| Literature DB >> 29190478 |
Mahmood Ahmed1, Muhammad Abdul Qadir2, Abdul Hameed3, Muhammad Nadeem Arshad4, Abdullah M Asiri4, Muhammad Muddassar5.
Abstract
Curcumin is a multi-functional pharmacologically safe natural agent with proven cytoprotective effects to healthy human cells. In this study, a new series of sulfonamides with curcumin scaffold were synthesized, characterized and investigated for their carbonic anhydrase isoenzyme I (human) and II (bovine) isoforms. The structures of newly synthesized compounds were described by IR, 1H NMR and 13C NMR spectral data. Compound 14 showed the Ki value of 0.99 µM with highest inhibitory activity among all other synthesized compounds against hCA-I enzyme. Similarly enzyme kinetic studies of compound 14, 16 and 30 against bCAII enzyme showed Ki values of 0.71, 0.67 and 0.71 µM respectively. Our biological assays results showed that most of active compounds have similar inhibitory activities compared to standard acetazolamide drug. The molecular docking predicted binding modes showed that these compounds bind with hCA-1 enzyme in similar fashion.Entities:
Keywords: Carbonic anhydrase; Curcumin; Molecular docking; Sulfonamides
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Year: 2017 PMID: 29190478 DOI: 10.1016/j.bioorg.2017.11.015
Source DB: PubMed Journal: Bioorg Chem ISSN: 0045-2068 Impact factor: 5.275