Journal of Medicinal Chemistry p. 4214 - 4220 (1993)
Update date:2022-08-04
Topics:
Pinza
Farina
Cerri
Pfeiffer
Riccaboni
Banfi
Biagetti
Pozzi
Magnani
Dorigotti
A series of dihydro-1H-pyrrolo[1,2-a]imidazole-2,5(3H,6H)-diones were synthesized. These bicylic derivatives contain both the 2-pyrrolidinone and 4-imidazolidinone nuclei, already recognized as important for cognition enhancing activity. In addition, these structures maintain the backbone of piracetam and oxiracetam with the acetamide side chain restricted in a folded conformation. Their ability to reverse scopolamine-induced amnesia was assessed in a one trial, step-through, passive avoidance paradigm. The main features observed are a potent antiamnestic activity after ip administration (minimal effective dose being between 0.3 and 1 mg/kg ip for most compounds), the presence of a bell-shaped dose-response curve and, generally, a reduction of biological activity after po administration. However, the unsubstituted compound (15, dimiracetam) shows no evidence of a bell-shaped dose-response curve and completely retains activity when given orally, being 10-30 times more potent than the reference drug oxiracetam.
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Doi:10.1007/BF00780407
(1993)Doi:10.1039/CC9960000349
(1996)Doi:10.1021/jo00078a032
(1993)Doi:10.1016/0223-5234(94)90122-8
(1994)Doi:10.1016/S0040-4039(00)91819-7
(1993)Doi:10.1021/acsmedchemlett.9b00515
(2020)