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Synthesis and Biological Activities of Diquaternary Dipiperazinium Salts Containing Dithiocarboxyl Groups
Author(s) -
Ge ZeMei,
Li RunTao,
Cheng TieMing,
Cui JingRong
Publication year - 2001
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/1521-4184(200105)334:5<173::aid-ardp173>3.0.co;2-#
Subject(s) - chemistry , biological activity , stereochemistry , organic chemistry , biochemistry , in vitro
A series of diquaternary dipiperazinium salts containing dithiocarboxyl groups 6a — f and 9 were synthesized and evaluated for their analgesic and sedative activities. The result showed that the presence of two quaternary ammonium cations and the distance between them are very important for the activities of the salts. Compound 6b exhibited the best activities (at dose 2 mg/kg, analgesic, 57%; sedative, 59%) among compounds 6a — f . Compound 9 not only showed the most potent analgesic (85.4%, dose 1 mg/kg) and sedative (93.1%, dose 1 mg/kg) activities, but also exhibited anticancer activity against KB (68.7%, dose 10 μM).