Search Results - "Souza Macchi, Fernanda"
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Synthesis and Antimycobacterial Activity of 3-Phenyl-1H-indoles
Published in Molecules (Basel, Switzerland) (25-08-2021)“…Tuberculosis has been described as a global health crisis since the 1990s, with an estimated 1.4 million deaths in the last year. Herein, a series of 20…”
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2
Design of Novel Inhibitors of Human Thymidine Phosphorylase: Synthesis, Enzyme Inhibition, in Vitro Toxicity, and Impact on Human Glioblastoma Cancer
Published in Journal of medicinal chemistry (14-02-2019)“…Overexpressed human thymidine phosphorylase (hTP) has been associated with cancer aggressiveness and poor prognosis by triggering proangiogenic and…”
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3
Synthesis and mechanistic investigation of iron(II) complexes of isoniazid and derivatives as a redox-mediated activation strategy for anti-tuberculosis therapy
Published in Journal of inorganic biochemistry (01-02-2018)“…The emergence of multidrug-resistant strains of Mycobacterium tuberculosis (MTB) represents a major threat to global health. Isoniazid (INH) is a prodrug used…”
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4
8-Mercaptoguanine-based inhibitors of Mycobacterium tuberculosis dihydroneopterin aldolase: synthesis, in vitro inhibition and docking studies
Published in Journal of enzyme inhibition and medicinal chemistry (01-01-2021)“…The dihydroneopterin aldolase (DHNA, EC 4.1.2.25) activity of FolB protein is required for the conversion of 7,8-dihydroneopterin (DHNP) to…”
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5
Exploring Scaffold Hopping for Novel 2‑(Quinolin-4-yloxy)acetamides with Enhanced Antimycobacterial Activity
Published in ACS medicinal chemistry letters (11-04-2024)“…Utilizing a scaffold-hopping strategy from the drug candidate telacebec, a novel series of 2-(quinolin-4-yloxy)acetamides was synthesized and evaluated as…”
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Antitubercular Activity of Novel 2‑(Quinoline-4-yloxy)acetamides with Improved Drug-Like Properties
Published in ACS medicinal chemistry letters (11-08-2022)“…Using cycloalkyl and electron-donating groups to decrease the carbonyl electrophilicity, a novel series of 2-(quinoline-4-yloxy)acetamides was synthesized and…”
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7
Effect of LPS on the Viability and Proliferation of Human Oral and Esophageal Cancer Cell Lines
Published in Brazilian Archives of Biology and Technology (2016)“…The esophagus and mouth tumors are very frequent malignancies worldwide. Lipopolysaccharides (LPS) are capable of regulating gene expression of…”
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8
Design, synthesis, and evaluation of new 2-(quinoline-4-yloxy)acetamide-based antituberculosis agents
Published in European journal of medicinal chemistry (15-04-2020)“…Using a classical molecular simplification approach, a series of 36 quinolines were synthesized and evaluated as in vitro inhibitors of Mycobacterium…”
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9
Identification of potential inhibitors of Mycobacterium tuberculosis shikimate kinase: molecular docking, in silico toxicity and in vitro experiments
Published in Journal of computer-aided molecular design (01-03-2023)“…Tuberculosis (TB) is one of the main causes of death from a single pathological agent, Mycobacterium tuberculosis ( Mtb ). In addition, the emergence of…”
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10
1H-Benzo[d]imidazoles and 3,4-dihydroquinazolin-4-ones: Design, synthesis and antitubercular activity
Published in European journal of medicinal chemistry (15-07-2018)“…Using a classical hybridization approach, a series of 1H-benzo[d]imidazoles and 3,4-dihydroquinazolin-4-ones were synthesized (39 examples) and evaluated as…”
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11
Ultrasound-assisted synthesis of 2-amino-1,3,4-oxadiazoles through NBS-mediated oxidative cyclization of semicarbazones
Published in Synthetic communications (18-07-2017)“…A ultrasound-assisted oxidative cyclization of semicarbazones using N-bromosuccinimide in the presence of sodium acetate was established providing efficient…”
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12
Pentacyanoferrate(II) complex of pyridine-4- and pyrazine-2-hydroxamic acid as source of HNO: investigation of anti-tubercular and vasodilation activities
Published in Journal of biological inorganic chemistry (01-09-2020)“…A pharmacophore design approach, based on the coordination chemistry of an intimate molecular hybrid of active metabolites of pro-drugs, known to release…”
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13
Novel 4-aminoquinolines: Synthesis, inhibition of the Mycobacterium tuberculosis enoyl-acyl carrier protein reductase, antitubercular activity, SAR, and preclinical evaluation
Published in European journal of medicinal chemistry (05-01-2023)“…Herein a series of 4-aminoquinolines were synthesized in an attempt to optimize and study the structural features related to LABIO-17 biological activity, a…”
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