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Author Alessandro De Logu

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6-Fluorophenylbenzohydrazides inhibit Mycobacterium tuberculosis growth through alteration of tryptophan biosynthesis.

Sara Consalvi, Giulia Venditti, Junhao Zhu, Helena I Boshoff, Kriti Arora, Alessandro De Logu, Thomas R Ioerger, Eric J Rubin, Mariangela Biava, Giovanna Poce,

A major constraint in reducing tuberculosis epidemic is the emergence of strains resistant to one or more of clinically approved antibiotics, which emphasizes the need of novel drugs with novel targets. Genetic knockout strains of Mycobacterium tuberculosis (Mtb) have established that tryptophan (Trp) biosynthesis is essential for the bacterium to ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2021, 226:113843]

Cited: 0 times

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Novel Pyrazole-Containing Compounds Active against Mycobacterium tuberculosis.

Giovanna Poce, Sara Consalvi, Giulia Venditti, Salvatore Alfonso, Nicoletta Desideri, Raquel Fernandez-Menendez, Robert H Bates, Lluis Ballell, David Barros Aguirre, Joaquin Rullas, Alessandro De Logu, Michelle Gardner, Thomas R Ioerger, Eric J Rubin, Mariangela Biava,

In this study, a series of 49 five-membered heterocyclic compounds containing either a pyridine- or a pyrrole-type nitrogen were synthesized and tested against Mycobacterium tuberculosis. Among them, only the 1,3,5-trisubstituted pyrazoles 5-49 exhibited minimum inhibitory concentration values in the low micromolar range, and some also exhibited an improved physicochemical profile ... Read more >>

ACS Med Chem Lett (ACS medicinal chemistry letters)
[2019, 10(10):1423-1429]

Cited: 4 times

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Design, synthesis and antimycobacterial activity of benzoxazinone derivatives and open-ring analogues: Preliminary data and computational analysis.

Daniele Zampieri, Maria Grazia Mamolo, Julia Filingeri, Sara Fortuna, Alessandro De Logu, Adriana Sanna, Davide Zanon,

This study examines in depth benzoxazine nucleus for antimycobacterial property. We synthesized some benzoxazin-2-one and benzoxazin-3-one derivatives, which were tested for activity against a panel of Mycobacterium tuberculosis (Mtb) strains, including H37Ra, H37Rv and some resistant strains. Several compounds displayed a high antimycobacterial activity and the three isoniazid analogue derivatives ... Read more >>

Bioorg Med Chem Lett (Bioorganic & medicinal chemistry letters)
[2019, 29(17):2468-2474]

Cited: 1 time

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Imidazole and 1,2,4-Triazole-based Derivatives Gifted with Antitubercular Activity: Cytotoxicity and Computational Assessment.

Daniele Zampieri, Francesca Cateni, Mariarosa Moneghini, Marina Zacchigna, Erik Laurini, Domenico Marson, Alessandro De Logu, Adriana Sanna, Maria G Mamolo,

<h4>Background</h4>Mycobacterium Tuberculosis (Mtb) is the causative pathogen of Tuberculosis (TB) and outbreaks are more common among immunosuppressed persons infected with HIV. The current treatment regimens are lengthy and toxic, yet the therapy has remained unchanged for many decades, so there is a need to find new structures with selective mechanism ... Read more >>

Curr Top Med Chem (Current topics in medicinal chemistry)
[2019, 19(8):620-632]

Cited: 1 time

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Design, synthesis, SAR and biological investigation of 3-(carboxymethyl)rhodanine and aminothiazole inhibitors of Mycobacterium tuberculosis Zmp1.

Mattia Mori, Davide Deodato, Mohan Kasula, Davide M Ferraris, Adriana Sanna, Alessandro De Logu, Menico Rizzi, Maurizio Botta,

Sixteen 3-(carboxymethyl)rhodanines, and twelve aminothiazoles as rhodanine-mimetics were designed, synthesized and tested as inhibitors of the Zmp1 enzyme from Mycobacterium tuberculosis (Mtb). Almost all rhodanines (5a-d, 5f-n, and 7a-b) exhibited Zmp1 inhibition with IC50 values in the range 1.3-43.9 µM, whereas only aminothiazoles 12b and 12d proved active with IC50 values ... Read more >>

Bioorg Med Chem Lett (Bioorganic & medicinal chemistry letters)
[2018, 28(4):637-641]

Cited: 0 times

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In vivo potent BM635 analogue with improved drug-like properties.

Giovanna Poce, Martina Cocozza, Salvatore Alfonso, Sara Consalvi, Giulia Venditti, Raquel Fernandez-Menendez, Robert H Bates, David Barros Aguirre, Lluis Ballell, Alessandro De Logu, Giulio Vistoli, Mariangela Biava,

BM635 is the hit compound of a promising anti-TB compound class. Herein we report systematic variations around the central pyrrole core of BM635 and we describe the design, synthesis, biological evaluation, pharmacokinetic analysis, as well as in vivo TB mouse efficacy studies of novel BM635 analogues that show improved physicochemical properties. ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2018, 145:539-550]

Cited: 5 times

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Naturally occurring Diels-Alder-type adducts from Morus nigra as potent inhibitors of Mycobacterium tuberculosis protein tyrosine phosphatase B.

Alessandra Mascarello, Angela Camila Orbem Menegatti, Andrea Calcaterra, Priscila Graziela Alves Martins, Louise Domeneghini Chiaradia-Delatorre, Ilaria D'Acquarica, Franco Ferrari, Valentina Pau, Adriana Sanna, Alessandro De Logu, Maurizio Botta, Bruno Botta, Hernán Terenzi, Mattia Mori,

Mycobacterium tuberculosis (Mtb) protein tyrosine phosphatases A and B (PtpA and PtpB) have been recognized as potential molecular targets for the development of new therapeutic strategies against tuberculosis (TB). In this context, we have recently reported that the naturally occurring Diels-Alder-type adduct Kuwanol E is an inhibitor of PtpB (Ki = 1.6 ± 0.1 μM). ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2018, 144:277-288]

Cited: 2 times

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Antimycobacterial activity of new N(1)-[1-[1-aryl-3-[4-(1H-imidazol-1-yl)phenyl]-3-oxo]propyl]-pyridine-2-carboxamidrazone derivatives.

Daniele Zampieri, Maria Grazia Mamolo, Luciano Vio, Maurizio Romano, Nataša Skoko, Marco Baralle, Valentina Pau, Alessandro De Logu,

N(1)-[1-[1-aryl-3-[4-(1H-imidazol-1-yl)phenyl]-3-oxo]propyl]-pyridine-2-carboxamidrazone derivatives were design, synthesized and tested for their in vitro antimycobacterial activity. The new compounds showed a moderate antimycobacterial activity against the tested strain of Mycobacterium tuberculosis H37Ra and a significant antimycobacterial activity against several mycobacteria other than tuberculosis strains. ... Read more >>

Bioorg Med Chem Lett (Bioorganic & medicinal chemistry letters)
[2016, 26(14):3287-3290]

Cited: 0 times

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Discovery of in vitro antitubercular agents through in silico ligand-based approaches.

Daniela De Vita, Fabiana Pandolfi, Roberto Cirilli, Luigi Scipione, Roberto Di Santo, Laura Friggeri, Mattia Mori, Diego Fiorucci, Giorgio Maccari, Robert Selwyne Arul Christopher, Claudio Zamperini, Valentina Pau, Alessandro De Logu, Silvano Tortorella, Maurizio Botta,

The development of new anti-tubercular agents represents a constant challenge mostly due to the insurgency of resistance to the currently available drugs. In this study, a set of 60 molecules were selected by screening the Asinex and the ZINC collections and an in house library by means of in silico ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2016, 121:169-180]

Cited: 5 times

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Exploring the thiazole scaffold for the identification of new agents for the treatment of fluconazole resistant Candida.

Rita Meleddu, Simona Distinto, Angela Corona, Elias Maccioni, Antonella Arridu, Claudia Melis, Giulia Bianco, Peter Matyus, Filippo Cottiglia, Adriana Sanna, Alessandro De Logu,

Cyclohexyliden- and 2-methylcyclohexyliden-hydrazo-4-arylthiazoles were synthesized and tested as antifungal agents. All compounds exhibited minimal inhibitory concentration (MIC) values comparable with those of fluconazole (FLC). Moreover, some compounds showed fungicidal activity at low concentration. Worth noting five out of nine compounds were active towards Candida albicans 25 FLC resistant isolated from ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2016, 31(6):1672-1677]

Cited: 3 times

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Improved BM212 MmpL3 inhibitor analogue shows efficacy in acute murine model of tuberculosis infection.

Giovanna Poce, Robert H Bates, Salvatore Alfonso, Martina Cocozza, Giulio Cesare Porretta, Lluís Ballell, Joaquin Rullas, Fátima Ortega, Alessandro De Logu, Emanuela Agus, Valentina La Rosa, Maria Rosalia Pasca, Edda De Rossi, Baojie Wae, Scott G Franzblau, Fabrizio Manetti, Maurizio Botta, Mariangela Biava,

1,5-Diphenyl pyrroles were previously identified as a class of compounds endowed with high in vitro efficacy against M. tuberculosis. To improve the physical chemical properties and drug-like parameters of this class of compounds, a medicinal chemistry effort was undertaken. By selecting the optimal substitution patterns for the phenyl rings at ... Read more >>

PLoS One (PloS one)
[2013, 8(2):e56980]

Cited: 37 times

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Ungeremine effectively targets mammalian as well as bacterial type I and type II topoisomerases.

Laura Casu, Filippo Cottiglia, Marco Leonti, Alessandro De Logu, Emanuela Agus, Yuk-Ching Tse-Dinh, Valentina Lombardo, Claudia Sissi,

From the methanol extract of the bulbs of Pancratium illyricum L., three phenanthridine type alkaloids, ungeremine (1), (-)-lycorine (2) and (+)-vittatine (3) were isolated. For the evaluation of their anticancer and antibacterial potential, compounds 1-3 were tested against human (I, IIα) and bacterial (IA, IV) topoisomerases. Our data demonstrated that ... Read more >>

Bioorg Med Chem Lett (Bioorganic & medicinal chemistry letters)
[2011, 21(23):7041-7044]

Cited: 16 times

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MmpL3 is the cellular target of the antitubercular pyrrole derivative BM212.

Valentina La Rosa, Giovanna Poce, Julio Ortiz Canseco, Silvia Buroni, Maria Rosalia Pasca, Mariangela Biava, Ravikiran M Raju, Giulio Cesare Porretta, Salvatore Alfonso, Claudio Battilocchio, Babak Javid, Flavia Sorrentino, Thomas R Ioerger, James C Sacchettini, Fabrizio Manetti, Maurizio Botta, Alessandro De Logu, Eric J Rubin, Edda De Rossi,

The 1,5-diarylpyrrole derivative BM212 was previously shown to be active against multidrug-resistant clinical isolates and Mycobacterium tuberculosis residing within macrophages as well as against Mycobacterium avium and other atypical mycobacteria. To determine its mechanism of action, we identified the cellular target. Spontaneous Mycobacterium smegmatis, Mycobacterium bovis BCG, and M. tuberculosis ... Read more >>

Antimicrob Agents Chemother (Antimicrobial agents and chemotherapy)
[2012, 56(1):324-331]

Cited: 105 times

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Developing pyrrole-derived antimycobacterial agents: a rational lead optimization approach.

Mariangela Biava, Giulio Cesare Porretta, Giovanna Poce, Claudio Battilocchio, Salvatore Alfonso, Alessandro de Logu, Fabrizio Manetti, Maurizio Botta,

Tuberculosis (TB) represents a never-ending challenge toward which research efforts are needed. Drug resistance is the key problem that scientists in the field need to fight. The development of new drugs endowed with novel modes of action against different biological targets is of extreme importance; these new agents should also ... Read more >>

ChemMedChem (ChemMedChem)
[2011, 6(4):593-599]

Cited: 13 times

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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, Giulio Cesare Porretta, Giovanna Poce, Claudio Battilocchio, Salvatore Alfonso, Alessandro De Logu, Nadia Serra, Fabrizio Manetti, Maurizio Botta,

A hit optimization procedure based on isosteric and bioisosteric replacement of decorating groups at both the N1 and the C5 phenyl rings of 1,5-diarylpyrroles led to identification of 4-((1-(4-fluorophenyl)-2-methyl-5-(4-(methylthio)phenyl)-1H-pyrrol-3-yl)methyl)thiomorpholine that is characterized by a very high activity toward both Mycobacterium tuberculosis 103471 and H37Rv strains (MIC values of 0.125μg/mL), and ... Read more >>

Bioorg Med Chem (Bioorganic & medicinal chemistry)
[2010, 18(22):8076-8084]

Cited: 7 times

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Synthesis, biological evaluation, and SAR study of novel pyrazole analogues as inhibitors of Mycobacterium tuberculosis: part 2. Synthesis of rigid pyrazolones.

Daniele Castagnolo, Fabrizio Manetti, Marco Radi, Beatrice Bechi, Mafalda Pagano, Alessandro De Logu, Rita Meleddu, Manuela Saddi, Maurizio Botta,

Two series of novel rigid pyrazolone derivatives were synthesized and evaluated as inhibitors of Mycobacterium tuberculosis (MTB), the causative agent of tuberculosis. Two of these compounds showed a high activity against MTB (MIC=4 microg/mL). The newly synthesized pyrazolones were also computationally investigated to analyze if their properties fit the pharmacophoric ... Read more >>

Bioorg Med Chem (Bioorganic & medicinal chemistry)
[2009, 17(15):5716-5721]

Cited: 28 times

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Synthesis, biological evaluation and SAR study of novel pyrazole analogues as inhibitors of Mycobacterium tuberculosis.

Daniele Castagnolo, Alessandro De Logu, Marco Radi, Beatrice Bechi, Fabrizio Manetti, Matteo Magnani, Sibilla Supino, Rita Meleddu, Lorenza Chisu, Maurizio Botta,

As a continuation of our previous work that turned toward the identification of antimycobacterial compounds with innovative structures, two series of pyrazole derivatives were synthesized by parallel solution-phase synthesis and were assayed as inhibitors of Mycobacterium tuberculosis (MTB), which is the causative agent of tuberculosis. One of these compounds showed ... Read more >>

Bioorg Med Chem (Bioorganic & medicinal chemistry)
[2008, 16(18):8587-8591]

Cited: 24 times

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Rifampicin-loaded liposomes for the passive targeting to alveolar macrophages: in vitro and in vivo evaluation.

Marco Zaru, Chiara Sinico, Alessandro De Logu, Carla Caddeo, Francesco Lai, Maria Letizia Manca, Anna Maria Fadda,

Mycobacterium avium complex (MAC), the most frequent cause of opportunistic nontuberculous pulmonary infection, is made up of a group of intracellular pathogens that are able to survive and multiply inside lung alveolar macrophages. As nebulized liposomes are reported to be effective to target antibacterial agents to macrophages, in this work ... Read more >>

J Liposome Res (Journal of liposome research)
[2009, 19(1):68-76]

Cited: 26 times

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1,5-Diaryl-2-ethyl pyrrole derivatives as antimycobacterial agents: design, synthesis, and microbiological evaluation.

Mariangela Biava, Giulio C Porretta, Giovanna Poce, Alessandro De Logu, Rita Meleddu, Edda De Rossi, Fabrizio Manetti, Maurizio Botta,

During the search of novel antitubercular drugs related to BM 212, new diarylpyrroles were designed and synthesized on the basis of a structure-activity relationship analysis of many pyrroles previously described by us. Among them, 1-(4-fluorophenyl)-2-ethyl-3-(thiomorpholin-4-yl)methyl-5-(4-methylphenyl)-1H-pyrrole (2b) proved to be particularly active, with a minimum inhibitory concentration (MIC, expressed as microg/mL) ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2009, 44(11):4734-4738]

Cited: 15 times

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Synthesis and biological evaluation of new enantiomerically pure azole derivatives as inhibitors of Mycobacterium tuberculosis.

Daniele Castagnolo, Marco Radi, Filippo Dessì, Fabrizio Manetti, Manuela Saddi, Rita Meleddu, Alessandro De Logu, Maurizio Botta,

A series of novel enantiomerically pure azole derivatives was synthesized. The new compounds, bearing both an imidazole as well as a triazole moiety, were evaluated as antimycobacterial agents. One of them proved to have activity against Mycobaterium tuberculosis comparable to those of the classical antibacterial/antifungal drugs Econazole and Clotrimazole. ... Read more >>

Bioorg Med Chem Lett (Bioorganic & medicinal chemistry letters)
[2009, 19(8):2203-2205]

Cited: 18 times

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Novel N-aryl- and N-heteryl phenazine-1-carboxamides as potential agents for the treatment of infections sustained by drug-resistant and multidrug-resistant Mycobacterium tuberculosis.

Alessandro De Logu, Larisa H Palchykovska, Valentina H Kostina, Adriana Sanna, Rita Meleddu, Lorenza Chisu, Inna V Alexeeva, Anatoly D Shved,

We investigated the in vitro activity of a new class of N-aryl and N-heteryl phenazine-1-carboxamide derivatives against Mycobacterium tuberculosis H37Rv and against drug-resistant ATCC M. tuberculosis strains. The activity against M. tuberculosis in J774 macrophage cells was also investigated. In most cases, minimum inhibitory concentrations (MICs) ranging between 0.19 mg/L ... Read more >>

Int J Antimicrob Agents (International journal of antimicrobial agents)
[2009, 33(3):223-229]

Cited: 4 times

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2-Acylhydrazino-5-arylpyrrole derivatives: synthesis and antifungal activity evaluation.

Valentina Onnis, Alessandro De Logu, Maria T Cocco, Roberta Fadda, Rita Meleddu, Cenzo Congiu,

The synthesis and antifungal activity of 2-acylhydrazino-5-arylpyrroles 21-62 are described. Pyrrole derivatives 21-62 were evaluated for their antifungal activity towards Candida albicans ATCC 10231 and three Candida non-albicans isolated from clinical specimens. Most of them showed very good antifungal activities against Candidae, having MIC values in the 0.39-3.12 microg/mL range ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2009, 44(3):1288-1295]

Cited: 9 times

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1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings.

Mariangela Biava, Giulio Cesare Porretta, Giovanna Poce, Alessandro De Logu, Manuela Saddi, Rita Meleddu, Fabrizio Manetti, Edda De Rossi, Maurizio Botta,

Synthesis and biological evaluation of new derivatives of 1,5-bis(4-chlorophenyl)-2-methyl-3-(4-methylpiperazin-1-yl)methyl-1H-pyrrole (BM 212, 16) are reported. Variously substituted phenyl rings with different substitution pattern and lipophilicity were added to the pyrrole nucleus to evaluate their influence on the activity toward Mycobacterium tuberculosis (MTB) and atypical mycobacteria. The most active derivatives showed activity ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2008, 51(12):3644-3648]

Cited: 14 times

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Ligand-based virtual screening, parallel solution-phase and microwave-assisted synthesis as tools to identify and synthesize new inhibitors of mycobacterium tuberculosis.

Fabrizio Manetti, Matteo Magnani, Daniele Castagnolo, Laura Passalacqua, Maurizio Botta, Federico Corelli, Manuela Saddi, Delia Deidda, Alessandro De Logu,

In an attempt to identify new inhibitors of the growth of Mycobacterium tuberculosis (MTB), the causative agent of tuberculosis, a procedure for the generation, design, and screening of a ligand-based virtual library was applied. This used both an in silico protocol centered on a recursive partitioning (RP) model described herein, ... Read more >>

ChemMedChem (ChemMedChem)
[2006, 1(9):973-989]

Cited: 13 times

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In vitro antimycobacterial activity of newly synthesised S-alkylisothiosemicarbazone derivatives and synergistic interactions in combination with rifamycins against Mycobacterium avium.

Alessandro De Logu, Manuela Saddi, Valentina Onnis, Clara Sanna, Cenzo Congiu, Rita Borgna, Maria Teresa Cocco,

The antimycobacterial activities of two new S-alkylisothiosemicarbazone derivatives (1i and 1f) against 32 Mycobacterium avium isolates were investigated. The minimum inhibitory concentrations (MICs) were significantly lower than those of rifampicin and other reference drugs. The two derivatives also showed excellent intracellular activity against M. avium residing in the macrophage-like J774 ... Read more >>

Int J Antimicrob Agents (International journal of antimicrobial agents)
[2005, 26(1):28-32]

Cited: 11 times

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