Novel Anthranilic Acid Hybrids—An Alternative Weapon against Inflammatory Diseases
Anti-inflammatory drugs are used to relieve pain, fever, and inflammation while protecting the cardiovascular system. However, the side effects of currently available medications have limited their usage. Due to these adverse effects, there is a significant need for new drugs. The current trend of r...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-11-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/16/12/1660 |
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| author | Miglena Milusheva Mina Todorova Vera Gledacheva Iliyana Stefanova Mehran Feizi-Dehnayebi Mina Pencheva Paraskev Nedialkov Yulian Tumbarski Velichka Yanakieva Slava Tsoneva Stoyanka Nikolova |
| author_facet | Miglena Milusheva Mina Todorova Vera Gledacheva Iliyana Stefanova Mehran Feizi-Dehnayebi Mina Pencheva Paraskev Nedialkov Yulian Tumbarski Velichka Yanakieva Slava Tsoneva Stoyanka Nikolova |
| author_sort | Miglena Milusheva |
| collection | DOAJ |
| description | Anti-inflammatory drugs are used to relieve pain, fever, and inflammation while protecting the cardiovascular system. However, the side effects of currently available medications have limited their usage. Due to these adverse effects, there is a significant need for new drugs. The current trend of research has shifted towards the synthesis of novel anthranilic acid hybrids as anti-inflammatory agents. Phenyl- or benzyl-substituted hybrids exerted very good anti-inflammatory effects in preventing albumin denaturation. To confirm their anti-inflammatory effects, additional ex vivo tests were conducted. These immunohistochemical studies explicated the same compounds with better anti-inflammatory potential. To determine the binding affinity and interaction mode, as well as to explain the anti-inflammatory activities, the molecular docking simulation of the compounds was investigated against human serum albumin. The biological evaluation of the compounds was completed, assessing their antimicrobial activity and spasmolytic effect. Based on the experimental data, we can conclude that a collection of novel hybrids was successfully synthesized, and they can be considered anti-inflammatory drug candidates—alternatives to current therapeutics. |
| first_indexed | 2024-03-08T20:27:04Z |
| format | Article |
| id | doaj.art-859710c41d264c9a8a36f496ca527460 |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-08T20:27:04Z |
| publishDate | 2023-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-859710c41d264c9a8a36f496ca5274602023-12-22T14:31:21ZengMDPI AGPharmaceuticals1424-82472023-11-011612166010.3390/ph16121660Novel Anthranilic Acid Hybrids—An Alternative Weapon against Inflammatory DiseasesMiglena Milusheva0Mina Todorova1Vera Gledacheva2Iliyana Stefanova3Mehran Feizi-Dehnayebi4Mina Pencheva5Paraskev Nedialkov6Yulian Tumbarski7Velichka Yanakieva8Slava Tsoneva9Stoyanka Nikolova10Department of Organic Chemistry, Faculty of Chemistry, University of Plovdiv, 4000 Plovdiv, BulgariaDepartment of Organic Chemistry, Faculty of Chemistry, University of Plovdiv, 4000 Plovdiv, BulgariaDepartment of Medical Physics and Biophysics, Faculty of Pharmacy, Medical University of Plovdiv, 4002 Plovdiv, BulgariaDepartment of Medical Physics and Biophysics, Faculty of Pharmacy, Medical University of Plovdiv, 4002 Plovdiv, BulgariaDepartment of Chemistry, Faculty of Science, University of Sistan and Baluchestan, Zahedan P.O. Box 98135-674, IranDepartment of Medical Physics and Biophysics, Faculty of Pharmacy, Medical University of Plovdiv, 4002 Plovdiv, BulgariaDepartment of Pharmacognosy, Faculty of Pharmacy, Medical University of Sofia, 1000 Sofia, BulgariaDepartment of Microbiology, Technological Faculty, University of Food Technologies, 4002 Plovdiv, BulgariaDepartment of Microbiology, Technological Faculty, University of Food Technologies, 4002 Plovdiv, BulgariaDepartment of Analytical Chemistry and Computer Chemistry, University of Plovdiv, 4000 Plovdiv, BulgariaDepartment of Organic Chemistry, Faculty of Chemistry, University of Plovdiv, 4000 Plovdiv, BulgariaAnti-inflammatory drugs are used to relieve pain, fever, and inflammation while protecting the cardiovascular system. However, the side effects of currently available medications have limited their usage. Due to these adverse effects, there is a significant need for new drugs. The current trend of research has shifted towards the synthesis of novel anthranilic acid hybrids as anti-inflammatory agents. Phenyl- or benzyl-substituted hybrids exerted very good anti-inflammatory effects in preventing albumin denaturation. To confirm their anti-inflammatory effects, additional ex vivo tests were conducted. These immunohistochemical studies explicated the same compounds with better anti-inflammatory potential. To determine the binding affinity and interaction mode, as well as to explain the anti-inflammatory activities, the molecular docking simulation of the compounds was investigated against human serum albumin. The biological evaluation of the compounds was completed, assessing their antimicrobial activity and spasmolytic effect. Based on the experimental data, we can conclude that a collection of novel hybrids was successfully synthesized, and they can be considered anti-inflammatory drug candidates—alternatives to current therapeutics.https://www.mdpi.com/1424-8247/16/12/1660synthesishybrid moleculesanthranilic acidin silicoDFT calculationsdocking |
| spellingShingle | Miglena Milusheva Mina Todorova Vera Gledacheva Iliyana Stefanova Mehran Feizi-Dehnayebi Mina Pencheva Paraskev Nedialkov Yulian Tumbarski Velichka Yanakieva Slava Tsoneva Stoyanka Nikolova Novel Anthranilic Acid Hybrids—An Alternative Weapon against Inflammatory Diseases Pharmaceuticals synthesis hybrid molecules anthranilic acid in silico DFT calculations docking |
| title | Novel Anthranilic Acid Hybrids—An Alternative Weapon against Inflammatory Diseases |
| title_full | Novel Anthranilic Acid Hybrids—An Alternative Weapon against Inflammatory Diseases |
| title_fullStr | Novel Anthranilic Acid Hybrids—An Alternative Weapon against Inflammatory Diseases |
| title_full_unstemmed | Novel Anthranilic Acid Hybrids—An Alternative Weapon against Inflammatory Diseases |
| title_short | Novel Anthranilic Acid Hybrids—An Alternative Weapon against Inflammatory Diseases |
| title_sort | novel anthranilic acid hybrids an alternative weapon against inflammatory diseases |
| topic | synthesis hybrid molecules anthranilic acid in silico DFT calculations docking |
| url | https://www.mdpi.com/1424-8247/16/12/1660 |
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