SYNTHESIS OF NOVEL 4,6-DIPHENYLPYRIMIDINE SUBSTITUTED BENZAMIDE DERIVATIVES ITS CHARACTERIZATION AND EVALUATION FOR ANTI-OXIDANT AND ANTI-MICROBIAL ACTIVITIES

Main Article Content

Dr. AJITHA MAKULA
SANA TABASSUM

Abstract

The research work involves the estimation and evaluation of pharmacological activity of designed 4, 6-diphenylpyrimidine substituted benzamide derivatives that act as HDAC inhibitors. The Histone deacetylases inhibitors are a new class of cytostatic agents that exhibits promising results cancer treatment. The four HDAC inhibitors approved by FDA for cancer chemotherapy is SAHA (Vorinostat), Belinostat (PXD-101), Panobinostat (LBH-589), and Romidepsin (FK-228). The six novel 4, 6-diphenylpyrimidine substituted benzamide derivatives were synthesized, characterized and evaluated for anti-microbial and anti-oxidant activities. The designed molecule with cap group as substituted 4, 6-diphenylpyrimidine of functional groups adjacent to the metal-binding benzamide was evaluated for the pharmacological activity evaluation. Prior to this, the work was done on in-silico studies by molecular docking and confirmed the anti-cancer activity. The Anti-oxidant and Anti-microbial activity was evaluated as per standard methods. Anti-microbial activities involve the Anti-bacterial and Anti-fungal activity estimation. Hence, based on the pharmacological activity results, it is confirmed that the designed and characterized novel 4, 6-diphenylpyrimidine substituted benzamide exhibited the biological activity of Anti-oxidant and Anti-microbial activity.

Downloads

Download data is not yet available.

Article Details

How to Cite
MAKULA, D. A., & TABASSUM, S. (2023). SYNTHESIS OF NOVEL 4,6-DIPHENYLPYRIMIDINE SUBSTITUTED BENZAMIDE DERIVATIVES ITS CHARACTERIZATION AND EVALUATION FOR ANTI-OXIDANT AND ANTI-MICROBIAL ACTIVITIES. Journal of Advanced Scientific Research, 14(04), 13-25. https://doi.org/10.55218/JASR.202314404
Section
Research Article

References

1. Kelly WK, Marks PA. Nature Clinical Practice Oncology, 2005; 2(3): 150–157. Doi: https://doi.org/10.1038/ncponc0106.
2. Anna G, Nikolaos G, Christos D, et al. Journal of the Balkan Union of Oncology, 2018; 23(4): 846-861.
3. Sabrina SF, Maureen JO, et al. Scientific Reports, 2018; 8: 1-11. Doi: https://doi.org/10.1038/s41598-018-31125-x
4. Kristensen LS, Nielsen HM, et al. European Journal of Pharmacology, 2009; 625: 131-142. Doi: https://doi.org/10.1016/j.ejphar.2009.10.011.
5. Ajitha Raj M, Sandhya Rani N. Journal of Pharma Research, 2022; 11(3): 1-11. Doi: https://doi.org/10.5281/zenodo.6844683
6. Bing W, Xiaolei Z, et al. Free Radical Biology and Medicine, 2012; 52(5): 928–936. Doi: https://doi.org/10.1016/j.freeradbiomed.2011.12.006.
7. Simona B, Emilia C, et al. Journal of Medicinal Chemistry, 2022; 65: 3080-3097. Doi: https://doi.org/10.1021/acs.jmedchem.1c02067
8. Roche J, Bertrand P. European Journal of Medicinal Chemistry, 2016; 121: 451-483. Doi: https://doi.org/10.1016/j.ejmech.2016.05.047.
9. Di Micco S, Chini MG, et al. Bioorganic & Medicinal Chemistry, 2013; 21(13): 3795–3807. Doi: https://doi.org/10.1016/j.bmc.2013.04.036.
10. Mounyr B, Moulay S, Saad KI. Journal of Pharmaceutical Analysis, 2016; 6(2): 71-79. Doi: https://doi.org/10.1016/j.jpha.2015.11.005
11. Moharram HA, Youssef MM. Alexandria Journal of Food Science and Technology, 2014; 11(1): 31-42.