Studies on synthesis and biological properties of pyrazolo[4,3-c]-pyrido[3,2-e]-1,2-thiazine-5,5-dioxide bearing 4-substituted-1-piperazinylpropyl moiety.
Derivatives of the pyrazolopyridothiazine-5,5-dioxide 6 and the pyridothiazine-1,1-dioxide 2 bearing 4-phenyl-(heteroaryl)-1-piperazinylpropyl substituent at the nitrogen of the thiazine ring were synthesized. The acute toxicity and preliminary results of the CNS activity of some derivatives 2 and 6 are described. A structure-activity relationship is discussed.
Malinka
W
W
Department of Drug Chemistry, Wroclaw University of Medicine, Poland.
Sieklucka-Dziuba
M
M
Rajtar-Cynke
G
G
Borowicz
K
K
Kleinrok
Z
Z
D000818:Animals; D002490:Central Nervous System / Q000187:drug effects*; D005260:Female; D007928:Lethal Dose 50; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000633:toxicity; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship; D013843:Thiazines / Q000138:chemical synthesis* / Q000633:toxicity
D011720:Pyrazoles; D013843:Thiazines