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2 results on '"Roberto Tomatis"'

1. Synthesis and Binding of 3-Aminopyridine Derivatives at Central Nicotinic Receptors

Author

Roberto Tomatis, Pier Andrea Borea, Gianfranco Balboni, Mauro Marastoni, and Stefania Merighi

Subjects
Central Nervous System, Male, Nicotine, Chemical Phenomena, 3-Aminopyridine, Stereochemistry, Aminopyridines, In Vitro Techniques, Receptors, Nicotinic, Chemical synthesis, Structure-Activity Relationship, chemistry.chemical_compound, Low affinity, Drug Discovery, Animals, Nicotinic Agonists, Rats, Wistar, Acetylcholine receptor, Cerebral Cortex, Nicotinic Receptors, Chemistry, Physical, Ligand, Rats, Nicotinic agonist, chemistry, Amine gas treating
Abstract

A series of secondary and tertiary pyridyl amides as potential central nicotinic acetylcholine receptors (nAChRs) ligands were prepared. Amides displayed negligible or very low affinity, whereas two amines achieved by reduction of corresponding secondary amides, showed affinity in the nanomolar range for nAChRs.

Published
2011
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2. Synthesis and Activity of New Acylated Diaminohydroxyalkanes as Human Immunodeficiency Virus Protease Inhibitors

Author

Mauro Marastoni, Roberto Tomatis, Fabrizio Bortolotti, and Martina Bazzaro

Subjects
Chemical Phenomena, Optical Rotation, Peptidomimetic, Stereochemistry, medicine.medical_treatment, Mass Spectrometry, Structure-Activity Relationship, Alkanes, Drug Discovery, medicine, Humans, HIV Protease Inhibitor, Structure–activity relationship, HIV-1 protease inhibitors, Peptidomimetics, Cells, Cultured, Chromatography, High Pressure Liquid, chemistry.chemical_classification, Protease, biology, Chemistry, Physical, Biological activity, HIV Protease Inhibitors, Amino acid, Enzyme, chemistry, Biochemistry, Enzyme inhibitor, HIV-1, biology.protein
Abstract

A series of HIV-1 protease inhibitors based on the lead compound Pc (IC50 = 165 nmol/l) with structural modifications at P1/P1' substituents or with a lengthening at its core unit were synthesized from amino acid starting materials. All analogues were less active than Pc against the protease.

Published
2011
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