Francesca Magnanini

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We report the design, synthesis, QSPR and QSAR of a new class of H(3)-antagonists, having a 2-aminobenzimidazole moiety connected to the 4(5) position of an imidazole ring through di- or tri-methylene chains. Eleven substituents, selected by experimental design to obtain broad and non-correlated variation in their lipophilic, electronic and steric(More)
Two new GABA derivatives, 1 and 2, were synthesized and tested for their capacity to display CNS activity, which was assessed by determining the effects on the duration of pentobarbital-induced hypnosis in rats. Compound 1, peripherally injected, significantly prolonged the hypnosis time, a typical GABA-mimetic effect, while both intracerebroventricular and(More)
H3-antagonists possess promising pharmacological effects on awakening, learning and memory, but few data on their access to the central nervous system (CNS) have been reported so far. The purpose of this work was to investigate the relationships between structure and brain penetration of a series of H3-antagonists, using ex vivo binding experiments in rats.(More)
A series of 2-methoxy-5H[1]benzopyrano[4,3-d]pyrimidin-5-amines were prepared and screened for their in vitro antiplatelet activity inducing the aggregation by ADP, arachidonic acid (AA) and collagen. In vivo experiments were performed in order to evaluate their antiphlogistic, analgesic and antipyretic activities. Title compounds showed antiplatelet(More)
PTC was performed in 86 patients with obstructive jaundice, between February/80--March/81 diagnosing 20 cases of the hepatic hilium carcinoma, 14 of pancreatic carcinoma, and 2 multiplex abscess of the liver. PTC-D was successfully attempted on 16 patients, catheterizing the intrahepatic biliary tree in 15 and maintaining a good biliary flow in 10 of them.(More)
Several experimental findings suggest that histamine H3antagonists are potentially useful for the treatment of central disorders such as attention/learning disabilities, narcolepsy and epilepsy [1]. An essential requirement for such use is easy penetration into the central nervous system (CNS). Using the ex vivo binding technique in rats, we evaluated CNS(More)
It has been recently reported that compounds composed of an imidazole connected through an alkyl spacer to a 2-aminobenzimidazole showed high affinity towards the H(3)-receptor. The guanidine fragment of the 2-aminobenzimidazole is probably involved in hydrogen bond interactions at the binding site, and is referred to as the 'polar fragment'. In the present(More)