Lubeluzole: from anti-ischemic drug to preclinical antidiarrheal studies

Cavalluzzi, Maria Maddalena; Budriesi, Roberta; Salvia, Maria Antonietta De; Quintieri, Laura; Piarulli, Monica; Milani, Gualtiero; Gualdani, Roberta; Micucci, Matteo; Corazza, Ivan; Rosato, Antonio; Viale, Maurizio; Caputo, Leonardo; Franchini, Carlo; Lentini, Giovanni

doi:10.1007/s43440-020-00167-2

Cited by 8 publications

(7 citation statements)

References 44 publications

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“…Following a previously reported procedure [ 31 ], the minimum inhibitory concentration (MIC), i.e., the lowest concentration of the tested compound, expressed as μg/mL (γ), which prevented any visible growth of the stated bacteria, was evaluated. Briefly, MIC determinations were performed by the microdilution method, according to the Clinical laboratory Standards Institute (CLSI) guidelines with few modifications.…”

Section: Methodsmentioning

confidence: 99%

Densely Functionalized 2-Methylideneazetidines: Evaluation as Antibacterials

et al. 2021

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Twenty-two novel, variously substituted nitroazetidines were designed as both sulfonamide and urethane vinylogs possibly endowed with antimicrobial activity. The compounds under study were obtained following a general procedure recently developed, starting from 4-nitropentadienoates deriving from a common β-nitrothiophenic precursor. While being devoid of any activity against fungi and Gram-negative bacteria, most of the title compounds performed as potent antibacterial agents on Gram-positive bacteria (E. faecalis and three strains of S. aureus), with the most potent congener being the 1-(4-chlorobenzyl)-3-nitro-4-(p-tolyl)azetidine 22, which displayed potency close to that of norfloxacin, the reference antibiotic (minimum inhibitory concentration values 4 and 1–2 μg/mL, respectively). Since 22 combines a relatively efficient activity against Gram-positive bacteria and a cytotoxicity on eucharyotic cells only at 4-times higher concentrations (inhibiting concentration on 50% of the cultured eukaryotic cells: 36 ± 10 μM, MIC: 8.6 μM), it may be considered as a promising hit compound for the development of a new series of antibacterials selectively active on Gram-positive pathogens. The relatively concise synthetic route described herein, based on widely available starting materials, could feed further structure–activity relationship studies, thus allowing for the fine investigation and optimization of the toxico-pharmacological profile.

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Section: Methodsmentioning

confidence: 99%

Densely Functionalized 2-Methylideneazetidines: Evaluation as Antibacterials

et al. 2021

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“…Chemistry 2024, 6, FOR PEER REVIEW 2 the 2-substituted BT moiety, showcasing the diverse applications and structural variations in this pharmacophore in medicinal chemistry [32][33][34][35][36][37][38].…”

Section: Synthetic Aspects Of 2-substituted Btsmentioning

confidence: 99%

“…Figure 1. Compounds ncorporating the 2-substituted BT moiety in pharmaceuticals [32][33][34][35][36][37][38].…”

Section: Synthetic Aspects Of 2-substituted Btsmentioning

confidence: 99%

“…Beyond their pharmacological significance, these compounds find diverse industrial applications such as corrosion inhibition [26], dyes [27], polymer chemistry [28], pesticides [29], textiles [30], and vulcanization acceleration [31]. Categorized in Figure 1 are various drugs incorporating the 2-substituted BT moiety, showcasing the diverse applications and structural variations in this pharmacophore in medicinal chemistry [32][33][34][35][36][37][38].…”

Section: Introductionmentioning

confidence: 99%

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Pioneering Synthetic Strategies of 2-Substituted Benzothiazoles Using 2-Aminothiophenol

Teli,

Sethiya,

Agarwal

2024

Chemistry

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Heterocycles, compounds featuring heteroatoms like nitrogen, sulfur, and oxygen, are integral in fields such as synthesis, pharmacology, and medicine. Among these, benzothiazoles, formed by fusing thiazole with benzene, hold significant prominence. Their unique reactivity, especially at the carbon position between nitrogen and sulfur, has sparked wide interest. Notably, 2-substituted benzothiazoles exhibit diverse biological activities, including anticonvulsant, antimicrobial, and antioxidant properties, making them valuable in drug discovery. This review unveils an array of mesmerizing methods employed by chemists to prepare these compounds using 2-aminothiophenol as one of the precursors with other varied reactants. From novel strategies to sophisticated methodologies, each section of this review provides a glimpse into the fascinating world of synthetic chemistry of 2-substituted benzothiazoles. Delving into the diverse synthetic applications of 2-substituted benzothiazoles, this paper not only enriches our understanding of their synthesis but also sparks the imagination with the possibilities for future advancements.

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“…There are two core ways for synthesizing thiazole: addition reaction and cyclization reaction (3) . Chemically, thiazoles (1,3 thiazole) occupy an important position due to their unique 5-membered heterocyclic ring structure (4) . Many heterocyclic products contain thiazoles and thiazole derivatives, such as antibiotics, antimicrobials, anticancer medications, anti-inflammatory drugs, and anticonvulsants (6) .…”

Section: Introductionmentioning

confidence: 99%

Preparation, spectroscopic characterization and study of biological activity as anticancer of some compounds using a new azo-Schiff base ligand (N,N,O) derived from 2-amino-5-methyl thiazol

Al-Adilee

Hassan

2022

ijhs

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The biological activity of the Co(III) complex of azo-Schiff bases derived from 2-amino-5-methylthiazole azo-Schiff bases was studied. Elementary examines, attractive instant volumes, spectroscopy (IR, electronic, 1 H NMR, and XRD), then thermogravimetric investigations described the azo-Schiff bases and their mineral complexes. For the cobalt complex, an octahedral geometry has been proposed. Thermal and infrared data of the mineral complexes confirmed the presence of the collected water. Schiff bases and mineral complexes have been tested for their anti-cancer properties

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Lubeluzole: from anti-ischemic drug to preclinical antidiarrheal studies

Cited by 8 publications

References 44 publications

Densely Functionalized 2-Methylideneazetidines: Evaluation as Antibacterials

Densely Functionalized 2-Methylideneazetidines: Evaluation as Antibacterials

Pioneering Synthetic Strategies of 2-Substituted Benzothiazoles Using 2-Aminothiophenol

Preparation, spectroscopic characterization and study of biological activity as anticancer of some compounds using a new azo-Schiff base ligand (N,N,O) derived from 2-amino-5-methyl thiazol

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