In:
Scientific Reports, Springer Science and Business Media LLC, Vol. 10, No. 1 ( 2020-06-30)
Abstract:
In continuation of our work on enzyme inhibition, the benzofuran-based-thiazoldinone analogues ( 1–14 ) were synthesized, characterized by HREI-MS, 1 H and 13 CNMR and evaluated for urease inhibition. Compounds 1–14 exhibited a varying degree of urease inhibitory activity with IC 50 values between 1.2 ± 0.01 to 23.50 ± 0.70 µM when compared with standard drug thiourea having IC 50 value 21.40 ± 0.21 µM. Compound 1, 3, 5 and 8 showed significant inhibitory effects with IC 50 values 1.2 ± 0.01, 2.20 ± 0.01, 1.40 ± 0.01 and 2.90 ± 0.01 µM respectively, better than the rest of the series. A structure activity relationship (SAR) of this series has been established based on electronic effects and position of different substituents present on phenyl ring. Molecular docking studies were performed to understand the binding interaction of the compounds.
Type of Medium:
Online Resource
ISSN:
2045-2322
DOI:
10.1038/s41598-020-67414-7
Language:
English
Publisher:
Springer Science and Business Media LLC
Publication Date:
2020
detail.hit.zdb_id:
2615211-3
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