SYNTHESIS AND BIOLOGICAL EVALUATION OF 1H-(INDOLE-5-YL)-3-SUBSTITUTED-1,2,4-OXADIAZOLES AS NOVEL 5-LOX INHIBITORS
: A series of indolyloxadiazoles were synthesized from amidoxime and indole 3-carboxaldehyde using CAN as a catalyst and PEG as a solvent. In vitro, a 5-LOX inhibitory assay has been performed for all the synthesized compounds. Among the tested compounds, 4bf showed the highest potency (IC50 18.78 µ...
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| Format: | Article |
| Language: | English |
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Turkish Chemical Society
2024-02-01
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| Series: | Journal of the Turkish Chemical Society, Section A: Chemistry |
| Subjects: | |
| Online Access: | https://dergipark.org.tr/tr/download/article-file/3292409 |
| _version_ | 1797215228214116352 |
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| author | Siddaiah Vidavalur Sunanda Kumari Kadiri Berihu Tekluu |
| author_facet | Siddaiah Vidavalur Sunanda Kumari Kadiri Berihu Tekluu |
| author_sort | Siddaiah Vidavalur |
| collection | DOAJ |
| description | : A series of indolyloxadiazoles were synthesized from amidoxime and indole 3-carboxaldehyde using CAN as a catalyst and PEG as a solvent. In vitro, a 5-LOX inhibitory assay has been performed for all the synthesized compounds. Among the tested compounds, 4bf showed the highest potency (IC50 18.78 µg/ml). The synthesized compound carried out docking on the 5-LOX enzyme protein crystal structure. Compound (4bf) docked snugly into the receptor site with a score of -9.1 Kcal/mol, and it showed strong hydrogen bond interactions with two key amino acids, His368 and Asn555. |
| first_indexed | 2024-04-24T11:26:44Z |
| format | Article |
| id | doaj.art-68e2113f6acf4e73ba7617a618877ea8 |
| institution | Directory Open Access Journal |
| issn | 2149-0120 |
| language | English |
| last_indexed | 2024-04-24T11:26:44Z |
| publishDate | 2024-02-01 |
| publisher | Turkish Chemical Society |
| record_format | Article |
| series | Journal of the Turkish Chemical Society, Section A: Chemistry |
| spelling | doaj.art-68e2113f6acf4e73ba7617a618877ea82024-04-10T16:03:42ZengTurkish Chemical SocietyJournal of the Turkish Chemical Society, Section A: Chemistry2149-01202024-02-01111111810.18596/jotcsa.1334005182SYNTHESIS AND BIOLOGICAL EVALUATION OF 1H-(INDOLE-5-YL)-3-SUBSTITUTED-1,2,4-OXADIAZOLES AS NOVEL 5-LOX INHIBITORSSiddaiah Vidavalur0Sunanda Kumari Kadiri1Berihu Tekluu2AndhraGitamAksum: A series of indolyloxadiazoles were synthesized from amidoxime and indole 3-carboxaldehyde using CAN as a catalyst and PEG as a solvent. In vitro, a 5-LOX inhibitory assay has been performed for all the synthesized compounds. Among the tested compounds, 4bf showed the highest potency (IC50 18.78 µg/ml). The synthesized compound carried out docking on the 5-LOX enzyme protein crystal structure. Compound (4bf) docked snugly into the receptor site with a score of -9.1 Kcal/mol, and it showed strong hydrogen bond interactions with two key amino acids, His368 and Asn555.https://dergipark.org.tr/tr/download/article-file/32924091-2-4-oxadiazolesindolyloxadiazoles5-lox inhibitors |
| spellingShingle | Siddaiah Vidavalur Sunanda Kumari Kadiri Berihu Tekluu SYNTHESIS AND BIOLOGICAL EVALUATION OF 1H-(INDOLE-5-YL)-3-SUBSTITUTED-1,2,4-OXADIAZOLES AS NOVEL 5-LOX INHIBITORS Journal of the Turkish Chemical Society, Section A: Chemistry 1-2-4-oxadiazoles indolyloxadiazoles 5-lox inhibitors |
| title | SYNTHESIS AND BIOLOGICAL EVALUATION OF 1H-(INDOLE-5-YL)-3-SUBSTITUTED-1,2,4-OXADIAZOLES AS NOVEL 5-LOX INHIBITORS |
| title_full | SYNTHESIS AND BIOLOGICAL EVALUATION OF 1H-(INDOLE-5-YL)-3-SUBSTITUTED-1,2,4-OXADIAZOLES AS NOVEL 5-LOX INHIBITORS |
| title_fullStr | SYNTHESIS AND BIOLOGICAL EVALUATION OF 1H-(INDOLE-5-YL)-3-SUBSTITUTED-1,2,4-OXADIAZOLES AS NOVEL 5-LOX INHIBITORS |
| title_full_unstemmed | SYNTHESIS AND BIOLOGICAL EVALUATION OF 1H-(INDOLE-5-YL)-3-SUBSTITUTED-1,2,4-OXADIAZOLES AS NOVEL 5-LOX INHIBITORS |
| title_short | SYNTHESIS AND BIOLOGICAL EVALUATION OF 1H-(INDOLE-5-YL)-3-SUBSTITUTED-1,2,4-OXADIAZOLES AS NOVEL 5-LOX INHIBITORS |
| title_sort | synthesis and biological evaluation of 1h indole 5 yl 3 substituted 1 2 4 oxadiazoles as novel 5 lox inhibitors |
| topic | 1-2-4-oxadiazoles indolyloxadiazoles 5-lox inhibitors |
| url | https://dergipark.org.tr/tr/download/article-file/3292409 |
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