Synthesis, Transformation of 3-[(4-Arylthiazol-2-yl)(p-tolyl)amino]propanoic Acids, Bis(thiazol-5-yl)phenyl-, Bis(thiazol-5-yl)methane Derivatives, and Their Antimicrobial Activity

Mickevičius, Vytautas; Grybaitė, Birutė; Vaickelionienė, Rita; Stasevych, Maryna; Komarovska‐Porokhnyavets, Olena; Novikov, Volodymyr

doi:10.3987/com-17-13833

Cited by 5 publications

(1 citation statement)

References 28 publications

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“…mdpi.com/article/10.3390/ijms241713491/s1. References [41][42][43][44][45][46] are cited in the supplementary materials.…”

Section: Supplementary Materialsmentioning

confidence: 99%

Screening, Synthesis and Biochemical Characterization of SARS-CoV-2 Protease Inhibitors

Bagdonas,

Čerepenkaitė,

Mickevičiūtė

et al. 2023

IJMS

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The severe acute respiratory syndrome-causing coronavirus 2 (SARS-CoV-2) papain-like protease (PLpro) and main protease (Mpro) play an important role in viral replication events and are important targets for anti-coronavirus drug discovery. In search of these protease inhibitors, we screened a library of 1300 compounds using a fluorescence thermal shift assay (FTSA) and identified 53 hits that thermally stabilized or destabilized PLpro. The hit compounds structurally belonged to two classes of small molecules: thiazole derivatives and symmetrical disulfide compounds. Compound dissociation constants (Kd) were determined using an enzymatic inhibition method. Seven aromatic disulfide compounds were identified as efficient PLpro inhibitors with Kd values in the micromolar range. Two disulfides displayed six-fold higher potency for PLpro (Kd = 0.5 µM) than for Mpro. The disulfide derivatives bound covalently to both proteases, as confirmed through mass spectrometry. The identified compounds can serve as lead compounds for further chemical optimization toward anti-COVID-19 drugs.

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“…mdpi.com/article/10.3390/ijms241713491/s1. References [41][42][43][44][45][46] are cited in the supplementary materials.…”

Section: Supplementary Materialsmentioning

confidence: 99%

Screening, Synthesis and Biochemical Characterization of SARS-CoV-2 Protease Inhibitors

Bagdonas,

Čerepenkaitė,

Mickevičiūtė

et al. 2023

IJMS

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Synthesis and Antimicrobial Activity of Novel Thiazoles with Reactive Functional Groups

et al. 2019

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A series of substituted thiazoles bearing different functional groups, such as carboxyethylamino, carboxyl, chloromethyl, (phenylamino)methyl, ethoxyoxoethyl, methoxyoxoethylidene, ethoxycarbonyl, (methoxy or hydrazinyl)oxopropyl, carbohydrazinyl, formyl, and ((phenyl, carbamothioyl or isonicotinoyl)hydrazono)methyl, incorporated into their structure were synthesized. The synthesized compounds were tested for their antimicrobial activity against Escherichia coli, Staphylococcus aureus, and Mycobacterium luteum bacteria strains, and Candida tenuis and Aspergillus niger fungi. Compounds exhibiting exclusive antifungal activity against Aspergillus niger (MIC 0.9, 1.9 μg/mL) and Candida tenuis (MIC 7.8 μg/mL) have been identified among the novel thiazole derivatives.

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Synthesis and antibacterial activity of 3-substituted 1-(2-methyl-5-nitrophenyl)-5-oxopyrrolidine derivatives

et al. 2019

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Synthesis, Transformation of 3-[(4-Arylthiazol-2-yl)(p-tolyl)amino]propanoic Acids, Bis(thiazol-5-yl)phenyl-, Bis(thiazol-5-yl)methane Derivatives, and Their Antimicrobial Activity

Cited by 5 publications

References 28 publications

Screening, Synthesis and Biochemical Characterization of SARS-CoV-2 Protease Inhibitors

Screening, Synthesis and Biochemical Characterization of SARS-CoV-2 Protease Inhibitors

Synthesis and Antimicrobial Activity of Novel Thiazoles with Reactive Functional Groups

Synthesis and antibacterial activity of 3-substituted 1-(2-methyl-5-nitrophenyl)-5-oxopyrrolidine derivatives

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