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139 results on '"La Colla P"'

1. Synthesis and Biological Evaluation of New 3-Phenyl-1-[(4-arylpiperazin-1-yl)alkyl]- piperidine-2,6-diones

Author

Loddo R, La Colla P, Anna Bielenica, Jerzy Kossakowski, Ibba C, Izabela Dybała, and Struga M

Subjects
chemistry.chemical_classification, Antifungal, 3-Phenylpiperidine-2,6-dione, Stereochemistry, medicine.drug_class, Cytotoxicity, Pharmaceutical Science, Combinatorial chemistry, In vitro, chemistry.chemical_compound, chemistry, medicine, Piperidine, Antiviral activity, Alkyl, Research Article, X-ray crystallography, Biological evaluation
Abstract

A set of 13 alkyl derivatives of 3-phenylpiperidine-2,6-dione were synthesized. Newly obtained compounds were investigated in vitro against HIV-1 and other selected viruses. The benzyl 3f and fluorophenyl 3g derivatives showed moderate protection against CVB-2 and the compound 3g also against HSV-1. Derivatives were tested also for their antibacterial and antifungal activity. The molecular structures of 3a and 3d were determined by an X-ray analysis.

Published
2011
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2. 2,3-Dihydro-1,2-Diphenyl-substituted 4H-Pyridinone Derivatives as New Anti Flaviviridae Inhibitors

Author

Peduto, A, Massa, A, Di Mola, A, de Caprariis, P, La Colla, P, Loddo, R, Altamura, S, Maga, G, FILOSA, Rosanna, Peduto, A, Massa, A, Di Mola, A, de Caprariis, P, La Colla, P, Loddo, R, Altamura, S, Maga, G, and Filosa, Rosanna

Subjects
3-dihydro-1, flavivirus, viruses, 2-diphenyl-substituted 4H-pyridinone
Abstract

With the aim of identifying novel lead compounds active against emergent human infectious diseases, a series of 2,3-dihydro-4H-pyridinone derivatives has been prepared and evaluated for antiviral activity. Compounds were evaluated in vitro in cell-based assays for cytotoxicity and against a wide spectrum of viruses. In the antiviral screening, several compounds showed to be fairly active against viruses belonging to the Flaviviridae family. The Pestiviruses (bovine viral diarrhoea virus) were inhibited by 4acis (CC(50) > 100 mu m; EC(50) = 14 mu m), compounds 4ccis and 6a showed a significant activity against Flaviviruses (Yellow Fever Virus) (CC(50) > 100 mu m; EC(50) = 18 mu m, CC(50) > 100 mu m; EC(50) = 10 mu m). Among these, compound 6a displayed great inhibitory activity against Hepaciviruses (hepatitis C virus) in replicon assay [CC(50) > 100 mu m; EC(50)(1b) = 4 mu m]. In vitro inhibitory activity against the HCV RNA-dependent RNA polymerase (NS5B) of title compounds is discussed. The antiviral screening of viral strains indicated that compound 6a can be selected as promising tool in novel anti-flaviviruses development.

Published
2011

3. Antiviral and cytotoxic activities of aminoarylazo compoundsand aryltriazene derivatives

Author

Tonelli, M, Vazzana, I, Tasso, B, Boido, V, Sparatore, F, Fermeglia, Maurizio, Paneni, Maria Silvia, Posocco, Paola, Pricl, Sabrina, LA COLLA, P, Ibba, C, Secci, B, Collu, G, Loddo, R., Tonelli, M, Vazzana, I, Tasso, B, Boido, V, Sparatore, F, Fermeglia, Maurizio, Paneni, Maria Silvia, Posocco, Paola, Pricl, Sabrina, LA COLLA, P, Ibba, C, Secci, B, Collu, G, and Loddo, R.

Subjects
antiviral research
Published
2009

4. Isolation and characterisation of novel surface active compound-producing bacteria

Author

Tamburini, E, Ruggeri, C, Berta, M, Pintus, M, Sergi, S, La Colla, P., FRANZETTI, ANDREA, BESTETTI, GIUSEPPINA, Tamburini, E, Ruggeri, C, Franzetti, A, Bestetti, G, Berta, M, Pintus, M, Sergi, S, and La Colla, P

Subjects
compound-producing bacteria, novel surface active, BIO/19 - MICROBIOLOGIA GENERALE
Published
2009

6. Biodiversity of new surface active compound-producing bacteria

Author

Ruggeri, C, La Colla, P, Berta, M, Pintus, M, Sergi, S, Tamburini, E., FRANZETTI, ANDREA, BESTETTI, GIUSEPPINA, Ruggeri, C, Franzetti, A, Bestetti, G, La Colla, P, Berta, M, Pintus, M, Sergi, S, and Tamburini, E

Subjects
surface active, bacteria, BIO/19 - MICROBIOLOGIA GENERALE
Abstract

ANALYSIS OF THE PHYLOGENETIC DIVERSITY OF NEW SURFACE ACTIVE COMPOUND-PRODUCING BACTERIA

Published
2009

7. Design, synthesis and anti flaviviridae activity of N6-, -O- and 5 O-substituted adenine nucleoside analogs

Author

ANGUSTI A, MANFREDINI S, DURINI E, CILIBERTI N, VERTUANI S, SOLAROLI N, LODDO R, SECCI B, VISIOLI A, SANNA T, COLLU G, PEZZULLO M, LA COLLA P., PRICL, SABRINA, FERRONE, MARCO, FERMEGLIA, MAURIZIO, Angusti, A, Manfredini, S, Durini, E, Ciliberti, N, Vertuani, S, Solaroli, N, Pricl, Sabrina, Ferrone, Marco, Fermeglia, Maurizio, Loddo, R, Secci, B, Visioli, A, Sanna, T, Collu, G, Pezzullo, M, and LA COLLA, P.

Published
2008

9. Pyrazole Related Nucleosides 5.1Synthesis and Biological Activity of 2′-Deoxy- 2′, 3′-dideoxy- and Acyclo-analogues of 4-Iodo-1-β-D-ribofuranosyl-3-carboxymethyl Pyrazole (IPCAR)

Author

Demontis F, Pier Giovanni Baraldi, Silvia Vertuani, L. Vargiu, Stefano Manfredini, La Colla P, Elisa Durini, Tiziana Marceddu, Alessandra Pani, and R. Bazzanini

Subjects
chemistry.chemical_compound, Chemistry, Stereochemistry, Genetics, Molecular Medicine, Structure–activity relationship, Moiety, Biological activity, General Medicine, Pyrazole, Biochemistry, Medicinal chemistry
Abstract

Continuing our studies on the structure-activity relationships (SAR) of 4-iodo-1-beta-D-ribofuranosyl-3-carboxymethyl pyrazole (IPCAR), the ribofuranosyl moiety has been substituted with acyclic chains, namely 1-[(2-hydroxyethoxy)methyl]- and 1-[(1,3-dihydroxy-2-propoxy)methyl]-pyrazole derivatives (4, 5 and 8, 9 respectively), with the 2'-deoxy-beta-D-ribofuranosyl group (12 and 13) and finally with the 2',3'-dideoxy-D-glycero-pentofuranosyl-moiety (16 and 17). None of the new compounds display any interesting biological activity.

Published
2000
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10. Surface-active compounds and their role in the access to hydrocarbons in Gordonia strains

Author

FRANZETTI, ANDREA, BESTETTI, GIUSEPPINA, Caredda, P, La Colla, P, Tamburini, E., Franzetti, A, Bestetti, G, Caredda, P, La Colla, P, and Tamburini, E

Subjects
Sequence Analysis, RNA, Surface Properties, biosurfactant, BIO/19 - MICROBIOLOGIA GENERALE, Bacterial Adhesion, Hydrocarbons, RNA, Bacterial, Surface-Active Agents, Biodegradation, Environmental, RNA, Ribosomal, 16S, Soil Pollutants, Gordonia Bacterium, Hydrophobic and Hydrophilic Interactions, Sequence Alignment, Phylogeny
Abstract

Three new bacterial strains (M22, BS25 and BS29) belonging to the Gordonia genus were isolated from a site chronically contaminated by diesel. Those Gordonia strains were able to grow using a wide range of straight and branched aliphatic hydrocarbons as carbon and energy sources and to produce at least two classes of surface-active compounds. Emulsifying agents were released in the culture medium when bacteria grew both on hydrocarbons and water-soluble substrates. Cell-bound biosurfactants, which reduce the surface tension, were produced on hydrocarbons; however, their production was significantly lower on water soluble substrates. The relationship of growth phase, surface-active compound production and cell-surface properties was analyzed in kinetic experiments on hydrocarbons. Gordonia sp. BS29 synthesized, and released extracellularly, bioemulsans during the exponential phase with n-hexadecane as carbon and energy source. The production of biosurfactants started in the exponential phase and their concentration increased during the following linear growth. Furthermore, the adhesion of bacterial cells to hydrocarbons decreased during growth. Our results led us to hypothesize a change in the mode by which Gordonia cells access the substrate during growth on hydrocarbons. © 2007 Federation of European Microbiological Societies.

Published
2007

12. Laboratory Tests and Bioremediation of a Chronically Diesel-Contaminated Site

Author

Caredda, P, La Colla, P, Tamburini, E, Viola, A, Suardi, A, FRANZETTI, ANDREA, BESTETTI, GIUSEPPINA, Caredda, P, La Colla, P, Tamburini, E, Viola, A, Suardi, A, Franzetti, A, and Bestetti, G

Subjects
bioremediation, diesel
Abstract

The investigated contaminated site is situated in the proximity of a former crude oil refinery. Contamination took place in the 1970s, following the spilling of huge amount of diesel. GC/MS analyses demonstrate that the major components of nonaqueous liquid phase contaminant mixture are branched alkanes and alkyl-substituted naphthalenes. In the site, bioslurping technology was under experimental investigation. The aim of this work was: (1) to evaluate whether the weathered diesel hydrocarbons present as residual contamination can be further degraded by stimulation of indigenous microorganisms; (2) to monitor the effect of the bioslurping on the hydrocarbondegrading bacterial community; and (3) to characterize the weathered diesel-degrading bacterial community. Enumeration of hydrocarbon-degrading bacteria and respirometric tests were carried out during bioslurping treatment. An increase in number and metabolic activity of degrading bacteria was demonstrated. Hydrocarbon-degrading bacteria enriched from capillary fringe and from the NAPL samples were isolated and characterized by 16S ribosomal RNA gene analysis. The majority of the isolates were assigned to the Actinomycetales or to the Rhizobiales orders. A new Gordonia strain (M22) was selected and its degradation capabilities were evaluated. Gordonia sp. M22 strain was capable of degrading the major components of the contaminant mixture.

Published
2007

13. Design, synthesis and preliminary in vitro and in silico antiviral activity of [4,7]phenantrolines and 1-oxo-1,4-dihydro-[4,7]phenantrolines against a single-stranded positive sense RNA genome viruses

Author

CARTA A, LORIGA M, PAGLIETTI G, SANNA T, IBBA C, LA COLLA P, LODDO R., FERRONE, MARCO, FERMEGLIA, MAURIZIO, PRICL, SABRINA, Carta, A, Loriga, M, Paglietti, G, Ferrone, Marco, Fermeglia, Maurizio, Pricl, Sabrina, Sanna, T, Ibba, C, LA COLLA, P, and Loddo, R.

Subjects
Antiviral Agents
Published
2007

14. Chasing the evaders. Design, synthesis, activity and molecular modelling of a new small molecule with activity against drug-resistant HIV-1-mutants

Author

Pricl, Sabrina, Ferrone, Marco, Posocco, Paola, Fermeglia, Maurizio, Sanna, G., Collu, G., La Colla, P., Loddo, R., Sias, A., Piras, S., Carta, A., Pricl, Sabrina, Ferrone, Marco, Posocco, Paola, Fermeglia, Maurizio, Sanna, G., Collu, G., La Colla, P., Loddo, R., Sias, A., Piras, S., and Carta, A.

Subjects
reverse transcriptase, hiv, Computer simulation
Published
2006

15. A new twist for an old song. The DABO story revisited

Author

Pricl, Sabrina, Ferrone, Marco, Posocco, Paola, Pavan, G. M., Fermeglia, Maurizio, La Colla, P., Loddo, R., Pricl, Sabrina, Ferrone, Marco, Posocco, Paola, Pavan, G. M., Fermeglia, Maurizio, La Colla, P., and Loddo, R.

Subjects
hiv, reverse transcriptase, computer simulation
Published
2006

16. Hindered nucleoside analogs as hinibitors of HCV RNA-dependent RNA-polymerase: evolving vistas

Author

MANFREDINI S., ANGUSTI A., CILIBERTI N., DURINI E., VERTUANI S., BUZZONI L., COSLANICH A., FERMEGLIA, MAURIZIO, FERRONE M., PANENI M. S., LA COLLA P., SANNA G., CADEDDU A., MURA M., LODDO R., PRICL, SABRINA, SCHINAZI, R., E. SCHIFF, Manfredini, S., Angusti, A., Ciliberti, N., Durini, E., Vertuani, S., Buzzoni, L., Coslanich, A., Fermeglia, Maurizio, Ferrone, M., Paneni, M. S., Pricl, Sabrina, LA COLLA, P., Sanna, G., Cadeddu, A., Mura, M., and Loddo, R.

Published
2005

17. Three-dimensional Pharmacophore Modeling of Hindered Nucleoside Analogs (HNAs) as Inhibitors of the Hepatitis C virus NS5B Polymerase

Author

Ferrone, Marco, Pricl, Sabrina, Fermeglia, Maurizio, Paneni, Maria Silvia, Angusti, A., Ciliberti, N., Buzzoni, L., Durini, E., Vertuani, S., Manfredini, S., Loddo, R., La Colla, P., Ferrone, Marco, Pricl, Sabrina, Fermeglia, Maurizio, Paneni, Maria Silvia, Angusti, A., Ciliberti, N., Buzzoni, L., Durini, E., Vertuani, S., Manfredini, S., Loddo, R., and La Colla, P.

Subjects
HCV, computer-assisted drug design
Published
2005

18. Non-nucleoside anti-Flaviviridae agents from different molecular classes: a jointed experimental/modeling effort

Author

Angusti A., Auzzas L., Boido V., Canu C., Carta A., Ciliberti N., Loddo R., La Colla P., Loriga M., Manfredini S., Mazzei M., Nieddu E., Paglietti G., Paneni M. S., Rassu G., Sparatore F., Tasso B., Vitale G., FERRONE, MARCO, PRICL, SABRINA, Angusti, A., Auzzas, L., Boido, V., Canu, C., Carta, A., Ciliberti, N., Ferrone, Marco, Loddo, R., La Colla, P., Loriga, M., Manfredini, S., Mazzei, M., Nieddu, E., Paglietti, G., Paneni, M. S., Pricl, Sabrina, Rassu, G., Sparatore, F., Tasso, B., and Vitale, G.

Subjects
HCV, RdRp inhibitors, computer-assisted drug design, RdRp inhibitor
Published
2005

20. 'Fatty' nucleoside analogs as HCV NS5b inhibitors

Author

PRICL, SABRINA, FERMEGLIA, MAURIZIO, FERRONE, MARCO, COSLANICH, ALESSANDRO, PANENI, Maria Silvia, Manfredini S., Angusti A., La Colla P., Mura M., AIChE, Pricl, Sabrina, Fermeglia, Maurizio, Ferrone, Marco, Coslanich, Alessandro, Paneni, Maria Silvia, Manfredini, S., Angusti, A., La Colla, P., and Mura, M.

Subjects
HCV, RdRp inhibitors, computer-assisted drug design, RdRp inhibitor
Published
2004

21. Hindered Nucleoside Analogs (HNA) as Antiflaviviridae Agents

Author

Manfredini, S., Angusti, A., Veronese, A. C., Durini, E., Vertuani, S., Nalin, F., Solaroli, N., Ferrone, Marco, Pricl, Sabrina, Mura, M., Piano, M. A., Poddesu, B., Cadeddu, A., LA COLLA, P., Loddo, R., Manfredini, S., Angusti, A., VERONESE A., C, Durini, E., Vertuani, S., Nalin, F., Solaroli, N., Ferrone, Marco, Pricl, Sabrina, Mura, M., PIANO M., A, Poddesu, B., Cadeddu, A., LA COLLA, P., and Loddo, R.

Published
2004

22. Prediction fo HIV-1 resistance to NNRITs: a computer-aided molecular-based rationale

Author

Pricl, Sabrina, Coslanich, Alessandro, Fermeglia, Maurizio, Ferrone, Marco, Paneni, Maria Silvia, Loddo, R., Cabizza, A., Sanna, G., Murreddu, M., La Colla, P., Pricl, Sabrina, Coslanich, Alessandro, Fermeglia, Maurizio, Ferrone, Marco, Paneni, Maria Silvia, Loddo, R., Cabizza, A., Sanna, G., Murreddu, M., and La Colla, P.

Subjects
antiviral drug design, HIV, computer-assisted drug design
Published
2004

23. Synthesis of a New Series of Nucleoside Analogs with Antiflaviviridae Activity and Their Interaction with RNA-Dependent RNA-Polymerase

Author

Pricl, S., Coslanich, A., Fermeglia, M., Ferrone, M., Merzek, M., Angusti, Angela, Ciliberti, Nunzia, Durini, Elisa, Stefano Manfredini, Musiu, C., Marco Mura, Loddo, R., La Colla, P., Pricl, Sabrina, Coslanich, A., Fermeglia, Maurizio, Ferrone, Marco, Merzek, M., Angusti, A., Ciliberti, N., Durini, E., Manfredini, S., Musiu, C., Mura, M., Loddo, R., and La Colla, P.

Subjects
antiviral drug, HCV, computer assistged drug design
Published
2003

25. Antitumor agents. 1. Synthesis, Biological evaluation and molecular modeling of 5H-pyrido[3,2-a]phenoxazin-5-one, a new actynomicin D analog with potent antiproliferative activity

Author

BOLOGNESE A., CORREALE G., MANFRA M., LAVECCHIA A., MAZZONI O., NOVELLINO E., LA COLLA P., LODDO R., MURGIONI C., PANI A., SERRA I., SETZU G., BARONE, VINCENZO, Bolognese, A., Correale, G., Manfra, M., Lavecchia, A., Mazzoni, O., Novellino, E., Barone, Vincenzo, LA COLLA, P., Loddo, R., Murgioni, C., Pani, A., Serra, I., and Setzu, G.

Published
2002

26. Structure-Based Design, Synthesis and Biological Evaluation of Conformationally Restricted Novel 2-Alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones (S-DABOs) as Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase

Author

MAI A., SBARDELLA G., ARTICO M., RAGNO R., MASSA S., MUSIU C., LA COLLA M., MURGIONI C., LA COLLA P., LODDO R., NOVELLINO, ETTORE, GRECO, GIOVANNI, LAVECCHIA, ANTONIO, Mai, A., Sbardella, G., Artico, M., Ragno, R., Massa, S., Novellino, Ettore, Greco, Giovanni, Lavecchia, Antonio, Musiu, C., LA COLLA, M., Murgioni, C., LA COLLA, P., and Loddo, R.

Published
2001

27. Synthesis and Biological Evaluation of 5H-Indolo[3,2-b]benzothiazepine Derivatives, Designed as Conformationally Constrained Analogues of the Human Immunodeficiency Virus Type 1 Reverse Transcriptase Inhibitor L-737,126

Author

Silvestri R., Artico M., Bruno B., Massa S., Marongiu M. E., Pani A., De Montis A., La Colla P., NOVELLINO, ETTORE, GRECO, GIOVANNI, Silvestri, R., Artico, M., Bruno, B., Massa, S., Novellino, Ettore, Greco, Giovanni, Marongiu, M. E., Pani, A., De Montis, A., and La Colla, P.

Published
1998

30. Structure-based Design, Parallel Synthesis, SAR and Molecular Modelling Studies of Thiocarbamates, New Potent Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitor Isosteres of Phenethylthiazolylthiourea (PETT) Derivatives

Author

Ranise, Angelo, Spallarossa, Andrea, Cesarini, Sara, Bondavalli, Francesco, Schenone, Silvia, Bruno, Olga, Menozzi, Giulia, Fossa, Paola, Mosti, Luisa, LA COLLA, M., Sanna, G., Murreddu, M., Collu, G., Busonera, B., Marongiu, M. E., Pani, A., LA COLLA, P., and Loddo, R.

Subjects
molecular modeling, HIV-1, reverse transcriptase inhibitor
Published
2005

35. 2,6-Bis(3,4,5-trihydroxybenzylydene) derivatives of cyclohexanone: novel potent HIV-1 integrase inhibitors that prevent HIV-1 multiplication in cell-based assays

Author

Costi, Roberta, DI SANTO, Roberto, Artico, Marino, Massa, S., Ragno, Rino, Loddo, R., La Colla, M., Tramomtano, E., La Colla, P., and Pani, A.

Subjects
anti-hiv-1-in agents, Anti-HIV Agents, Cyclohexanones, Cell Line, Tumor, cyclohexanone derivatives, polyhydroxylated aromatics, qsar studies, HIV-1, Humans, HIV Integrase, HIV Integrase Inhibitors, Virus Replication
Abstract

A number of 2,6-bisbenzylidenecyclohexane-1-one derivatives have been synthesized and tested as HIV-1 integrase (IN) inhibitors with the aim of obtaining compounds capable to elicit antiviral activity at non-cytotoxic concentrations in cell-based assays. 3,5-Bis(3,4,5-trihydroxybenzylidene)-4-oxocyclohexaneacetic acid (20d) resulted one of the most potent and selective derivatives in acutely infected MT-4 cells (EC(50) and CC(50) values of 2 and 40 microM, respectively). In enzyme assays with recombinant HIV-1 integrase (rIN), this compound proved able to inhibit both 3'-processing and disintegration with IC(50) values of 0.2 and 0.5 microM, respectively. In order to develop a model capable to predict the anti HIV-IN activity and useful to design novel derivatives, we performed a comparative molecular field analysis (CoMFA) like 3-D-QSAR. In our model the ligands were described quantitatively in the GRID program, and the model was optimized by selecting only the most informative variables in the GOLPE program. We found the predictive ability of the model to increase significantly when the number of variables was reduced from 20,925 to 1327. A Q(2) of 0.73 was obtained with the final model, confirming the predictive ability of the model. By studying the PLS coefficients in informative 3-D contour plots, ideas for the synthesis of new compounds could be generated.

Published
2003

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