-622X-C2-020