Academic Journal
Design, Synthesis, and In Vivo Evaluation of a New Series of Indole-Chalcone Hybrids as Analgesic and Anti-Inflammatory Agents
| العنوان: | Design, Synthesis, and In Vivo Evaluation of a New Series of Indole-Chalcone Hybrids as Analgesic and Anti-Inflammatory Agents |
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| المؤلفون: | Iman Baramaki, Mehlika Dilek Altıntop, Rana Arslan, Feyza Alyu Altınok, Ahmet Özdemir, Ilhem Dallali, Ahmed Hasan, Nurcan Bektaş Türkmen |
| سنة النشر: | 2024 |
| مصطلحات موضوعية: | Biochemistry, Genetics, Neuroscience, Pharmacology, Biological Sciences not elsewhere classified, Chemical Sciences not elsewhere classified, inhibiting edema formation, induced writhing tests, heteroaromatic aldehydes carrying, form pivotal interactions, different time intervals, thermal stimulus significantly, peripheral antinociceptive activities, highest efficacy results, one (< b, positive control drug, plate test similar, 7 , 4 , 1 -( 1, inflammatory agents indole, chalcones (< b, spinal response ), inflammatory activities, significantly effective, results revealed, immersion test, vivo <, silico <, p < |
| الوصف: | Indole-chalcone hybrids have burst into prominence as potent weapons in the battle against pain and inflammation due to their unique features, allowing these ligands to form pivotal interactions with biological targets. In this context, the base-catalyzed Claisen–Schmidt condensation of 3′,4′-(methylenedioxy)acetophenone with heteroaromatic aldehydes carrying an indole scaffold yielded new chalcones ( 1 – 7 ). The central and peripheral antinociceptive activities of all chalcones (compounds 1 – 7 ) at the dose of 10 mg/kg ( i.p .) were evaluated by hot plate (supraspinal response), tail immersion (spinal response), and acetic acid-induced writhing tests in mice. The anti-inflammatory activities of compounds 1 – 7 were also investigated by means of a carrageenan-induced mouse paw edema model. The results revealed that compounds 1 – 7 extended the latency of response to thermal stimulus significantly in a hot-plate test similar to dipyrone (300 mg/kg; i.p .), the positive control drug. However, only compounds 2 – 7 were found to be significantly effective in the tail-immersion test. Compounds 1 – 7 also significantly showed analgesic effect by reducing the number of writhes and anti-inflammatory activity by inhibiting edema formation at different time intervals and levels. 1-(1,3-Benzodioxol-5-yl)-3-(1-methyl-1 H -indol-2-yl)prop-2-en-1-one ( 4 ) drew attention by providing the highest efficacy results in both acute analgesia and inflammation models. Based on the in silico data acquired from the QikProp module, compound 4 was predicted to possess favorable oral bioavailability and drug-like properties. Taken together, it can be concluded that chalcones ( 1 – 7 ), especially compound 4 , are outstanding candidates for further research to investigate their potential use in the management of pain and inflammation. |
| نوع الوثيقة: | article in journal/newspaper |
| اللغة: | unknown |
| Relation: | https://figshare.com/articles/journal_contribution/Design_Synthesis_and_i_In_Vivo_i_Evaluation_of_a_New_Series_of_Indole-Chalcone_Hybrids_as_Analgesic_and_Anti-Inflammatory_Agents/25308544 |
| DOI: | 10.1021/acsomega.4c00026.s001 |
| الاتاحة: | https://doi.org/10.1021/acsomega.4c00026.s001 https://figshare.com/articles/journal_contribution/Design_Synthesis_and_i_In_Vivo_i_Evaluation_of_a_New_Series_of_Indole-Chalcone_Hybrids_as_Analgesic_and_Anti-Inflammatory_Agents/25308544 |
| Rights: | CC BY-NC 4.0 |
| رقم الانضمام: | edsbas.FC1717F7 |
| قاعدة البيانات: | BASE |
| DOI: | 10.1021/acsomega.4c00026.s001 |
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