Microwave assisted synthesis, biological evaluation, and molecular docking of novel chroman scaffolds incorporating spirochromanone framework
| Autor: | Gundu Srinivas, Aamate Vikas Kumar, Manga Vijjulatha, Malladi Srinivas Reddy, Dongamanti Ashok, Devulapally Mohan Gandhi, Sivan Sree Kanth |
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| Rok vydání: | 2016 |
| Předmět: |
Antioxidant
010405 organic chemistry Chemistry medicine.medical_treatment Organic Chemistry Pharmacology toxicology 010402 general chemistry Mass spectrometry Ascorbic acid 01 natural sciences Microwave assisted 0104 chemical sciences Microwave irradiation medicine Proton NMR Organic chemistry General Pharmacology Toxicology and Pharmaceutics Biological evaluation |
| Zdroj: | Medicinal Chemistry Research. 25:2882-2894 |
| ISSN: | 1554-8120 1054-2523 |
| Popis: | A series of novel chroman scaffold incorporate spirochromanone derivatives were synthesized from 2-hydroxyacetophenone and cyclic alkanones under microwave irradiation in good yields. Newly synthesized compounds were characterized by analytical and spectral (IR, proton nuclear magnetic resonance, 13C nuclear magnetic resonance, and mass spectrometry) methods. The synthesized compounds were evaluated for their antioxidant and anti-inflammatory activities and were compared with standard drugs. Among all the synthesized compounds 3d (6.09), 3g (5.32), 3h (2.03), 4a (1.17), 4b (0.50), 4c (6.59), 4d (7.86), 4e (6.85), 4f (4.82), and 4g (6.59) were exhibited higher antioxidant activity comparable to that of ascorbic acid (IC50 8.64 µM). The compounds 3a, 3b, 3c, 4c, and 4d were found to have good anti-inflammatory activity. The binding mode of the titled compounds has been proposed based on the molecular docking studies. |
| Databáze: | OpenAIRE |
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