Spiro Benzodiazepine Substituted Fluorocoumarins as Potent Anti-Anxiety Agents
1,5-Benzodiazepines are one of the important class of tranquilizers. The fusion of heterocyclic systems like coumarins and indolines with the benzodiazepine seems quite encouraging for the synthesis of derivatives with enhanced anti-anxiety property. The benzodiazepine derivatives containing fluorin...
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| Veröffentlicht in: | Russian journal of bioorganic chemistry 2021-03, Vol.47 (2), p.390-398 |
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| container_title | Russian journal of bioorganic chemistry |
| container_volume | 47 |
| creator | Patagar, Dayanand Uttarkar, Akshay Patra, Swarna M. Patil, Jagadish H. Kusanur, Raviraj Niranjan, Vidya Kumar, H. G. Ashok |
| description | 1,5-Benzodiazepines are one of the important class of tranquilizers. The fusion of heterocyclic systems like coumarins and indolines with the benzodiazepine seems quite encouraging for the synthesis of derivatives with enhanced anti-anxiety property. The benzodiazepine derivatives containing fluorine were synthesized and studied for their anti-anxiety activity on mice using plus maze apparatus with sodium pentabarbitone as the standard. Compound with mono substituted fluorine showed comparable anti-anxiety activity with the standard. The docking studies with Translocator protein (TSPO) (PDB: 4UC2) were done and further supported by molecular dynamics simulations. The in vivo test results are in well agreement with docking and molecular dynamics simulation studies. |
| doi_str_mv | 10.1134/S1068162021020199 |
| format | Article |
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The in vivo test results are in well agreement with docking and molecular dynamics simulation studies.</description><subject>Anxiety</subject><subject>Benzodiazepines</subject><subject>Biochemistry</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedical materials</subject><subject>Biomedicine</subject><subject>Bioorganic Chemistry</subject><subject>Fluorine</subject><subject>Heterocyclic compounds</subject><subject>In vivo methods and tests</subject><subject>Life Sciences</subject><subject>Molecular docking</subject><subject>Molecular dynamics</subject><subject>Organic Chemistry</subject><subject>Substitutes</subject><subject>Tranquilizers</subject><issn>1068-1620</issn><issn>1608-330X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2021</creationdate><recordtype>article</recordtype><recordid>eNp1UN9LwzAQDqLgnP4BvhV8ruaSJksf63AqDBWq4FtJ03RkzKQmKbj99WZM8EF8uTvu-3Hch9Al4GsAWtzUgLkATjABTDCU5RGaAMcipxS_H6c5wfkeP0VnIawxBoyZmKCnejDeZbfa7lxn5E4PxuqsHtsQTRyj7rLFZnTeKTd-SG9syGTIXlzUNmaVjSav7JfRcZtVq7QK5-ikl5ugL376FL0t7l7nD_ny-f5xXi1zRYHHvBOy7cqSs54KQmZAFAZFZClmqoW-7KmUBcOCFZRymopWvBCFmDEiOmCtpFN0dfAdvPscdYjN2o3eppMNYZCInAieWHBgKe9C8LpvBm_SG9sGcLOPrfkTW9KQgyYkrl1p_-v8v-gbyh9t-g</recordid><startdate>20210301</startdate><enddate>20210301</enddate><creator>Patagar, Dayanand</creator><creator>Uttarkar, Akshay</creator><creator>Patra, Swarna M.</creator><creator>Patil, Jagadish H.</creator><creator>Kusanur, Raviraj</creator><creator>Niranjan, Vidya</creator><creator>Kumar, H. 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| source | Springer Nature - Complete Springer Journals |
| subjects | Anxiety Benzodiazepines Biochemistry Biomedical and Life Sciences Biomedical materials Biomedicine Bioorganic Chemistry Fluorine Heterocyclic compounds In vivo methods and tests Life Sciences Molecular docking Molecular dynamics Organic Chemistry Substitutes Tranquilizers |
| title | Spiro Benzodiazepine Substituted Fluorocoumarins as Potent Anti-Anxiety Agents |
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