Synthesis, neuropsychopharmacological effects and analgesic-antiinflammatory activities of pyrrole analogues of lefetamine.
The synthesis of pyrrole analogues of the analgesic drug lefetamine is reported. These derivatives bear the 1-phenyl-2-(1H-pyrrol-1-yl)ethylamino moiety. Compounds were evaluated for analgesic activities in mice by the hot plate and Randall-Selitto tests. Antiinflammatory activity was tested by the carrageenan-induced rat paw edema method. General neuropsychopharmacological effects were also screened. The most interesting compound, N,N-dimethyl-1-phenyl-2-(1H-pyrrol-1-yl)ethylamine, showed an analgesic effect comparable to that of lefetamine, but devoid of the neurotoxicity of this drug.
Massa
S
S
Dipartimento di Studi Farmaceutici, Facoltà di Farmacia, Università degli Studi di Roma La Sapienza, Italy.
Stefancich
G
G
Artico
M
M
Corelli
F
F
Silvestri
R
R
Pantaleoni
G C
GC
Fanini
D
D
Palumbo
G
G
Giorgi
R
R
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis*; D000927:Anticonvulsants / Q000138:chemical synthesis; D055598:Chemical Phenomena; D002621:Chemistry; D005106:Exploratory Behavior / Q000187:drug effects; D005260:Female; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D009125:Muscle Relaxants, Central / Q000138:chemical synthesis; D010627:Phenethylamines / Q000138:chemical synthesis / Q000494:pharmacology*; D011597:Psychomotor Performance / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D011930:Reaction Time / Q000187:drug effects
D000894:Anti-Inflammatory Agents, Non-Steroidal; D000927:Anticonvulsants; D009125:Muscle Relaxants, Central; D010627:Phenethylamines; C011896:lephetamine