Design, Synthesis, and Evaluation of Novel Quinazoline Derivatives as Anti-Inflammatory Agents

Year : 2026 | Volume : 13 | 01 | Page :
    By

    Pankaj Chaturvedi,

  • Abhinav Prasoon Mishra,

  • Vivek Dwivedi,

  • Saif Mohammed Saleh Ansari,

  1. Research Scholar, Departmen of Pharmaceutical Chemistry, Advance Institute of Biotech and Paramedical Sciences, Kanpur, Uttar Pradesh, India
  2. Professor, Departmen of Pharmaceutical Chemistry, Chandra Shekhar Singh College of Pharmacy, Koilaha, Kaushambi, Uttar Pradesh, India
  3. Professor, Departmen of Pharmaceutical Chemistry, Chandra Shekhar Singh College of Pharmacy, Koilaha, Kaushambi, Uttar Pradesh, India
  4. Junior Scientist, Department of Laboratory Animal Facility, Sam Higginbottom University of Agriculture, Technology & Sciences, Prayagraj, Uttar Pradesh, India

Abstract

Novel quinazoline derivatives are well-known heterocyclic scaffolds that are renowned for having a wide range of biological functions. A new quinazoline derivative was synthesized from anthranilic acid through a multi-step sequence involving amide formation, cyclization, and aromatic group substitution. The structure of the methoxy- and chloro-substituted final compound was confirmed by IR and 1H NMR spectroscopy. Evaluation of synthesized molecules anti-inflammatory activity using paw edema caused by carrageenan paradigm in Wistar rats demonstrated a significant reduction in edema, with efficacy comparable to the conventional drug diclofenac sodium. We propose that the enhanced activity stems from the electron-donating and withdrawing substituents, which may improve receptor binding and the overall pharmacodynamics profile. These findings position this quinazoline derivative could be potential alternative for new anti-inflammatory agents.

Keywords: Quinazoline, heterocyclic scaffolds, anthranilic acid, methoxy, spectroscopy, anti-inflammatory.

How to cite this article:
Pankaj Chaturvedi, Abhinav Prasoon Mishra, Vivek Dwivedi, Saif Mohammed Saleh Ansari. Design, Synthesis, and Evaluation of Novel Quinazoline Derivatives as Anti-Inflammatory Agents. Research & Reviews: A Journal of Drug Formulation, Development and Production. 2025; 13(01):-.
How to cite this URL:
Pankaj Chaturvedi, Abhinav Prasoon Mishra, Vivek Dwivedi, Saif Mohammed Saleh Ansari. Design, Synthesis, and Evaluation of Novel Quinazoline Derivatives as Anti-Inflammatory Agents. Research & Reviews: A Journal of Drug Formulation, Development and Production. 2025; 13(01):-. Available from: https://journals.stmjournals.com/rrjodfdp/article=2025/view=232355


References

  1. Serya RAT, Abbas AH, Ismail NSM, Esmat A, El Ella DAA. Design, synthesis and biological evaluation of novel quinazoline-based anti-inflammatory agents acting as PDE4B inhibitors. Chem Pharm Bull. 2015;63(2):102-116. doi:10.1248/cpb.c14-00737
  2. Nam KY, Damodar K, Lee Y, et al. Design and synthesis of π-extended resveratrol analogues and in vitro antioxidant and anti-inflammatory activity evaluation. Molecules. 2021;26(3). doi:10.3390/molecules26030646
  3. Abuelizz HA, Hassane A El, Marzouk M, Ezzeldin E, Ali AA, Al-Salahi R. Molecular modeling, enzyme activity, anti-inflammatory and antiarthritic activities of newly synthesized quinazoline derivatives. Future Med Chem. 2017;9(17):1995-2009. doi:10.4155/fmc-2017-0157
  4. Dash B, Dash S, Laloo D, Medhi C. Design, synthesis and Preliminary pharmacological screening (antimicrobial, analgesic and anti-inflammatory activity) of some novel quinazoline derivatives. J Appl Pharm Sci. 2017;7(6):083-096. doi:10.7324/JAPS.2017.70612
  5. Chandrika PM, Yakaiah T, Rao ARR, et al. Synthesis of novel 4,6-disubstituted quinazoline derivatives, their anti-inflammatory and anti-cancer activity (cytotoxic) against U937 leukemia cell lines. Eur J Med Chem. 2008;43(4):846-852. doi:10.1016/j.ejmech.2007.06.010
  6. Faraj FL, Zahedifard M, Paydar M, et al. Synthesis, characterization, and anticancer activity of new quinazoline derivatives against MCF-7 cells. Sci World J. 2014;2014. doi:10.1155/2014/212096
  7. Faisal M, Saeed A. Chemical Insights Into the Synthetic Chemistry of Quinazolines: Recent Advances. Front Chem. 2021;8(January):1-24. doi:10.3389/fchem.2020.594717
  8. Jafari E, Khajouei MR, Hassanzadeh F, Hakimelahi GH, Khodarahmi GA. Quinazolinone and quinazoline derivatives: Recent structures with potent antimicrobial and cytotoxic activities. Res Pharm Sci. 2016;11(1):1-14.
  9. Abdel-Aziz AAM, Abou-Zeid LA, ElTahir KEH, Mohamed MA, Abu El-Enin MA, El-Azab AS. Design, synthesis of 2,3-disubstitued 4(3H)-quinazolinone derivatives as anti-inflammatory and analgesic agents: COX-1/2 inhibitory activities and molecular docking studies. Bioorganic Med Chem. 2016;24(16):3818-3828. doi:10.1016/j.bmc.2016.06.026
  10. Poojari S, P PN, G K, Jithendra JK, N SK, Naik S. Anti-inflammatory, antibacterial and molecular docking studies of novel spiro-piperidine quinazolinone derivatives. J Taibah Univ Sci. 2017;11(3):497-511. doi:10.1016/j.jtusci.2016.10.003
  11. Mohamed MS, Kamel MM, Kassem EMM, Abotaleb N, Khedr M, Ahmed MF. Synthesis, biological evaluation and molecular docking of quinazoline-4(1H)-one derivatives as anti-inflammatory and analgesic agents. Acta Pol Pharm – Drug Res. 2011;68(5):665-675.
  12. Krishnarth N, Verma SK, Chaudhary A. Synthesis and anti-inflammatory activity of some novel quinazolinone derivatives. Fabad J Pharm Sci. 2020;45(3):205-210.
  13. Fayez N, Khalil W, Abdel-Sattar E, Abdel-Fattah AFM. In vitro and in vivo assessment of the anti-inflammatory activity of olive leaf extract in rats. Inflammopharmacology. 2023;31(3):1529-1538. doi:10.1007/s10787-023-01208-x
  14. Kolomoets O, Voskoboynik O, Antypenko O, et al. Design, synthesis and anti-inflammatory activity of derivatives 10-R-3-Aryl-6, 7-dihydro-2H-[1, 2, 4] triazino[2, 3-c]quinazolin-2-ones of spiro-fused cyclic frameworks. Acta Chim Slov. 2017;64(4):902-910. doi:10.17344/acsi.2017.3575
  15. Babu AN, Nadendla RR. Synthesis of some new quinazolinone formazans as anti-inflammatory and anthelmintic agents. J Pharm Res. 2011;4(March):2-5. http://jpronline.info/index.php/jpr/article/view/6835/3483

 

Ahead of Print Subscription Original Research
Volume 13
01
Received 24/10/2025
Accepted 31/10/2025
Published 16/11/2025
Publication Time 23 Days
202

Login


My IP

PlumX Metrics