Synthesis, Characterization and Antitubercular Activity of Novel Chalcone Derivatives by Inha Targeting

Santanu Kumar Hotta; Biswanath Prusty; Jochhana Rani Bhuyan; Subhrarani Sahu

doi:10.37022/jiaps.v10i2.705

Santanu Kumar Hotta Associate professor, Department of Pharmaceutical Chemistry, College of Pharmaceutical Sciences, Berhampur, Ganjam, Odisha, pin- 760002, India
Biswanath Prusty Assistant professor, Department of Pharmaceutical Analysis, College of Pharmaceutical Sciences, Berhampur, Ganjam, Odisha, pin- 760002, India
Jochhana Rani Bhuyan Assistant professor, Department of Pharmaceutics, College of Pharmaceutical Sciences, Berhampur, Ganjam, Odisha, pin- 760002, India
Subhrarani Sahu Assistant professor, Department of Pharmaceutical Chemistry, College of Pharmaceutical Sciences, Berhampur, Ganjam, Odisha, pin- 760002, India

DOI https://doi.org/10.37022/jiaps.v10i2.705

Abstract

Background: The authors targeted InhA to estimate the therapeutic potential of novel chalcones against tuberculosis. Methods: 07 synthesized compounds were tested for in vitro antimycobacterial activity against Mycobacterium tuberculosis (H37RV; American Type Culture Collection number: 27294) using the microplate Alamar Blue assay. Results: The most potent compounds, trans-1-(2-napthyl)-3-phenyl-2-propen-1-one showed in vitro activity, with a minimum inhibitory concentration (MIC) of 1.16 μg/ml. Conclusion: Compound code 1e i.e. trans-1-(2-napthyl)-3-phenyl-2-propen-1-one showed strong in vitro antimycobacterial activity at a concentration of 1,16 μg/ml.

Keywords: Chalcones, InhA, H37RV strain, microplate Alamar Blue assay, Anti-tubercular activity

Downloads

Download data is not yet available.

References

1. Bharathi, R., & Santhi, N. (2021). Synthesis, Characterization, In-Silico Docking Study and In-Vitro AntiInflammatory Activities of Novel Chalcone Derivatives. Journal of Biotechnology & Bioinformatics Research, 3(2), 1–6. https://doi.org/10.47363/jbbr/2021(3)133
2. Global Tuberculosis Report 2020. World Health Organisation. 2020 October 15.
3. ChauhanA, KumarM, KumarA, KanchanK(2021) Comprehensive review on mechanism of action, resistance and evolution of antimycobacterial drugs. Life Sci 119301.
4. Martins F, Santos S, Ventura C, Elvas-Leitão R, Santos L, Vitorino S, Reis M, Miranda V, Correia HF, Aires-de-Sousa J, Kovalishyn V, Latino DaRS, Ramos J, Viveiros M. Design, synthesis and biological evaluation of novel isoniazid derivatives with potent antitubercular activity. Eur. J. Med. Chem. 2014; 81:119–138. DOI: 10.1016/j.ejmech.2014.04.077 [PubMed: 24836065]
5. E. Bogatcheva, C. Hanrahan, B. Nikonenko, R. Samala, P. Chen, J. Gearhart, F. Barbosa, L. Einck, C.A. Nacy, M. Protopopova, Identification of New Diamine Scaffolds with Activity against Mycobacterium tuberculosis, Journal of Medicinal Chemistry, Vol.49, No.11, 2006, pp. 30453048.
6. Y.L. Janin, Antituberculosis drugs: Ten years of research, Bioorganic and Medicinal Chemistry, Vol.15, No.7, 2007, pp. 2479 2513.
7. C.B. Inderlied, C.A. Kemper, and L.E. Bermudez, The Mycobacterium avium complex, Clinical Microbiology Reviews, Vol.6, No.3, 1993, pp. 266310.
8. Batran, R. Z., Sabt, A., Dziadek, J., & Kassem, A. F. (2024). Design, synthesis and computational studies of new azaheterocyclic coumarin derivatives as antiMycobacterium tuberculosis agents targeting enoyl acyl carrier protein reductase (InhA). RSC advances, 14(30), 21763-21777.
9. H. Getahun, A. Matteelli, R.E. Chaisson, M. Raviglione, Latent Mycobacterium tuberculosis infection, N. Engl. J. Med. 372 (2015) 2127e2135, https://doi.org/ 10.1056/NEJMra1405427.
10. Zhou, B.; Xing, C. Diverse Molecular Targets for Chalcones with Varied Bioactivities. Med. Chem. 2015, 5, 388−404. (2) Batovska, D. I.; Todorova, I. T. Trends in utilization of the pharmacological potential of chalcones. Curr. Clin. Pharmacol. 2010, 5, 1−29
11. Sahu, N. K.; Balbhadra, S. S.; Choudhary, J.; Kohli, D. V. Exploring pharmacological significance of chalcone scaffold: a review. Curr. Med. Chem. 2012, 19, 209−225
12. Dimmock, J. R.; Elias, D. W.; Beazely, M. A.; Kandepu, N. M. Bioactivities of chalcones. Curr. Med. Chem. 1999, 6, 1125−1149.