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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Badavath, Vishnu N. Baysal, Ipek Uçar, Gülberk Mondal, Susanta K. Sinha, Barij N. Jayaprakash, Venkatesan |
| Description | Country affiliation: India Author Affiliation: Badavath VN ( Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Ranchi, Jharkhand, India.); Baysal I ( Department of Biochemistry, Faculty of Pharmacy, Hacettepe University, Sihhiye, Ankara, Turkey.); Uçar G ( Department of Biochemistry, Faculty of Pharmacy, Hacettepe University, Sihhiye, Ankara, Turkey.); Mondal SK ( TCG Lifesciences Ltd, Block-EP&GP, BIPL, Tower-B, Saltlake, Sector-V, Kolkata, West Bengal, India.); Sinha BN ( Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Ranchi, Jharkhand, India.); Jayaprakash V ( Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Ranchi, Jharkhand, India.) |
| Abstract | Ferulic acid has structural similarity with curcumin which is being reported for its monoamine oxidase (MAO) inhibitory activity. Based on this similarity, we designed a series of ferulic acid amides 6a-m and tested for their inhibitory activity on human MAO (hMAO) isoforms. All the compounds were found to inhibit the hMAO isoforms either selectively or non-selectively. Nine compounds (6a, 6b, 6g-m) were found to inhibit hMAO-B selectively, whereas the other four (6c-f) were found to be non-selective. There is a gradual shift from hMAO-B selectivity (6a,b) to non-selectivity (6c-f) as there is an increase in chain length at the amino terminus. In case of compounds having an aromatic nucleus at the amino terminus, increasing the carbon number between N and the aromatic ring increases the potency as well as selectivity toward hMAO-B. Compounds 6f, 6j, and 6k were subjected to membrane permeability and metabolic stability studies by in vitro assay methods. They were found to have a better pharmacokinetic profile than curcumin, ferulic acid, and selegiline. In order to understand the structural features responsible for the potency and selectivity of 6k, we carried out a molecular docking simulation study. |
| File Format | HTM / HTML |
| ISSN | 03656233 |
| Issue Number | 1 |
| Journal | Archiv der Pharmazie |
| Volume Number | 349 |
| e-ISSN | 15214184 |
| Language | English |
| Publisher | Wiley-VCH Verlag |
| Publisher Date | 2016-01-01 |
| Publisher Place | Germany |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | Discipline Pharmacology |
| Content Type | Text |
| Resource Type | Article |
| Subject | Drug Discovery Pharmaceutical Science |
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