Crystal growth, single crystal structure, and biological activity of thiazolo-pyridine dicarboxylic acid derivatives

Hamdi Ben Yahia, Souhir Sabri, Rachid Essehli, Peter Kasak, Joanna Drogosz-Stachowicz, Anna Janecka, Brahim El Bali

Research output: Contribution to journalArticlepeer-review

6 Scopus citations

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 μM.

Original languageEnglish
Pages (from-to)27756-27765
Number of pages10
JournalACS Omega
Volume5
Issue number43
DOIs
StatePublished - Nov 3 2020

Funding

The authors would like to thank Dr. Said Mansour for the access to the characterization tools in the core lab. R.E. would like to thank the Oak Ridge National Laboratory managed by UT Battelle, LLC, for the U.S. Department of Energy (DOE) under contract DE-AC05-00OR22725. The publication of this article was funded by the Qatar National Library. The publication of this article was funded by the Qatar National Library. This work was also made possible by NPRP grant no. 8-878-1-172 from the Qatar National Research Fund (A Member of The Qatar Foundation). The finding achieved herein is solely the responsibility of the authors. The biological investigations were supported by a grant from the Medical University of Lodz No. 503/1-156-02/503-11-002.

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