Full Text Journal Articles by
Author Sara Consalvi

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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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Overcoming drug resistance in TB: an update.

Sara Consalvi, Giovanna Poce, Cristina Scarpecci, Mariangela Biava,

Future Microbiol (Future microbiology)
[2020, 15:1607-1609]

Cited: 0 times

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Therapeutic potential for coxibs-nitric oxide releasing hybrids in cystic fibrosis.

Sara Consalvi, Giovanna Poce, Carla Ghelardini, Lorenzo Di Cesare Mannelli, Paola Patrignani, Annalisa Bruno, Maurizio Anzini, Vincenzo Calderone, Alma Martelli, Lara Testai, Antonio Giordani, Mariangela Biava,

This review discusses the rational for further studies of COX-2 inhibitors-NO releaser hybrids (NO-Coxibs) in the pharmacological treatment of the airway inflammation in Cystic Fibrosis (CF). Our research group developed several classes of NO-Coxibs for the pharmacological treatment of arthritis, and among them several compounds showed an outstanding in vivo efficacy ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2021, 210:112983]

Cited: 0 times

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SAR Analysis of Small Molecules Interfering with Energy-Metabolism in Mycobacterium tuberculosis.

Federico Appetecchia, Sara Consalvi, Cristina Scarpecci, Mariangela Biava, Giovanna Poce,

Tuberculosis remains the world's top infectious killer: it caused a total of 1.5 million deaths and 10 million people fell ill with TB in 2018. Thanks to TB diagnosis and treatment, mortality has been falling in recent years, with an estimated 58 million saved lives between 2000 and 2018. However, ... Read more >>

Pharmaceuticals (Basel) (Pharmaceuticals (Basel, Switzerland))
[2020, 13(9):]

Cited: 2 times

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Chocolate Consumers and Lymphocyte-to-Monocyte Ratio: A Working Hypothesis from a Preliminary Report of a Pilot Study in Celiac Subjects.

Anna Raguzzini, Giovanna Poce, Sara Consalvi, Elisabetta Toti, Francesca Palmacci, Mariangela Biava, Ilaria Peluso,

BACKGROUND AND AIM:The aim of this work was to evaluate the relationship between platelet-to-lymphocyte ratio (PLR) and lymphocyte-to-monocyte ratio (LMR) with habitual consumption of dark chocolate in a group of celiac subjects in which chocolate consumption and lower neutrophil-to-lymphocyte ratio (NLR) association had already been observed. Additionally, due to the ... Read more >>

Antioxidants (Basel) (Antioxidants (Basel, Switzerland))
[2019, 8(10):]

Cited: 1 time

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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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Mycobacterial tryptophan biosynthesis: A promising target for tuberculosis drug development?

Sara Consalvi, Cristina Scarpecci, Mariangela Biava, Giovanna Poce,

The biosynthetic pathways of amino acids are attractive targets for drug development against pathogens with an intracellular behavior like M. tuberculosis (Mtb). Indeed, while in the macrophages Mtb has restricted access to amino acids such as tryptophan (Trp). Auxotrophic Mtb strains, with mutations in the Trp biosynthetic pathway, showed reduced ... Read more >>

Bioorg Med Chem Lett (Bioorganic & medicinal chemistry letters)
[2019, 29(23):126731]

Cited: 1 time

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Dietary flavonoids: Nano delivery and nanoparticles for cancer therapy.

Paola Aiello, Sara Consalvi, Giovanna Poce, Anna Raguzzini, Elisabetta Toti, Maura Palmery, Mariangela Biava, Marco Bernardi, Mohammad A Kamal, George Perry, Ilaria Peluso,

Application of nanotechnologies to cancer therapy might increase solubility and/or bioavailability of bioactive compounds of natural or synthetic origin and offers other potential benefits in cancer therapy, including selective targeting. In the present review we aim to evaluate in vivo studies on the anticancer activity of nanoparticles (NPs) obtained from ... Read more >>

Semin Cancer Biol (Seminars in cancer biology)
[2021, 69:150-165]

Cited: 5 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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Pharmaceutical salt of BM635 with improved bioavailability.

Giovanna Poce, Sara Consalvi, Martina Cocozza, Raquel Fernandez-Menendez, Robert H Bates, Fátima Ortega Muro, David Barros Aguirre, Lluis Ballell, Mariangela Biava,

BM635 is a small molecule endowed with outstanding anti-mycobacterial activity (minimum inhibitory concentration of 0.12μM against M. tuberculosis H37Rv) identified during a hit-to-lead campaign. Its poor aqueous solubility together with its high lipophilicity led to low exposure in vivo. Indeed, the half-life in vivo of BM635 was 1h, allowing a ... Read more >>

Eur J Pharm Sci (European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences)
[2017, 99:17-23]

Cited: 4 times

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A Series of COX-2 Inhibitors Endowed with NO-Releasing Properties: Synthesis, Biological Evaluation, and Docking Analysis.

Sara Consalvi, Giovanna Poce, Rino Ragno, Manuela Sabatino, Concettina La Motta, Stefania Sartini, Vincenzo Calderone, Alma Martelli, Carla Ghelardini, Lorenzo Di Cesare Mannelli, Mariangela Biava,

Herein we report the synthesis, biological evaluation, and docking analysis of a class of cyclooxygenase-2 (COX-2) inhibitors with nitric oxide (NO)-releasing properties. In an earlier study, a number of selective COX-2 inhibitors/NO donors were developed by conjugating a diarylpyrrole scaffold endowed with selective COX-2 inhibitory properties with various nitrooxyalkyl side ... Read more >>

ChemMedChem (ChemMedChem)
[2016, 11(16):1804-1811]

Cited: 1 time

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MmpL3 Inhibitors: Diverse Chemical Scaffolds Inhibit the Same Target.

Giovanna Poce, Sara Consalvi, Mariangela Biava,

MmpL3 belongs to the Resistance, Nodulation and Division (RND) superfamily whose role in mycobacteria is the formation of the outer membrane. Indeed, it has been shown that MmpL3 is associated with the export of mycolic acids in the form of trehalose monomycolates (TMM) to the periplasmic space or the outer ... Read more >>

Mini Rev Med Chem (Mini reviews in medicinal chemistry)
[2016, 16(16):1274-1283]

Cited: 10 times

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COX inhibitors: a patent review (2011 - 2014).

Sara Consalvi, Mariangela Biava, Giovanna Poce,

<h4>Introduction</h4>The COX enzymes play a central role in the biosynthetic pathway of important biological mediators called prostanoids. Differences in regulation of gene expression, stability of transcripts and proteins determine the different biological functions of COX-1 and COX-2. While the COX-1 gene has been considered to be a 'housekeeping' gene expressed ... Read more >>

Expert Opin Ther Pat (Expert opinion on therapeutic patents)
[2015, 25(12):1357-1371]

Cited: 15 times

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Synthesis, biological evaluation and docking analysis of a new series of methylsulfonyl and sulfamoyl acetamides and ethyl acetates as potent COX-2 inhibitors.

Sara Consalvi, Salvatore Alfonso, Angela Di Capua, Giovanna Poce, Adele Pirolli, Manuela Sabatino, Rino Ragno, Maurizio Anzini, Stefania Sartini, Concettina La Motta, Lorenzo Di Cesare Mannelli, Carla Ghelardini, Mariangela Biava,

We report herein the synthesis, biological evaluation and docking analysis of a new series of methylsulfonyl, sulfamoyl acetamides and ethyl acetates that selectively inhibit cyclooxygenase-2 (COX-2) isoform. Among the newly synthesized compounds, some of them were endowed with a good activity against COX-2 and a good selectivity COX-2/COX-1 in vitro ... Read more >>

Bioorg Med Chem (Bioorganic & medicinal chemistry)
[2015, 23(4):810-820]

Cited: 9 times

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SAR analysis of new anti-TB drugs currently in pre-clinical and clinical development.

Giovanna Poce, Martina Cocozza, Sara Consalvi, Mariangela Biava,

Despite enormous efforts have been made in the hunt for new drugs, tuberculosis (TB) still remains the first bacterial cause of mortality worldwide, causing an estimated 8.6 million new cases and 1.3 million deaths in 2012. Multi-drug resistant-TB strains no longer respond to first-line drugs and are inexorably spreading with ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2014, 86:335-351]

Cited: 16 times

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Enhancing the pharmacodynamic profile of a class of selective COX-2 inhibiting nitric oxide donors.

Mariangela Biava, Claudio Battilocchio, Giovanna Poce, Salvatore Alfonso, Sara Consalvi, Angela Di Capua, Vincenzo Calderone, Alma Martelli, Lara Testai, Lidia Sautebin, Antonietta Rossi, Carla Ghelardini, Lorenzo Di Cesare Mannelli, Antonio Giordani, Stefano Persiani, Milena Colovic, Melania Dovizio, Paola Patrignani, Maurizio Anzini,

We report herein the development, synthesis, physicochemical and pharmacological characterization of a novel class of pharmacodynamic hybrids that selectively inhibit cyclooxygenase-2 (COX-2) isoform and present suitable nitric oxide releasing properties. The replacement of the ester moiety with the amide group gave access to in vivo more stable and active derivatives ... Read more >>

Bioorg Med Chem (Bioorganic & medicinal chemistry)
[2014, 22(2):772-786]

Cited: 10 times

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A class of pyrrole derivatives endowed with analgesic/anti-inflammatory activity.

Claudio Battilocchio, Giovanna Poce, Salvatore Alfonso, Giulio Cesare Porretta, Sara Consalvi, Lidia Sautebin, Simona Pace, Antonietta Rossi, Carla Ghelardini, Lorenzo Di Cesare Mannelli, Silvia Schenone, Antonio Giordani, Luigia Di Francesco, Paola Patrignani, Mariangela Biava,

We report the synthesis and bio-pharmacological evaluation of a class of pyrrole derivatives featuring a small appendage fragment (carbaldehyde, oxime, nitrile) on the central core. Compound 1c proved to be extremely effective in vivo, showing an interesting anti-nociceptic profile that is comparable to reference compounds already marketed, hence representing a ... Read more >>

Bioorg Med Chem (Bioorganic & medicinal chemistry)
[2013, 21(13):3695-3701]

Cited: 8 times

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Improving the solubility of a new class of antiinflammatory pharmacodynamic hybrids, that release nitric oxide and inhibit cycloxygenase-2 isoenzyme.

Mariangela Biava, Claudio Battilocchio, Giovanna Poce, Salvatore Alfonso, Sara Consalvi, Giulio Cesare Porretta, Silvia Schenone, Vincenzo Calderone, Alma Martelli, Lara Testai, Carla Ghelardini, Lorenzo Di Cesare Mannelli, Lidia Sautebin, Antonietta Rossi, Antonio Giordani, Paola Patrignani, Maurizio Anzini,

The development of a novel class of pharmacodynamic hybrids that inhibits COX-2 isoform is reported. 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. ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2012, 58:287-298]

Cited: 7 times

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