N-(4-Nitrophenyl)-2-{2-[3-(4-chlorophenyl)-5-[4-(propan-2-yl)phenyl]-4,5-dihydro-1H-pyrazol-1-yl]-4-oxo-4,5-dihydro-1,3-thiazol-5-yl}acetamide

Salian, Vinutha V.; Narayana, B.; Sarojini, B. K.

doi:10.3390/m943

Cited by 3 publications

(2 citation statements)

References 13 publications

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“…The structure of the compound 2 was established by 1 H and 13 C NMR spectroscopy. The 1 H NMR spectrum reveals in particular, a singlet at 4,65ppm attributed to the proton of the secondary amino group (NH-CH-Ph).…”

Section: Chemistrymentioning

confidence: 99%

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Synthesis, characterization and antibacterial activity of Methyl (2R)-2-benzamido-2-{[(1R)-2-methoxy-2-oxo- 1-phenylethyl]amino}acetate

et al. 2018

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The present work covers the recent synthetic of methyl (2R)-2-benzamido-2-{[(1R)-2-methoxy-2-oxo-1-phenylethyl]amino}acetate, via N-alkylation of methyl a-azido glycinate N-benzoylated with methyl 2-amino-2-phenylacetate in methylene chloride and in presence of triethylamine as basic catalyst. The structure of the prepared compound was determined by spectroscopic methods: 1H-NMR, 13C-NMR, MS data, elemental analysis and confirmed by X-Ray diffraction. This compound was screened in vitro for its antibacterial activity against Gram-positive bacteria (Bacillus subtilis and Staphylococcus aureus) and Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa and Salmonella enteric). The MIC values confirmed that the title compound had a bactericidal effect against the strains tested.

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Section: Chemistrymentioning

confidence: 99%

“…Amino acid derivatives are an important group of peptidomimetics 1 . They exhibit several applications in medicinal chemistry.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, characterization and antibacterial activity of Methyl (2R)-2-benzamido-2-{[(1R)-2-methoxy-2-oxo- 1-phenylethyl]amino}acetate

et al. 2018

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Synthesis and antioxidant properties of novel hybrid molecules containing gallic acid and thiazolidinone moieties

Al Zahrani,

Al-Ghamdi,

El‐Shishtawy

2024

Journal of Molecular Structure

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Design, Synthesis, Docking and Computational Pharmacokinetic Profiling of New Pyrazolinyl Thiazolinone Biheterocycles as Potent Antimicrobial Agents

Salian

Narayana

Sarojini

et al. 2020

LDDD

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Background: Development of potential antimicrobial agents is a main aim in the drug discovery process to overcome the drug resistant problems. Pyrazolines and thiazolinones are extensively used as building blocks for the synthesis of diverse medicinally important compounds. Method: In this present work, a new series of functionalized pyrazolinyl-thiazolinone biheterocycles is designed and synthesized from N-pyrazolinecarbothioamide. Antimicrobial screening is carried out in order to discover their potential towards six bacterial and four fungal strains. The zone of inhibition (ZI in mm) was determined by disc diffusion method and minimum inhibitory concentration (MIC in μg/mL) by macro dilution method. The druggability of these new entities is done through in silico pharmacokinetic profiling using Maestro 2017-1 interface of Schrӧdinger software. Result: The compounds 4c and 4e with chloro and iodo substituents on N-phenylacetamide ring displayed good inhibitory antibacterial activity against tested bacterial strains with minimum MIC values when compared to the reference drug tetracycline. The compound 3 with an acetic acid derivative showed high antifungal activity among all the tested derivatives. The compound 3 not only showed antifungal activity but also qualified druggability test with no violation of Lipinski rule of five. Conclusion: The capability of the synthesized pyrazolinyl-thiazolinone derivatives was performed to efficiently inhibit the growth of microorganisms against selected bacterial and fungal strains. Further, these compounds are found to be effectively bound to the active sites of attractive target Escherichia coli FabH.

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N-(4-Nitrophenyl)-2-{2-[3-(4-chlorophenyl)-5-[4-(propan-2-yl)phenyl]-4,5-dihydro-1H-pyrazol-1-yl]-4-oxo-4,5-dihydro-1,3-thiazol-5-yl}acetamide

Cited by 3 publications

References 13 publications

Synthesis, characterization and antibacterial activity of Methyl (2R)-2-benzamido-2-{[(1R)-2-methoxy-2-oxo- 1-phenylethyl]amino}acetate

Synthesis, characterization and antibacterial activity of Methyl (2R)-2-benzamido-2-{[(1R)-2-methoxy-2-oxo- 1-phenylethyl]amino}acetate

Synthesis and antioxidant properties of novel hybrid molecules containing gallic acid and thiazolidinone moieties

Design, Synthesis, Docking and Computational Pharmacokinetic Profiling of New Pyrazolinyl Thiazolinone Biheterocycles as Potent Antimicrobial Agents

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