Mariangela Biava

Summary

Affiliation: University of Rome
Country: Italy

Publications

  1. doi request reprint 1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings
    Mariangela Biava
    Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Universita La Sapienza, Piazzale A Moro 5, I 00185 Rome, Italy
    J Med Chem 51:3644-8. 2008
  2. doi request reprint Synthesis, in vitro, and in vivo biological evaluation and molecular docking simulations of chiral alcohol and ether derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents
    Mariangela Biava
    Dipartimento di Studi di Chimica e Tecnologie del Farmaco, Universita La Sapienza, Piazzale Aldo Moro, 5, I 00185 Roma, Italy
    Bioorg Med Chem 16:8072-81. 2008
  3. doi request reprint Identification of a novel pyrrole derivative endowed with antimycobacterial activity and protection index comparable to that of the current antitubercular drugs streptomycin and rifampin
    Mariangela Biava
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Universita La Sapienza, Piazzale Aldo Moro 5, I 00185 Roma, Italy
    Bioorg Med Chem 18:8076-84. 2010
  4. doi request reprint 1,5-Diaryl-2-ethyl pyrrole derivatives as antimycobacterial agents: design, synthesis, and microbiological evaluation
    Mariangela Biava
    Dipartimento di Chimica e Tecnologie del Farmaco, Universita La Sapienza, I 00185 Roma, Italy
    Eur J Med Chem 44:4734-8. 2009
  5. doi request reprint Novel ester and acid derivatives of the 1,5-diarylpyrrole scaffold as anti-inflammatory and analgesic agents. Synthesis and in vitro and in vivo biological evaluation
    Mariangela Biava
    Dipartimento di Studi di Chimica e Tecnologie del Farmaco, Universita La Sapienza, Piazzale Aldo Moro 5, I 00185 Roma, Italy
    J Med Chem 53:723-33. 2010
  6. ncbi request reprint Antimycobacterial agents. Novel diarylpyrrole derivatives of BM212 endowed with high activity toward Mycobacterium tuberculosis and low cytotoxicity
    Mariangela Biava
    Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Universita La Sapienza, P le A Moro 5, 00185 Rome, Italy
    J Med Chem 49:4946-52. 2006
  7. ncbi request reprint Cyclooxygenase-2 inhibitors. 1,5-diarylpyrrol-3-acetic esters with enhanced inhibitory activity toward cyclooxygenase-2 and improved cyclooxygenase-2/cyclooxygenase-1 selectivity
    Mariangela Biava
    Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Universita La Sapienza, Piazzale Aldo Moro 5, I 00185 Roma, Italy
    J Med Chem 50:5403-11. 2007
  8. doi request reprint Developing pyrrole-derived antimycobacterial agents: a rational lead optimization approach
    Mariangela Biava
    Dipartimento di Chimica e Tecnologia del Farmaco, Istituto Pasteur, Fondazione Cenci Bolognetti, Universita degli Studi di Roma La Sapienza, Piazzale A Moro 5, 00185 Roma, Italy
    ChemMedChem 6:593-9. 2011
  9. ncbi request reprint Antimycobacterial compounds. Optimization of the BM 212 structure, the lead compound for a new pyrrole derivative class
    Mariangela Biava
    Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Universita La Sapienza, P le A Moro 5, 00185 Rome, Italy
    Bioorg Med Chem 13:1221-30. 2005
  10. ncbi request reprint Antimycobacterial compounds. New pyrrole derivatives of BM212
    Mariangela Biava
    Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Universita La Sapienza, P le A Moro 5, 00185 Rome, Italy
    Bioorg Med Chem 12:1453-8. 2004

Detail Information

Publications18

  1. doi request reprint 1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings
    Mariangela Biava
    Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Universita La Sapienza, Piazzale A Moro 5, I 00185 Rome, Italy
    J Med Chem 51:3644-8. 2008
    ..The most active derivatives showed activity between 0.125-0.5 microg/mL (better than 16 and streptomycin) and protection index (64-256) higher than 16 (4) and similar to isoniazid and streptomycin (128)...
  2. doi request reprint Synthesis, in vitro, and in vivo biological evaluation and molecular docking simulations of chiral alcohol and ether derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents
    Mariangela Biava
    Dipartimento di Studi di Chimica e Tecnologie del Farmaco, Universita La Sapienza, Piazzale Aldo Moro, 5, I 00185 Roma, Italy
    Bioorg Med Chem 16:8072-81. 2008
    ..The affinity data have been rationalized through docking simulations...
  3. doi request reprint Identification of a novel pyrrole derivative endowed with antimycobacterial activity and protection index comparable to that of the current antitubercular drugs streptomycin and rifampin
    Mariangela Biava
    Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Universita La Sapienza, Piazzale Aldo Moro 5, I 00185 Roma, Italy
    Bioorg Med Chem 18:8076-84. 2010
    ..Antitubercular activity and protection index of the new compound are comparable to those found for the current antitubercular drugs streptomycin and rifampin...
  4. doi request reprint 1,5-Diaryl-2-ethyl pyrrole derivatives as antimycobacterial agents: design, synthesis, and microbiological evaluation
    Mariangela Biava
    Dipartimento di Chimica e Tecnologie del Farmaco, Universita La Sapienza, I 00185 Roma, Italy
    Eur J Med Chem 44:4734-8. 2009
    ..Also the remaining compounds were very active, although their MIC and PI were in general lower than those of their parent 2-methyl analogues...
  5. doi request reprint Novel ester and acid derivatives of the 1,5-diarylpyrrole scaffold as anti-inflammatory and analgesic agents. Synthesis and in vitro and in vivo biological evaluation
    Mariangela Biava
    Dipartimento di Studi di Chimica e Tecnologie del Farmaco, Universita La Sapienza, Piazzale Aldo Moro 5, I 00185 Roma, Italy
    J Med Chem 53:723-33. 2010
    ..Isopropyl-2-methyl-5-[4-(methylsulfonyl)phenyl]-1-phenyl-1H-pyrrole-3-acetate (10a), a representative member of the series, was selected for pharmacokinetic and metabolic studies...
  6. ncbi request reprint Antimycobacterial agents. Novel diarylpyrrole derivatives of BM212 endowed with high activity toward Mycobacterium tuberculosis and low cytotoxicity
    Mariangela Biava
    Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Universita La Sapienza, P le A Moro 5, 00185 Rome, Italy
    J Med Chem 49:4946-52. 2006
    ..Finally, molecular modeling studies were performed to rationalize the activity of the new compounds in terms of both superposition onto a pharmacophoric model for antitubercular compounds and their hydrophobic character...
  7. ncbi request reprint Cyclooxygenase-2 inhibitors. 1,5-diarylpyrrol-3-acetic esters with enhanced inhibitory activity toward cyclooxygenase-2 and improved cyclooxygenase-2/cyclooxygenase-1 selectivity
    Mariangela Biava
    Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Universita La Sapienza, Piazzale Aldo Moro 5, I 00185 Roma, Italy
    J Med Chem 50:5403-11. 2007
    ....
  8. doi request reprint Developing pyrrole-derived antimycobacterial agents: a rational lead optimization approach
    Mariangela Biava
    Dipartimento di Chimica e Tecnologia del Farmaco, Istituto Pasteur, Fondazione Cenci Bolognetti, Universita degli Studi di Roma La Sapienza, Piazzale A Moro 5, 00185 Roma, Italy
    ChemMedChem 6:593-9. 2011
    ..Some compounds identified are extremely promising and represent a step towards the design of novel lead structures in the fight against TB. Our efforts to this end are reviewed here...
  9. ncbi request reprint Antimycobacterial compounds. Optimization of the BM 212 structure, the lead compound for a new pyrrole derivative class
    Mariangela Biava
    Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Universita La Sapienza, P le A Moro 5, 00185 Rome, Italy
    Bioorg Med Chem 13:1221-30. 2005
    ..Microbiological data showed interesting in vitro activity toward Mycobacterium tuberculosis and atypical mycobacteria...
  10. ncbi request reprint Antimycobacterial compounds. New pyrrole derivatives of BM212
    Mariangela Biava
    Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Universita La Sapienza, P le A Moro 5, 00185 Rome, Italy
    Bioorg Med Chem 12:1453-8. 2004
    ..The microbiological data showed interesting in vitro activity against Mycobacterium tuberculosis and atypical mycobacteria...
  11. doi request reprint Improving the solubility of a new class of antiinflammatory pharmacodynamic hybrids, that release nitric oxide and inhibit cycloxygenase-2 isoenzyme
    Mariangela Biava
    Dipartimento di Chimica e Tecnologie del Farmaco, Universita La Sapienza, Piazzale Aldo Moro 5, I 00185 Roma, Italy
    Eur J Med Chem 58:287-98. 2012
    ..These molecules display enhanced nitric oxide releasing properties due to the presence of an ionisable moiety. The in vivo analgesic/anti-inflammatory activity was maintained in relation to the parent compounds...
  12. ncbi request reprint Importance of the thiomorpholine introduction in new pyrrole derivatives as antimycobacterial agents analogues of BM 212
    Mariangela Biava
    Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Universita La Sapienza, P le A Moro 5, 00185, Rome, Italy
    Bioorg Med Chem 11:515-20. 2003
    ..These findings prompted us to prepare new pyrrole derivatives 1-10 in the hope of increasing the activity. The microbiological data showed interesting in vitro activity against Mycobacterium tuberculosis and atypical mycobacteria...
  13. doi request reprint HPLC enantioseparation and absolute configuration of novel anti-inflammatory pyrrole derivatives
    Mariangela Biava
    Universita La Sapienza, Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, 00185 Rome, Italy
    Chirality 20:775-80. 2008
    ..The key step of our stereochemical characterization approach is the production at mg-scale of enantiomerically pure forms by HPLC on Chiralpak IA stationary phase...
  14. ncbi request reprint 1,5-Diarylpyrrole-3-acetic acids and esters as novel classes of potent and highly selective cyclooxygenase-2 inhibitors
    Mariangela Biava
    Dipartimento di Studi di Chimica e Tecnolgia delle Sostanze Biologicamente Attive, Universita La Sapienza, P le A Moro 5, I 00185 Roma, Italy
    J Med Chem 48:3428-32. 2005
    ..Some compounds proved to be highly selective COX-2 inhibitors, and their affinity data have been rationalized through docking simulations in terms of interactions with a crystallographic model of the COX-2 binding site...
  15. ncbi request reprint BM 212 and its derivatives as a new class of antimycobacterial active agents
    Mariangela Biava
    Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Universita La Sapienza, P le A Moro 5, 00185 Rome, Italy
    Curr Med Chem 9:1859-69. 2002
    ..On the base of microbiological results we have hypothesized a pharmacophore model that was also optimized. The rational design, and the evaluation of the in vitro activity against mycobacteria are described...
  16. doi request reprint Inhibition of Leishmania infantum Trypanothione Reductase by Azole-Based Compounds: a Comparative Analysis with Its Physiological Substrate by X-ray Crystallography
    Paola Baiocco
    Dipartimento di Scienze Biochimiche, Sapienza Universita di Roma, Piazzale A Moro 5, 00185 Roma Italy
    ChemMedChem 8:1175-83. 2013
    ..Analysis of the structure of LiTR in complex with trypanothione shows that Glu18 and Tyr110 are also involved in substrate binding, according to a competitive inhibition mechanism. ..
  17. doi request reprint C-9 Alkenylidine bridged macrolides: WO2008061189. Enanta Pharmaceuticals, Inc
    Giovanna Poce
    Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza University of Rome, Piazzale A Moro 5, I 00185 Rome, Italy
    Expert Opin Ther Pat 19:901-6. 2009
    ..discloses a series of novel C-9 alkenylidine bridged macrolides belonging to BBK. These compounds are 3,6- and 6,11-bicyclolides, which have the alkenylidine second anchor portion attached to C-9 of the molecule...
  18. doi request reprint Synthesis, biological evaluation, and enzyme docking simulations of 1,5-diarylpyrrole-3-alkoxyethyl ethers as selective cyclooxygenase-2 inhibitors endowed with anti-inflammatory and antinociceptive activity
    Maurizio Anzini
    Dipartimento Farmaco Chimico Tecnologico, Universita di Siena, Siena, Italy
    J Med Chem 51:4476-81. 2008
    ..0.5, GRID 21, and MacroModel 8.5 using the complex between COX-2 and SC-558 (1b), refined at a 3 A resolution (Brookhaven Protein Data Bank entry: 6cox )...