Novel peptidomimetic peptide deformylase (PDF) inhibitors of Mycobacterium tuberculosis.
Chem Biol Drug Des. 2020 Aug 03;:
Authors: Gokhale KM, Telvekar VN
Emergence of MDR and XDR-TB led to the failure of available anti-tubercular drugs. In-order to explore, identify and develop new antitubercular drugs, novel peptidomimetic series of Mtb-Peptide Deformylase (PDF) inhibitors was designed and synthesized. In-vitro antimycobacterial potential of compounds was established by screening of compounds against Mycobacterium tuberculosis H37Rv strain using MABA assay. Among them ester series of compounds 4a, 4b, 4c, 4d, 4e were found most active, with compound 4c being highly active and exhibiting minimum inhibitory concentration of 6.25 µg/ml against M.tb H37Rv strain. Additionally; the compounds were docked to determine the probable binding interactions and understand the mechanism of action of most active molecules on Mtb-peptide deformylase (PDF), which is involved in the mycobacterium protein synthesis.
PMID: 32745362 [PubMed - as supplied by publisher]