Synthesis and biological evaluation of thiazole derivatives as <i>Lb</i>SOD inhibitors

Brito, Camila Carane Bitencourt; Silva, Hélder Vinicius Carneiro da; Brondani, Daci José; Faria, Antônio Rodolfo de; Ximenes, Rafael Matos; Silva, Ivanildo Mangueira da; Albuquerque, Julianna Ferreira Cavalcanti de; Castilho, Marcelo Santos

doi:10.1080/14756366.2018.1550752

Cited by 18 publications

(6 citation statements)

References 47 publications

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“…Similar situations have also been reported in the literatures 35 , 37 . The accurate thermodynamic parameters need to be further studied in combination with other techniques, such as surface plasmon resonance (SPR) 38 , 39 and thermal shift assays (TSA) 40 , 41 .…”

Section: Resultssupporting

confidence: 70%

Benzonate derivatives of acetophenone as potent α-glucosidase inhibitors: synthesis, structure–activity relationship and mechanism

Dan

Zhang

et al. 2019

Journal of Enzyme Inhibition and Medicinal Chemistry

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In this article, 23 compounds (6 and 7a-7v) were prepared and evaluated for their in vitro a-glucosidase inhibitory activity. The compounds 7d, 7f, 7i, 7n, 7o, 7r, 7s, 7u, and 7v displayed the a-glucosidase inhibition activity with IC 50 values ranging from 1.68 to 7.88 mM. Among all tested compounds, 7u was found to be the most efficient, being 32-fold more active than the standard drug acarbose, which significantly attenuated postprandial blood glucose in mice. In addition, the compound 7u also induced the fluorescence quenching and conformational changes of enzyme, by forming a-glucosidase-7u complex in a mixed inhibition type. The thermodynamic constants recognised the interaction between 7u and a-glucosidase and was an enthalpy-driven spontaneous exothermic reaction. The synchronous fluorescence and CD spectra also indicate that the compound 7u changed the enzyme conformation. The findings identify the binding interactions between new ligands and a-glucosidase and reveal the compound 7u as a potent a-glucosidase inhibitor.

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Section: Resultssupporting

confidence: 70%

Benzonate derivatives of acetophenone as potent α-glucosidase inhibitors: synthesis, structure–activity relationship and mechanism

Dan

Zhang

et al. 2019

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…Brito et al [185], based on previous studies on the leishmanicidal activity of 1,3 thiazole derivatives [186] and that phthalimide-thiazole derivatives showed higher af finity to L. infantum FeSOD than human CuZnSOD [187], designed a series of 2,4 subst tuted thiazole derivatives in order to evaluate their LbSOD inhibitory activity. Com pounds were tested using thermal shift assay (TSA) as well as fluorescent protein labeled assays (FLPA).…”

Section: Neglected Diseasesmentioning

confidence: 99%

Thiazole Ring—A Biologically Active Scaffold

2021

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Background: Thiazole is a good pharmacophore nucleus due to its various pharmaceutical applications. Its derivatives have a wide range of biological activities such as antioxidant, analgesic, and antimicrobial including antibacterial, antifungal, antimalarial, anticancer, antiallergic, antihypertensive, anti-inflammatory, and antipsychotic. Indeed, the thiazole scaffold is contained in more than 18 FDA-approved drugs as well as in numerous experimental drugs. Objective: To summarize recent literature on the biological activities of thiazole ring-containing compounds Methods: A literature survey regarding the topics from the year 2015 up to now was carried out. Older publications were not included, since they were previously analyzed in available peer reviews. Results: Nearly 124 research articles were found, critically analyzed, and arranged regarding the synthesis and biological activities of thiazoles derivatives in the last 5 years.

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“…2-Iminothiazole derivatives [156], scorpiand-like azamacrocycles [157,158], pyrazole-containing polyamine macrocycles [159] phthalazine derivatives [161], triphenyl tin salicylanilide thiosemicarbazone [162], Se containing aromatics and heteroaromatic compounds [163], ruthenium complexes with purine analogs [164], fisetin-a flavanoid anolog [57] and dialkyl pyrazole-3,5-dicarboxylates [165] were reported as SOD inhibitors exhibiting antileishmanial activity in the literature.…”

Section: Superoxide Dismutase (Sod Ec 11511)mentioning

confidence: 99%

Toward New Antileishmanial Compounds: Molecular Targets for Leishmaniasis Treatment

Istanbullu¹,

Bayraktar²

2022

Leishmaniasis - General Aspects of a Stigmatized Disease

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The leishmaniases are a group of diseases caused by protozoan parasites—Leishmania sp. Leishmaniasis is classified among the 20 neglected diseases by WHO. Although the disease has been known for more than 120 years, the number of drugs used for the treatment is still limited to 5–6. The first-line drugs against leishmaniasis are pentavalent antimonials, which were introduced to the treatment 70 years ago—despite all their side effects. Molecular targets are becoming increasingly important for efficacy and selectivity in postgenomic drug research studies. In this chapter, we have discussed potential therapeutic targets of antileishmanial drug discovery such as pteridine reductase (PTR1), trypanothione reductase (TR), N-myristoyltransferase (NMT), trypanothione synthetase (TryS), IU-nucleoside hydrolase, and topoisomerases, enzymes and their inhibitors reported in the literature.

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Synthesis and biological evaluation of thiazole derivatives as LbSOD inhibitors

Cited by 18 publications

References 47 publications

Benzonate derivatives of acetophenone as potent α-glucosidase inhibitors: synthesis, structure–activity relationship and mechanism

Benzonate derivatives of acetophenone as potent α-glucosidase inhibitors: synthesis, structure–activity relationship and mechanism

Thiazole Ring—A Biologically Active Scaffold

Toward New Antileishmanial Compounds: Molecular Targets for Leishmaniasis Treatment

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