Author(s): Vidya Murugeshwari, Abhirami PV, Shridhar Deshpande N. Anusha S, Ranjitha Acharya, Arvinda Pai, Pradeep Kumar MR, Pankaj Kumar

Email(s): pankajpgr@gmail.com

DOI: 10.52711/0974-360X.2026.00372   

Address: Vidya Murugeshwari1, Abhirami PV1, Shridhar Deshpande N1. Anusha S1, Ranjitha Acharya1, Arvinda Pai2, Pradeep Kumar MR3, Pankaj Kumar1*
1Nitte (Deemed to be University), NGSM Institute of Pharmaceutical Sciences (NGSMIPS), Department of Pharmaceutical Chemistry, Mangalore, India.
2Department of Pharmaceutical Chemistry, MCOPS, MAHE, Manipal, Karnataka, India.
3Department of Pharmaceutical Chemistry, KLE College of Pharmacy, KAHER, Hubballi, Karnataka.
*Corresponding Author

Published In:   Volume - 19,      Issue - 6,     Year - 2026


ABSTRACT:
Depression is a common CNS disorder caused by serotonin and dopamine imbalances. In this study, we designed 1,3,4-oxadiazole-linked chromone derivatives. Molecular docking against 5-hydroxytryptamine 1A receptors revealed that various designed derivatives had a higher docking score than Imipramine. Further analysis predicted that these derivatives had the highest binding efficiency and adhered to the rule of five, suggesting favourable drug-like properties. Based on the In-silico study, nine different derivatives were synthesized using three-step reactions: firstly, Schiff base, followed by cyclization, and characterized by IR, mass, and ¹H NMR spectroscopy. Finally, these compounds were evaluated for antidepressant and antioxidant activity using the forced swim test, DPPH, and nitric oxide scavenging methods. The forced swim test revealed that VAD2 and VAD8 have substantial antidepressant activity at low and medium doses. DPPH and nitric oxide scavenging methods showed that compounds VAD1 and VAD9 had notable antioxidant activity.


Cite this article:
Vidya Murugeshwari, Abhirami PV, Shridhar Deshpande N. Anusha S, Ranjitha Acharya, Arvinda Pai, Pradeep Kumar MR, Pankaj Kumar. Design and Synthesis of Oxadiazole-integrated Chromone Derivatives Targeting 5-HT1A Receptor as Anti-depressant Agents. Research Journal Pharmacy and Technology. 2026;19(6):2598-4. doi: 10.52711/0974-360X.2026.00372

Cite(Electronic):
Vidya Murugeshwari, Abhirami PV, Shridhar Deshpande N. Anusha S, Ranjitha Acharya, Arvinda Pai, Pradeep Kumar MR, Pankaj Kumar. Design and Synthesis of Oxadiazole-integrated Chromone Derivatives Targeting 5-HT1A Receptor as Anti-depressant Agents. Research Journal Pharmacy and Technology. 2026;19(6):2598-4. doi: 10.52711/0974-360X.2026.00372   Available on: https://rjptonline.org/AbstractView.aspx?PID=2026-19-6-29


REFERENCES: 
1.    Chaurasia J, Mishra R, Mishra B. Synthesis and antidepressant evaluation of heteroaromatic derivatives of gallic acid. Research Journal of Pharmacy and Technology. 2023; 16(11):  5051-7. DOI: 10.52711/0974-360X.2023.00818 
2.    GD Rajesh, M Vidya, K Pankaj, K Abhishek, Design and in silico evaluation of oxadiazole-linked chromone derivatives as anti-depressant agents, Research Journal of Chemistry and Environment. 2024; 28(1). doi: https://doi.org/10.25303/281rjce73079
3.    Kumar A, Kumar P, Shravya H, Pai A. Coumarins as potential anticoagulant agents. Research Journal of Pharmacy and Technology. 2022; 15(4): 1659-63. DOI: 10.52711/0974-360X.2022.00277
4.    Kumar P, Kumar A. Synthesis and biological evaluation of pyrimidine derivatives via pyrrolyl chalcones. Research Journal of Pharmacy and Technology. 2017; 10(5): 1392-4. DOI:10.5958/0974-360X.2017.00248.7
5.    Yerrakula G, George SG, Kumar PR, Kumar DK, Venkatachalam S. Ensuring safety of novel oral anticoagulants' predictable dose response relationship. Research Journal of Pharmacy and Technology. 2022; 15(10): 4812-8. DOI: 10.52711/0974-360X.2022.00808
6.    Patil ML, Gaikwad SS, Kapare HS. A systematic review on antimicrobial applications of nanofibres. Research Journal of Pharmacy and Technology. 2024; 17(1): 427-3210.52711/0974-360X.2024.00067.
7.    Chaurasia J, Mishra R, Mishra B. Synthesis and antidepressant evaluation of heteroaromatic derivatives of gallic acid. Research Journal of Pharmacy and Technology. 2023; 16(11): 5051-7. DOI:10.52711/0974-360X.2023.00818
8.    Bhat KI, Apoorva A, Kumar A, Kumar P. Synthesis and antidiabetic evaluation of some new coumarin coupled 4-thiazolidinone derivatives. Research Journal of Pharmacy and Technology. 2019; 12(11): 5215-8 DOI: 10.5958/0974-360X.2017.00248.7.
9.    Bhat KI, Apoorva A, Kumar A, Kumar P. Synthesis and Antioxidant Activity of Some New Coumarin Incorporated 4-Thiazolidinone Derivatives. Research Journal of Pharmacy and Technology. 2018; 11(12): 5408-12. DOI: 10.5958/0974-360X.2018.00987.3 
10.    Akwu NA, Lekhooa M, Deqiang D, Aremu AO. Antidepressant effects of coumarins and their derivatives: A critical analysis of research advances. European Journal of Pharmacology. 2023 Oct 5; 956: 175958. DOI:.org/10.1016/j.ejphar.2023.175958
11.    Hamoud MM, Osman NA, Rezq S, Abd El-wahab HA, Hassan AE, Abdel-Fattah HA, Romero DG, Ghanim AM. Design and synthesis of novel 1, 3, 4-oxadiazole and 1, 2, 4-triazole derivatives as cyclooxygenase-2 inhibitors with anti-inflammatory and antioxidant activity in LPS-stimulated RAW264. 7 macrophages. Bioorganic Chemistry. 2022 Jul 1; 124: 105808. DOI: org/10.1016/j.bioorg.2022.105808
12.    Abhishek K, Jennifer F, Pankaj K. Synthesis, antimicrobial and antiinflammatory activity of newly synthesized isoxazoline incorporated 2-Quinolones. Int J Pharm Sci Drug Res. 2014; 6(2): 124-7.
13.    Tantray MA, Khan I, Hamid H, Alam MS, Dhulap A, Kalam A. Synthesis of benzimidazole-linked-1, 3, 4-oxadiazole carboxamides as GSK-3β inhibitors with in vivo antidepressant activity. Bioorganic Chemistry. 2018 Apr 1; 77: 393-401. DOI:org/10.1016/j.ejphar.2023.175958
14.    Rajesh GD, Koshy AJ, Akshay SD, Dwivedi PS, Ashtekar H, Rehman N, Kumar P. Inhibition of β-lactamase by Novel Benzothiazole-Coupled Azetidinone Derivatives: A Comprehensive Study Using an In silico and In vitro Approaches Against Multi Drug Resistant Bacteria. Journal of Computational Biophysics and Chemistry. 2024 Nov 8; 23(09): 1145-63. DOI: org/10.1142/S2737416524500340
15.    Rajesh GD, Apte K, Abhirami PV, Anusha S, Ranjitha A, Kumar SB, Sarvottam K, Kumar P. Comprehensive In Silico Analysis of Flavonoids in Breast Cancer Using Molecular Docking, ADME, and Molecular Dynamics Simulation Approach. Peptide Science. 2025; Jan; 117(1): e24391.DOI:10.1002/pep2.24391
16.    Niu P, Kang J, Tian X, Song L, Liu H, Wu J, Yu W, Chang J. Synthesis of 2-amino-1, 3, 4-oxadiazoles and 2-amino-1, 3, 4-thiadiazoles via sequential condensation and I2-mediated oxidative C–O/C–S bond formation. The Journal of Organic Chemistry. 2015 Jan 16; 80(2): 1018-24. DOI: org/10.1021/jo502518c.
17.    Kaviarasan, L., Gowramma, B., Kalirajan, R., Mevithra, M., and Chandralekha, S. (2020). Molecular docking studies and synthesis of a new class of chroman-4-one fused 1,3,4-thiadiazole derivatives and evaluation for their anticancer potential. Journal of the Iranian Chemical Society, 17(8), 2083–2094. DOI:10.1007@s13738-020-01913-2.
18.    G Dheeraj, P Kumar, K Apte, H Ashtekar, SR Dixit,Molecular docking, ADME analysis, and pharmacophore modelling of benzoxazole fused azetidinone derivatives as antibreast cancer agents,Ann. Phytomed, 2023; (12). DOI: http://dx.doi.org/10.54085/ap.2023.12.1.37
19.    Marref SE, Benkiki N, Melakhessou MA. In vitro antioxidant activity, total phenolics, and flavonoids contents of Gladiolus segetum Extracts. Research Journal of Pharmacy and Technology. 2018; 11(11): 5017-23.
20.    Kumar A, Fernandes J, Kumar P. Synthesis and biological evaluation of some novel isoxazoline derivatives of carbostyril. International Journal of Pharmacy and Pharmaceutical Sciences. 2014; 3: 1267-77. DOI:10.5958/0974-360X.2018.00915.0
21.    Ruhoğlu O, Özdemir Z, Çaliş U, Gümüşel B, Bilgin AA. Synthesis of and pharmacological studies on the antidepressant and anticonvulsant activities of some 1, 3, 5-trisubstituted pyrazolines. Arzneimittelforschung. 2005 Aug; 55(08): 431-6. DOI: 10.1055/s-0031-1296884
22.    Sahu RP, Gupta SP. Synthesis and Antidepressant activity of some N-substituted-2-phenyl indole derivatives. Research Journal of Pharmacy and Technology. 2023; 16(6): 2715-8. DOI:10.52711/0974-360X.2023.00446

Recomonded Articles:

Research Journal of Pharmacy and Technology (RJPT) is an international, peer-reviewed, multidisciplinary journal.... Read more >>>

RNI: CHHENG00387/33/1/2008-TC                     
DOI: 10.52711/0974-360X 

1.3
2021CiteScore
 
56th percentile
Powered by  Scopus


SCImago Journal & Country Rank

Journal Policies & Information


Recent Articles




Tags


Not Available