Journal
BIOORGANIC CHEMISTRY
Volume 75, Issue -, Pages 118-126Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2017.08.016
Keywords
Benzimidazole derivatives; Liquid phase combinatorial synthesis; Human dihydroorotate dehydrogenase (hDHODH) hDHODH inhibitors
Funding
- SERB project Government of India
- Department of Science and Technology (DST) India [SB/S1/OC-61/2013]
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The synthesis of 1,2,5-trisubstituted benzimidazole derivatives was carried out using liquid phase combinatorial approach using soluble polymer assisted support (PEG5000). Synthesised compounds were characterised by FTIR, ESI-MS, H-1 NMR and C-13 NMR. The purity of compounds was confirmed with HPLC analysis. Compounds were also docked into the binding site of human dihydroorotate dehydrogenase (hDHODH). The synthesised compounds were screened for hDHODH enzyme inhibition assay using brequinar as standard compound. The synthesised compounds demonstrated comparative biological activity. Synthesised compounds 8d and 8e demonstrated IC50 value of 81 +/- 2 nM and 97 +/- 2 nM, respectively. (C) 2017 Elsevier Inc. All rights reserved.
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