Synthesis and biological activities of diquaternary dipiperazinium salts containing dithiocarboxyl groups.
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 microM).
Ge
Z M
ZM
School of Pharmaceutical Sciences, Peking University, Beijing, 100083, P.R. China.
Li
R T
RT
Cheng
T M
TM
Cui
J R
JR
D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D019281:Dimerization; D004353:Drug Evaluation, Preclinical; D005260:Female; D006801:Humans; D006993:Hypnotics and Sedatives / Q000138:chemical synthesis* / Q000494:pharmacology; D007624:KB Cells / Q000187:drug effects; D008297:Male; D051379:Mice; D010879:Piperazines / Q000138:chemical synthesis / Q000494:pharmacology; D000644:Quaternary Ammonium Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000700:Analgesics; D000970:Antineoplastic Agents; D006993:Hypnotics and Sedatives; D010879:Piperazines; D000644:Quaternary Ammonium Compounds