M L Bolognesi

Summary

Affiliation: University of Bologna
Country: Italy

Publications

  1. ncbi request reprint Polymethylene tetraamine backbone as template for the development of biologically active polyamines
    Carlo Melchiorre
    Dipartimento di Scienze Farmaceutiche, Alma Mater Studiorum Universita di Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    Med Res Rev 23:200-33. 2003
  2. doi request reprint Multi-target-directed ligands to combat neurodegenerative diseases
    Andrea Cavalli
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Bologna, Italy
    J Med Chem 51:347-72. 2008
  3. ncbi request reprint Multitarget-directed ligands: innovative chemical probes and therapeutic tools against Alzheimer's disease
    Maria Laura Bolognesi
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    Curr Top Med Chem 11:2797-806. 2011
  4. ncbi request reprint Polypharmacology in a single drug: multitarget drugs
    M L Bolognesi
    Department of Pharmacy and Biotechnology, Alma Mater Studiorum, University of Bologna, Via Belmeloro, 6, 40126 Bologna, Italy
    Curr Med Chem 20:1639-45. 2013
  5. doi request reprint Synthesis of a small library of 2-phenoxy-1,4-naphthoquinone and 2-phenoxy-1,4-anthraquinone derivatives bearing anti-trypanosomal and anti-leishmanial activity
    Maria Laura Bolognesi
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, Bologna University, Via Belmeloro 6, I 40126 Bologna, Italy
    Bioorg Med Chem Lett 18:2272-6. 2008
  6. doi request reprint Parallel synthesis and cytotoxicity evaluation of a polyamine-quinone conjugates library
    Maria Laura Bolognesi
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    J Med Chem 51:5463-7. 2008
  7. ncbi request reprint From dual binding site acetylcholinesterase inhibitors to multi-target-directed ligands (MTDLs): a step forward in the treatment of Alzheimer's disease
    Maria Laura Bolognesi
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    Mini Rev Med Chem 8:960-7. 2008
  8. ncbi request reprint MTDL design strategy in the context of Alzheimer's disease: from lipocrine to memoquin and beyond
    M L Bolognesi
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Bologna, Italy
    Curr Pharm Des 15:601-13. 2009
  9. doi request reprint Structure-activity relationships of memoquin: Influence of the chain chirality in the multi-target mechanism of action
    Maria Laura Bolognesi
    Department of Pharmaceutical Sciences, Alma Mater Studiorum Bologna University, Via Belmeloro 6, I 40126 Bologna, Italy
    Bioorg Med Chem Lett 19:4312-5. 2009
  10. doi request reprint Toward a rational design of multitarget-directed antioxidants: merging memoquin and lipoic acid molecular frameworks
    Maria Laura Bolognesi
    Department of Pharmaceutical Sciences, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    J Med Chem 52:7883-6. 2009

Detail Information

Publications38

  1. ncbi request reprint Polymethylene tetraamine backbone as template for the development of biologically active polyamines
    Carlo Melchiorre
    Dipartimento di Scienze Farmaceutiche, Alma Mater Studiorum Universita di Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    Med Res Rev 23:200-33. 2003
    ..Thus, these polyamines, such as caproctamine (78), could have potential in the investigation of Alzheimer disease...
  2. doi request reprint Multi-target-directed ligands to combat neurodegenerative diseases
    Andrea Cavalli
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Bologna, Italy
    J Med Chem 51:347-72. 2008
  3. ncbi request reprint Multitarget-directed ligands: innovative chemical probes and therapeutic tools against Alzheimer's disease
    Maria Laura Bolognesi
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    Curr Top Med Chem 11:2797-806. 2011
    ..Herein, we discuss several examples of both types of compounds, taken from our own research and derived from the leads memoquin, lipocrine and bis(7)tacrine...
  4. ncbi request reprint Polypharmacology in a single drug: multitarget drugs
    M L Bolognesi
    Department of Pharmacy and Biotechnology, Alma Mater Studiorum, University of Bologna, Via Belmeloro, 6, 40126 Bologna, Italy
    Curr Med Chem 20:1639-45. 2013
    ..This review article focuses on MTDs from a medicinal chemistry perspective. I will explore their use in current clinical practice, their likely application in the future, and the challenges to be overcome to achieve this goal...
  5. doi request reprint Synthesis of a small library of 2-phenoxy-1,4-naphthoquinone and 2-phenoxy-1,4-anthraquinone derivatives bearing anti-trypanosomal and anti-leishmanial activity
    Maria Laura Bolognesi
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, Bologna University, Via Belmeloro 6, I 40126 Bologna, Italy
    Bioorg Med Chem Lett 18:2272-6. 2008
    ..28microM, and IC(50)=1.26microM, respectively)...
  6. doi request reprint Parallel synthesis and cytotoxicity evaluation of a polyamine-quinone conjugates library
    Maria Laura Bolognesi
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    J Med Chem 51:5463-7. 2008
    ..Entry 1b caused apoptotic EGFR-mediated intracellular signaling. Thus, polyamino-quinones emerged as readily accessible and easily diversified scaffolds for anticancer lead discovery...
  7. ncbi request reprint From dual binding site acetylcholinesterase inhibitors to multi-target-directed ligands (MTDLs): a step forward in the treatment of Alzheimer's disease
    Maria Laura Bolognesi
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    Mini Rev Med Chem 8:960-7. 2008
    ..The rational modification of their structures to provide them with additional biological properties has emerged as a successful approach...
  8. ncbi request reprint MTDL design strategy in the context of Alzheimer's disease: from lipocrine to memoquin and beyond
    M L Bolognesi
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Bologna, Italy
    Curr Pharm Des 15:601-13. 2009
    ..The pivotal role played by this target in AD pathogenesis suggests that 12 may be a promising new chemical entity in the MTDL gold rush...
  9. doi request reprint Structure-activity relationships of memoquin: Influence of the chain chirality in the multi-target mechanism of action
    Maria Laura Bolognesi
    Department of Pharmaceutical Sciences, Alma Mater Studiorum Bologna University, Via Belmeloro 6, I 40126 Bologna, Italy
    Bioorg Med Chem Lett 19:4312-5. 2009
    ..The RR stereoisomer 2 resulted more effective than 1 in reverting two important effects mediated by acetylcholinesterase (AChE), that is, acetylcholine hydrolysis and AChE-induced amyloid-beta aggregation...
  10. doi request reprint Toward a rational design of multitarget-directed antioxidants: merging memoquin and lipoic acid molecular frameworks
    Maria Laura Bolognesi
    Department of Pharmaceutical Sciences, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    J Med Chem 52:7883-6. 2009
    ..They also displayed a balanced inhibitory profile against amyloid-beta aggregation and acetylcholinesterase, emerging as promising molecules for neuroprotectant lead discovery...
  11. doi request reprint Discovery of a class of diketopiperazines as antiprion compounds
    Maria Laura Bolognesi
    Department of Pharmaceutical Sciences, University of Bologna, Italy
    ChemMedChem 5:1324-34. 2010
    ..This investigation suggests that DKP based antiprion compounds can serve as a promising lead scaffold in developing new drugs to combat prion diseases...
  12. doi request reprint Multitargeted drugs discovery: balancing anti-amyloid and anticholinesterase capacity in a single chemical entity
    Maria Laura Bolognesi
    Department of Pharmaceutical Sciences Alma Mater Studiorum Bologna University, Via Belmeloro 6, 40126 Bologna, Italy
    Bioorg Med Chem Lett 21:2655-8. 2011
    ..By properly combining two or more distinct pharmacological properties in a molecule, we can achieve greater effectiveness compared to single-targeted drugs for investigating AD...
  13. ncbi request reprint Multi-target-directed ligands as innovative tools to combat trypanosomatid diseases
    Maria Laura Bolognesi
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro, 6, 40126 Bologna, Italy
    Curr Top Med Chem 11:2824-33. 2011
    ..Herein, I discuss the pros and cons of this approach, together with examples taken from the recent literature...
  14. doi request reprint Synthesis of monomeric derivatives to probe memoquin's bivalent interactions
    Maria Laura Bolognesi
    Department of Pharmaceutical Sciences, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    J Med Chem 54:8299-304. 2011
    ..The most potent monovalent ligand 2 also inhibits BACE-1 in vitro and APP metabolism in primary chicken telencephalic neurons...
  15. ncbi request reprint Multi-target-directed drug design strategy: from a dual binding site acetylcholinesterase inhibitor to a trifunctional compound against Alzheimer's disease
    Maria Laura Bolognesi
    Department of Pharmaceutical Sciences, A Mangini, Alma Mater Studiorum, Bologna University, Italy
    J Med Chem 50:6446-9. 2007
    ..The multifunctional compounds show activity against human AChE, are able to inhibit the AChE-induced amyloid-beta aggregation, and chelate metals, such as iron and copper...
  16. ncbi request reprint Propidium-based polyamine ligands as potent inhibitors of acetylcholinesterase and acetylcholinesterase-induced amyloid-beta aggregation
    Maria Laura Bolognesi
    Alma Mater Studiorum, University of Bologna, Department of Pharmaceutical Sciences, Via Belmeloro 6, 40126 Bologna, Italy
    J Med Chem 48:24-7. 2005
    ..Compound 4 emerged as the most potent heterodimer so far available to inhibit AChE-induced A beta aggregation...
  17. ncbi request reprint Novel class of quinone-bearing polyamines as multi-target-directed ligands to combat Alzheimer's disease
    Maria Laura Bolognesi
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, Italy
    J Med Chem 50:4882-97. 2007
    ....
  18. ncbi request reprint Heterocyclic inhibitors of AChE acylation and peripheral sites
    Maria Laura Bolognesi
    Dipartimento di Scienze Farmaceutiche, Via Belmeloro, 6, 40126 Bologna, Italy
    Farmaco 60:465-73. 2005
    ..The therapeutic potential of the dual site inhibithors in inhibiting amyloid-beta aggregatrion and deposition is also briefly summarised...
  19. doi request reprint Cystamine-tacrine dimer: a new multi-target-directed ligand as potential therapeutic agent for Alzheimer's disease treatment
    A Minarini
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    Neuropharmacology 62:997-1003. 2012
    ..This article is part of a Special Issue entitled 'Post-Traumatic Stress Disorder'...
  20. ncbi request reprint Design, synthesis, and biological activity of methoctramine-related polyamines as putative G(i) protein activators
    C Melchiorre
    Department of Pharmaceutical Sciences, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    J Med Chem 44:4035-8. 2001
    ....
  21. ncbi request reprint Hexahydrochromeno[4,3-b]pyrrole derivatives as acetylcholinesterase inhibitors
    M L Bolognesi
    Department of Pharmaceutical Sciences, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    J Med Chem 44:105-9. 2001
    ..The two enantiomers of 4, (-)-4 and (+)-4, did not show a marked enantioselectivity. Finally, a similar time-dependent pattern of inhibition of AChE was observed for 3 and 4...
  22. ncbi request reprint Tacrine derivatives and Alzheimer's disease
    V Tumiatti
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    Curr Med Chem 17:1825-38. 2010
    ..This review will focus on and summarize the last two years of research into the development of tacrine derivatives able to hit AD targets beyond simple AChE inhibition...
  23. doi request reprint Polyamine conjugation of curcumin analogues toward the discovery of mitochondria-directed neuroprotective agents
    Elena Simoni
    Department of Pharmaceutical Sciences, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    J Med Chem 53:7264-8. 2010
    ..It also resulted in a significant decrease in the cytotoxicity effects. 2-5 are therefore promising molecules for neuroprotectant lead discovery...
  24. pmc Analysis of the muscarinic receptor subtype mediating inhibition of the neurogenic contractions in rabbit isolated vas deferens by a series of polymethylene tetra-amines
    R Budriesi
    Department of Pharmaceutical Sciences, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    Br J Pharmacol 132:1009-16. 2001
    ..This supports the view that the muscarinic receptor mediating inhibition of neurogenic contractions of rabbit vas deferens may not belong to the M(1) type but rather appears to be of the M(4) subtype...
  25. ncbi request reprint A small molecule targeting the multifactorial nature of Alzheimer's disease
    Andrea Cavalli
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro, 6, 40126 Bologna, Italy
    Angew Chem Int Ed Engl 46:3689-92. 2007
  26. ncbi request reprint Design, synthesis, and biological evaluation of conformationally restricted rivastigmine analogues
    Maria Laura Bolognesi
    Department of Pharmaceutical Sciences, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    J Med Chem 47:5945-52. 2004
    ....
  27. ncbi request reprint Analogues of prazosin that bear a benextramine-related polyamine backbone exhibit different antagonism toward alpha1-adrenoreceptor subtypes
    M L Bolognesi
    Department of Pharmaceutical Sciences, University of Bologna, Italy
    J Med Chem 44:362-71. 2001
    ..Finally, the effect of nonbasic substituents on the phenyl ring of prazosin analogues 16-28 on potency and selectivity for the different subtypes can hardly be rationalized...
  28. doi request reprint Memoquin: a multi-target-directed ligand as an innovative therapeutic opportunity for Alzheimer's disease
    Maria Laura Bolognesi
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, 40126 Bologna, Italy
    Neurotherapeutics 6:152-62. 2009
    ..The in vitro and in vivo biological profile of memoquin demonstrates the suitability of the new strategy for obtaining innovative drug candidates for the treatment of neurodegenerative diseases...
  29. ncbi request reprint A new EGFR inhibitor induces apoptosis in colon cancer cells
    N Calonghi
    Department of Biochemistry G Moruzzi, University of Bologna, Bologna, Italy
    Biochem Biophys Res Commun 354:409-13. 2007
    ..At concentration ranging from 30 nM to 5 microM, it activates apoptosis. FR18 seems therefore to have possible therapeutic applications in colon cancer...
  30. ncbi request reprint Multitarget-directed drug design strategy: a novel molecule designed to block epidermal growth factor receptor (EGFR) and to exert proapoptotic effects
    Alessandra Antonello
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    J Med Chem 49:6642-5. 2006
    ..The novel molecules were synthesized by combining the structural features of the EGFR inhibitor PD153035 (1) and lipoic acid, which among other therapeutic effects triggers apoptosis in human cancer cells...
  31. ncbi request reprint Design, synthesis and biological evaluation of ambenonium derivatives as AChE inhibitors
    Maria Laura Bolognesi
    Department of Pharmaceutical Sciences, University of Bologna, Via Belmeloro 6, I 40126 Bologna, Italy
    Farmaco 58:917-28. 2003
    ..To better clarify the interactions that account for the high affinity of 1, docking simulations and molecular dynamics studies on the AChE-1 complex were also carried out...
  32. doi request reprint Synthetic polyamines: an overview of their multiple biological activities
    Anna Minarini
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, 40126, Bologna, Italy
    Amino Acids 38:383-92. 2010
    ....
  33. doi request reprint Complementary medicinal chemistry-driven strategies toward new antitrypanosomal and antileishmanial lead drug candidates
    Andrea Cavalli
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Bologna, Italy
    FEMS Immunol Med Microbiol 58:51-60. 2010
    ..A combination of both approaches to hopefully overcome some of the challenges of anti-trypanosomatid drug discovery has eventually been proposed...
  34. doi request reprint Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer
    Vincenzo Tumiatti
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    J Med Chem 51:7308-12. 2008
    ..15 was the most interesting, inhibiting AChE in the nanomolar range and inhibiting AChE-induced and self-promoted beta-amyloid aggregation in the micromolar range...
  35. doi request reprint Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics
    Anna Minarini
    Department of Pharmaceutical Sciences, Alma Mater Studiorum University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    Bioorg Med Chem 16:7311-20. 2008
    ..Rather, compounds 3-6 displayed a reversed selectivity showing more affinity at the muscarinic M(2) receptor than at all the other subtypes tested...
  36. ncbi request reprint Insight into the kinetic of amyloid beta (1-42) peptide self-aggregation: elucidation of inhibitors' mechanism of action
    Manuela Bartolini
    Department of Pharmaceutical Sciences, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    Chembiochem 8:2152-61. 2007
    ....
  37. doi request reprint Investigation of the photostability properties of memoquin, a quinone derivative for the treatment of Alzheimer's disease
    Francesca Mancini
    Department of Pharmaceutical Sciences, Via Belmeloro 6, University of Bologna, 40126 Bologna, Italy
    J Pharm Biomed Anal 50:164-70. 2009
    ..Conversely, memoquin was found to be stable in the dark. These results suggest that, with appropriate handling and storage, memoquin's activity is not impaired...
  38. doi request reprint Privileged structure-guided synthesis of quinazoline derivatives as inhibitors of trypanothione reductase
    Andrea Cavalli
    Department of Pharmaceutical Sciences, Alma Mater Studiorum Bologna University, Bologna, Italy
    Bioorg Med Chem Lett 19:3031-5. 2009
    ..Furthermore, the use of privileged motifs might emerge as an innovative approach to antiparasitic lead candidates...