Design, synthesis and nootropic activity of new analogues of sunifiram and sapunifiram, two potent cognition-enhancers.
A series of amides and sulfonamides, structurally related to DM235 (sunifiram) and MN19 (sapunifiram), derived by ring expansion or contraction, or by inversion of the exocyclic amide function, have been synthesized and tested for cognition-enhancing activity in the mouse passive-avoidance test. Some of the compounds display good antiamnesic and procognitive activity, with higher potency than piracetam, and with a potency similar to the parent compounds.
Department of Pharmaceutical Sciences, Laboratory of Design, Synthesis and Study of Biologically Active Heterocycles (HeteroBioLab), University of Florence, 50019 Sesto Fiorentino, Italy.
Elisabetta
E
Martini
Alberto
A
Salvicchi
Carla
C
Ghelardini
Dina
D
Manetti
Silvia
S
Dei
Luca
L
Guandalini
Cecilia
C
Martelli
Michele
M
Melchiorre
Cristina
C
Cellai
Serena
S
Scapecchi
Elisabetta
E
Teodori
Maria Novella
MN
Romanelli
D000818:Animals; D003071:Cognition / Q000187:drug effects*; D004195:Disease Models, Animal; D015195:Drug Design; D051379:Mice; D018697:Nootropic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D018697:Nootropic Agents; D010879:Piperazines; D013449:Sulfonamides; C545789:sapunifiram; C416655:DM 235