Author(s):
Talitoshi Imchen, Abhishek Kumar, Pankaj Kumar, Gupta Dheeraj Rajesh, M Chandana Adiga, Krishnapriya K R, Aravinda Pai
Email(s):
abhi12bunty@nitte.edu.in
DOI:
10.52711/0974-360X.2025.00547 
Address:
Talitoshi Imchen1, Abhishek Kumar1*, Pankaj Kumar1, Gupta Dheeraj Rajesh1, M Chandana Adiga1, Krishnapriya K R1, Aravinda Pai2
1Nitte (Deemed to be University), NGSM Institute of Pharmaceutical Sciences (NGSMIPS), Department of Pharmaceutical Chemistry, Mangalore, India.
2Department of Pharmaceutical Chemistry, Manipal Academy of Higher Education, Manipal College of Pharmaceutical Sciences (MCOPS), Manipal, (Karnataka) India.
*Corresponding Author
Published In:
Volume - 18,
Issue - 8,
Year - 2025
ABSTRACT:
Depression is a frequent mental illness that can alter a person's social and psychological behaviour by raising or lowering their mood. An estimated 700,000 deaths annually are attributed to depression, making it the fourth leading cause of suicide death for people between the ages of 15 and 29. Depression continues to be a significant worldwide health burden despite improvements in knowledge and treatment. Nowadays, antidepressant medications, surgery, and lifestyle changes are used to treat depression. Antidepressant medications, however, have the potential to have negative effects and may not work for certain depressed individuals. Research is now being conducted to find novel drugs and therapies for depression. Ten compounds were synthesized in this study based on two different ring configurations, and their in silico activity was evaluated (PDB ID: 6OL9). Targeting the M5-T4L receptor was the goal, with imipramine as the reference drug. According to the results, the ten newly developed compounds had much higher docking scores than the typical medication. These substances also showed a high propensity for binding and hydrophobic interaction.
Cite this article:
Talitoshi Imchen, Abhishek Kumar, Pankaj Kumar, Gupta Dheeraj Rajesh, M Chandana Adiga, Krishnapriya K R, Aravinda Pai. Design and Evaluation of Furan Incorporated 1,5-benzodiazepine Targeting M5-T4L Receptor as Antidepressant. Research Journal Pharmacy and Technology. 2025;18(8):3800-6. doi: 10.52711/0974-360X.2025.00547
Cite(Electronic):
Talitoshi Imchen, Abhishek Kumar, Pankaj Kumar, Gupta Dheeraj Rajesh, M Chandana Adiga, Krishnapriya K R, Aravinda Pai. Design and Evaluation of Furan Incorporated 1,5-benzodiazepine Targeting M5-T4L Receptor as Antidepressant. Research Journal Pharmacy and Technology. 2025;18(8):3800-6. doi: 10.52711/0974-360X.2025.00547 Available on: https://www.rjptonline.org/AbstractView.aspx?PID=2025-18-8-50
REFERENCE:
1. Depression n.d. https://www.who.int/news-room/fact-sheets/detail/depression (accessed November 24, 2022).
2. Margret Chandira, Mehul, BS Venkateshwarlu, Chiranjib, Debjit, B Jayakar. Design, Development and Evaluation of Extended Release Multiunit Particulate System of Novel Class-I Antidepressant Drug. Research J. Pharm. and Tech. 2010; 3(1): Jan-Mar. 277-286.
3. Cianconi P, Betrò S, Janiri L. The impact of climate change on mental health: a systematic descriptive review. Frontiers in Psychiatry. 2020; Mar 6; 11: 490206.
4. Benazzi F. Various forms of depression. Dialogues Clin Neurosci. 2006;8:151–61. https://doi.org/10.31887/DCNS.2006.8.2/fbenazzi.
5. Owens MJ, Nemeroff CB. Role of serotonin in the pathophysiology of depression: focus on the serotonin transporter. Clin Chem. 1994; 40: 288–95. https://doi.org/10.1093/clinchem/40.2.288.
6. G. Venkatesha, C. Kalaiyarasia, M. Ramanathana. Antidepressant like Effect of Gabapentin Decreases the Immobility Time in Despair Animal Models in Mice: Roll of Serotonergic System in it. Research J. Pharm. and Tech. 2011; 4(11): 1702-1706.
7. Lunkad A.S., Kothawade S.N., Jadhav D.V., Chaudhari P.S., Bornare S.P. Synthesis and Antimicrobial Activity of Some New Chalcones Containing Benzofuran and Benzofuran Schiff Bases. Research J. Pharm. and Tech. 2015; 8(3): 276-279.
8. Saeid H, Al-sayed H, Bader M. A review on biological and medicinal significance of furan. AJMAS. 2023; Feb 18: 44-58. https://journal.utripoli.edu.ly/index.php/Alqalam/article/view/145
9. Chetan M Bhalgat, Sachin L Patil, Sandeep K Chitale, Krantisinha Randive, Kumar G Patil, Santosh Patil. Synthesis and Cytotoxic Studies of Newer 3-(1-Benzofuran-2-Yl)-5-(Substituted Aryl) Isoxazole. Research J. Pharm. and Tech. 2011; 4(2): 247-251.
10. Chandak BG, Sarpate RV, Chatterjee NR, Baheti KG. Synthesis, Spectral Studies and Biological Activity of Some 1, 5-Benzodiazepine Derivatives. Research J. Pharm. and Tech. 2010; 3 (3): 938-941.
11. Parag S. Mahadik, Senthilkumar G.P., Amol S. Powar, Devprakash D., Tamizh Mani T., Sulbha A. Gavali. Chemical and Biological Properties of Benzodiazepines- An overview. Research J. Pharm. and Tech. 2012; 5(2): 181-189.
12. Aastha P, Navneet K, Anshu A, Pratima S, Dharma K. 1, 5 Benzodiazepines: overview of properties and synthetic aspects. Res. J. Chem. 2013; 3(7): 90-103.
13. Du Y, Du B, Diao Y, Yin Z, Li J, Shu Y, Zhang Z, Chen L. Comparative efficacy and acceptability of antidepressants and benzodiazepines for the treatment of panic disorder: A systematic review and network meta-analysis. Asian Journal of Psychiatry. 2021; Jun 1; 60: 102664.
14. Lim B, Sproule BA, Zahra Z, Sunderji N, Kennedy SH, Rizvi SJ. Understanding the effects of chronic benzodiazepine use in depression: a focus on neuropharmacology. Int Clin Psychopharmacol. 2020; Sep 1; 35(5): 243-53.
15. Ramjith U.S., Shahin Muhammed. Molecular Docking Study of Novel Imidazo[2,1-b]-1,3,4 thiadiazole derivatives. Research J. Pharm. and Tech. 2013; 6(6): June 688-694.
16. Pattar SV, Adhoni SA, Kamanavalli CM. In silico molecular docking studies and MM / GBSA analysis of coumarin- carbonodithioate hybrid derivatives divulge the anticancer potential against breast cancer. Beni-Suef University Journal of Basic and Apllied Sciences. 2020; https://doi.org/10.1186/s43088-020-00059-7.
17. Genheden S, Ryde U. The MM/PBSA and MM/GBSA methods to estimate ligand-binding affinities. Expert Opin Drug Discov. 2015;10:449–61. https://doi.org/10.1517/17460441.2015.1032936.
18. Kumar A, Kumar P, Chaithanya P, Suhasini S, Gupta DR, Bhaskar VK. Design and evaluation of thiophene incorporated benzothiazepines targeting GABA-A receptor as anticonvulsant. Research J. Pharm. and Tech. 2024: 17(5): 2114-20. DOI: 10.52711/0974-360X.2024.00335
19. A El-Helby AG, Ayyad RRA, Zayed MF, Abulkhair HS, Elkady H, El-Adl K. Design, synthesis, in silico ADMET profile and GABA ‐ A docking of novel phthalazines as potent anticonvulsants. Arch Pharm (Weinheim). 2019; 352(5): e1800387. https://doi.org/10.1002/ardp.201800387
20. Rajesh GD, Kumar P, Purohit S, Kumar A, Apte K. In-silico ADME, Docking Studies, Synthesis of Thiadiazolyl benzimidazole linked Azetidinone derivatives as an Antitubercular agent. Research J. Pharm. and Tech. 2024: 17(6): 2628-32. DOI: 10.52711/0974-360X.2024.00411
21. Zahran EM, Abdelmohsen UR, Kolkeila A, Salem A, Khalil HE, Desoukey SY, et al. Anti-epileptic potential, metabolic profiling and in silico studies of the aqueous fraction from Ocimum menthiifolium benth, family Lamiaceae. Nat Prod Res. 2021; 35(24): 5972-76. https://doi.org/10.1080/14786419.2020.1809396
22. Muhammad Arba, Jasriati Jasriati. Structure-based Pharmacophore Modelling for identifying VEGFR2 Inhibitor. Research J. Pharm. and Tech. 2020; 13(7): 3129-3134.