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Crystal Growth, Single Crystal Structure, and Biological Activity of Thiazolo-Pyridine Dicarboxylic Acid Derivatives.

ABSTRACT: Four novel TPDCA derivatives were prepared via a supersaturation method combining TPDCA with water, N-methyl-2-pyrrolidone (NMP), Na(PO2H2), and ammonia solution: 2(C9H7NO5S)H2O (1), (C9H7NO5S)C5H9NO (2), (C9H7NO5S)Na(PO2H2) (3), and (C9H5NO5S)(NH4)2(H2O) (4). Their crystal structures were determined by single-crystal X-ray diffraction. Compounds (1) and (2) crystallize in the monoclinic space groups P21 and P21/c, respectively, whereas compounds (3) and (4) crystallize in the triclinic space group P1?. Weak and moderate hydrogen bonds were detected in the four compounds. In the biological tests, (1) and (3) exhibited significant antibacterial activity against Escherichia coli and Staphylococcus aureus; in addition, (1) was cytotoxic against leukemia HL-60 cells with the IC50 value of 158.5 ± 12.5 ?M.

SUBMITTER: Yahia HB

PROVIDER: S-EPMC7643073 | biostudies-literature | 2020 Nov

REPOSITORIES: biostudies-literature

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Crystal Growth, Single Crystal Structure, and Biological Activity of Thiazolo-Pyridine Dicarboxylic Acid Derivatives.

Yahia Hamdi Ben HB Sabri Souhir S Essehli Rachid R Kasak Peter P Drogosz-Stachowicz Joanna J Janecka Anna A El Bali Brahim B

ACS omega 20201022 43

Four novel TPDCA derivatives were prepared via a supersaturation method combining TPDCA with water, N-methyl-2-pyrrolidone (NMP), Na(PO2H2), and ammonia solution: 2(C9H7NO5S)H2O (1), (C9H7NO5S)C5H9NO (2), (C9H7NO5S)Na(PO2H2) (3), and (C9H5NO5S)(NH4)<su ...[more]

PMID: 33163758

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