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Bacterial Peptide Deformylase Inhibition of Tetrazole‐Substituted Biaryl Acid Analogs: Synthesis, Biological Evaluations, and Molecular Docking Study

The synthesis and screening of tetrazole‐substituted biaryl acid analogs 7a–l as bacterial peptide deformylase (PDF) enzyme inhibitors is reported. The compounds 7e (IC50 value = 5.50 μM) and 7g (IC50 value = 7.25 μM) showed good PDF inhibition activity. The compounds 7e (MIC range = 10.75–11.66 μg/mL) and 7g (MIC range = 8.91–12.83 μg/mL) also showed potent antibacterial activity when compared with the standard ciprofloxacin (MIC range = 25–50 μg/mL). Thus, the active derivatives were not only potent PDF enzyme inhibitors but also efficient antibacterial agents. In order to gain more insight into the binding mode of the compounds with the PDF enzyme, the most active compounds 7e and 7g, the moderately active compound 7k, and the least active compound 7h were docked against the PDF enzyme of Escherichia coli. The docking study of the most active compounds 7e and 7g against the PDF enzyme exhibited good binding properties. Hence, we believe our synthesized compounds 7a–l could serve as reservoir for bacterial PDF inhibitor development.

The synthesis and in vitro biological screening of novel tetrazole‐substituted biaryl acid analogs as bacterial peptide deformylase (PDF) enzyme inhibitors and antibacterial agents are reported. The most active derivatives 7e and 7g were not only potent PDF enzyme inhibitors but also efficient antibacterial agents.

Autoren:   Firoz A. Kalam Khan, Rajendra H. Patil, Manjiri Patil, Rohidas Arote, Devanand B. Shinde, Jaiprakash N. Sangshetti
Journal:   Archiv der Pharmazie
Jahrgang:   2016
Seiten:   n/a
DOI:   10.1002/ardp.201600254
Erscheinungsdatum:   16.11.2016
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