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2 results on '"Manetti, D"'

1. Design, synthesis and preliminary evaluation of a series of histone deacetylase inhibitors carrying a benzodiazepine ring.

Author

Guandalini, L., Balliu, M., Cellai, C., Martino, M.V., Nebbioso, A., Mercurio, C., Carafa, V., Bartolucci, G., Dei, S., Manetti, D., Teodori, E., Scapecchi, S., Altucci, L., Paoletti, F., and Romanelli, M.N.

Subjects
*HISTONE deacetylase inhibitors, *DRUG design, *BENZODIAZEPINES, *HYDROXAMIC acid derivatives, *ENZYME inhibitors, *THERAPEUTICS
Abstract

Abstract: A series of new histone deacetylase inhibitors were designed and synthesized based on hybridization between SAHA or oxamflatin and 5-phenyl-1,4-benzodiazepines. The compounds were tested for their enzyme inhibitory activity on HeLa nuclear extracts, and on human recombinant HDAC1 and HDAC6. Antiproliferative activity was tested on different cancer cells types, while proapoptotic activity was primarily tested on NB4 cells. The compounds showed IC50 values similar to those of SAHA. Compound (S)-8 displayed interesting activity against hematological and solid malignancies. [Copyright &y& Elsevier]

Published
2013
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2. Influence of ring size on the cognition-enhancing activity of DM235 and MN19, two potent nootropic drugs

Author

Guandalini, L., Martini, E., Di Cesare Mannelli, L., Dei, S., Manetti, D., Scapecchi, S., Teodori, E., Ghelardini, C., and Romanelli, M.N.

Subjects
*NOOTROPIC agents, *DRUG synergism, *PIPERIDINE, *DRUG efficacy, *MOLECULAR structure, *LABORATORY mice
Abstract

Abstract: A series of analogs of DM235 and MN19, characterized by rings with different size, have been prepared and evaluated for their nootropic activity in the mouse passive-avoidance test. It was found that the optimal ring size for the analogs of DM235, showing endocyclic both amidic groups, is 6 or 7 atoms. For the compounds structurally related to MN19, carrying an exocyclic amide group, the piperidine ring is the moiety which gives the most interesting compounds. [Copyright &y& Elsevier]

Published
2012
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