Author(s): Kamya Goyal, Anju Goyal, Rajendra Awasthi, Nidhi Rani, Rajwinder Kaur


DOI: 10.52711/0974-360X.2023.00317   

Address: Kamya Goyal1,2, Anju Goyal2, Rajendra Awasthi3, Nidhi Rani2, Rajwinder Kaur2*
1Department of Pharmaceutical Chemistry and Analysis, Laureate Institute of Pharmacy, Jawalamukhi, Himachal Pradesh, India.
2Department of Pharmaceutical Chemistry, Chitkara College of Pharmacy, Chitkara University, Punjab, India.
3Department of Pharmaceutical Sciences, School of Health Sciences and Technology, University of Petroleum and Energy Studies (UPES), Energy Acres, Dehradun, Uttarakhand, India.
*Corresponding Author

Published In:   Volume - 16,      Issue - 4,     Year - 2023

In recent years, complications of micro-organisms, which becomes drug-resistant, have extended dreadful level across the globe. One of the significant challenges in drug discovery to overcome the increased development of drug resistance is developing novel chemical moieties that advantageously comprise chemical features different from existing chemical entities. This communication presents the synthesis, docking, and antibacterial and antifungal evaluation of nitro chalcones. New series of nitro substituted chalcone derivatives (1-12) were synthesized via Claisen-Schmidt condensation using substituted acetophenone and various substituted benzaldehydes in the presence of base and ethanol. Spectral analysis of the synthesized compounds was carried out using 1H-NMR, IR, 13C-NMR and HRMS methods. Synthesized derivatives were evaluated for antimicrobial potency via the microdilution method against two Gram-positive and two Gram-negative bacterial strains and two fungal strains. All compounds showed promising antimicrobial potency. However, compound 6 was the most potent derivative of the series against all the tested antibacterial strains. Compounds 10 and 12 were found to be the most potent analogues of the series against all the tested antifungal strains. All the synthesized derivatives had good antifungal potency in comparison to the antibacterial potency. Based on the preliminary study results, the study concluded that the synthesized chalcones derivatives promise antimicrobial activity that may be further investigated to achieve antimicrobial lead.

Cite this article:
Kamya Goyal, Anju Goyal, Rajendra Awasthi, Nidhi Rani, Rajwinder Kaur. Synthesis and Biological Evaluation of Nitro-substituted chalcones as potent Antibacterial and Antifungal agents. Research Journal of Pharmacy and Technology 2023; 16(4):1931-9. doi: 10.52711/0974-360X.2023.00317

Kamya Goyal, Anju Goyal, Rajendra Awasthi, Nidhi Rani, Rajwinder Kaur. Synthesis and Biological Evaluation of Nitro-substituted chalcones as potent Antibacterial and Antifungal agents. Research Journal of Pharmacy and Technology 2023; 16(4):1931-9. doi: 10.52711/0974-360X.2023.00317   Available on:

1.    Aslam B. Wang W. Arshad MI. Khurshid M. Muzammil S. Rasool MH. Nisar MA. Alvi RF. Aslam MA Qamar MU. Salamat MK. Antibiotic resistance: a rundown of a global crisis. Infection and Drug Resistance. 2018;11:1645-1658.
2.    Dadgostar P. Antimicrobial resistance: implications and costs. Infection and Drug Resistance. 2019;12:3903-3910.
3.    Juma A. Lemoine P. Simpson AB. Murray J. O’Hagan BM. Naughton PJ. Dooley JG. Banat IM. Microscopic investigation of the combined use of antibiotics and biosurfactants on methicillin resistant Staphylococcus aureus. Frontiers in Microbiology. 2020;11:1477.
4.    Song M. Liu Y. Huang X. Ding S. Wang Y. Shen J. Zhu K. A broad-spectrum antibiotic adjuvant reverses multidrug-resistant Gram-negative pathogens. Nature Microbiology. 2020;5(8):1040-1050.
5.    Dangi LL. Dulawat MS. Tiwari P. Dulawat SS. New substituted m-Phenoxy chalcones; their synthesis by microwave irradiation and antifungal activity. Asian Journal of Research in Chemistry. 2013;6(5):461-463.
6.    Rammohan A. Reddy JS. Sravya G. Rao CN. Zyryanov GV. Chalcone synthesis, properties and medicinal applications: a review. Environmental Chemistry Letters. 2020;18(2):433-458.
7.    Kaundal V. Singh D. Vipasha. Devi A. Jindal S. Ankalgi AD. Goyal K. A Laconic Review on Chalcones: Synthesis, Antimicrobial and Antioxidant activities. Sciences. 2022; 12(1):21-28.
8.    Baviskar B. Patel S. Baviskar B. Khadabadi SS. Shiradkar M. Design and synthesis of some novel chalcones as potent antimicrobial agent. Asian Journal of Research in Chemistry. 2008;1(2):67-69.
9.    Dawane BS. Shaikh BM. Khandare NT. Mandawad GG. Chobe SS. Konda SG. Synthesis of Some Novel Substituted Pyrazole Based Chalcones and Their In-Vitro Antimicrobial Activity. Asian Journal of Research in Chemistry. 2010;3(1):90-93.
10.    Singh D. Kaundal V. Aggarwal N. Jindal S. Ankalgi AD. Goyal K. A Concise Review on Synthesis, Anti-Inflammatory, and Antioxidant Activities of Chalcone. Asian Journal of Pharmaceutical Research. 2022; 12(1):37-44.
11.    Monga V. Goyal K. Steindel M. Malhotra M. Rajani DP. Rajani SD. Synthesis and evaluation of new chalcones, derived pyrazoline and cyclohexenone derivatives as potent antimicrobial, antitubercular and antileishmanial agents. Medicinal Chemistry Research. 2014;23(4):2019-2032.
12.    Bhat KI. Kumar A. Synthesis and Biological Evaluation of Some Novel Pyrazoline Derivatives Derived from Chalcones. Research Journal of Pharmacy and Technology. 2017;10(5):1344-6.
13.    ur Rashid H. Xu Y. Ahmad N. Muhammad Y. Wang L. Promising anti-inflammatory effects of chalcones via inhibition of cyclooxygenase, prostaglandin E2, inducible NO synthase and nuclear factor κb activities. Bioorganic Chemistry. 2019;87:335-365.
14.    Kumar P. Kumar A. Pinto JS. Akshata G. Synthesis and Biological Evaluation of Pyrimidine Derivatives Via Pyrrolyl Chalcones. Research Journal of Pharmacy and Technology. 2017;10(5):1392-4.
15.    Shaik A. Kishor P. Kancharlapalli V. Synthesis of novel and potential antimicrobial, antioxidant and anticancer chalcones and dihydropyrazoles bearing isoxazole scaffold. In Multidisciplinary Digital Publishing Institute Proceedings 2020 (Vol. 41, No. 1, p. 16).
16.    Rao GE. Rahaman SA. Rani AP. Rao CM. Synthesis, Characterization and Antimicrobial Activity of Novel Chalcones from 1-[4-(1H-imidazol-1-yl) Phenyl]Ethanone. Asian Journal of Research in Chemistry. 2013;6(7):7.
17.    Narwal S. Kumar S. Verma PK. Synthesis and biological activity of new chalcone scaffolds as prospective antimicrobial agents. Research on Chemical Intermediates. 2021;47(4):1625-1641.
18.    Prabhakar V. Babu KS. Ravindranath LK. Basha MS. Latha J. Application of Chalcones in Synthesis of Novel 1, 5-Benzodiazepine Derivatives Containing Thieno [2, 3-d] Pyrimidine Core Unit and its Biological Activity Screening. Asian Journal of Research in Chemistry. 2017;10(2):71-84.
19.    Goyal K. Kaur R. Goyal A. Awasthi R. Chalcones: A review on synthesis and pharmacological activities. Journal of Applied Pharmaceutical Science. 2021;11:001-14.
20.    Mokle SS. Sayyed MA. Vibhute AY. Khansole SV. Nalwar YS. Vibhute YB. Synthesis of Some New Bioactive Chalcones and Flavones. Research Journal of Pharmacy and Technology. 2009;2(4):846-9.
21.    Sharma P. Kumar S. Ali F. Anthal S. Gupta VK. Khan IA. Singh S. Sangwan PL. Suri KA. Gupta BD. Gupta DK. Synthesis and biologic activities of some novel heterocyclic chalcone derivatives. Medicinal Chemistry Research. 2013;22(8):3969-83.
22.    K Sahu N. S Balbhadra S. Choudhary J. V Kohli D. Exploring pharmacological significance of chalcone scaffold: a review. Current Medicinal Chemistry. 2012;19(2):209-25.
23.    Higuchi K. Watanabe T. Tanigawa T. Tominaga K. Fujiwara Y. Arakawa T. Sofalcone, a gastroprotective drug, promotes gastric ulcer healing following eradication therapy for Helicobacter pylori: A randomized controlled comparative trial with cimetidine, an H2‐receptor antagonist. Journal Of Gastroenterology and Hepatology. 2010;25:S155-60.
24.    Weindorf N. Schultz-Ehrenburg U. Controlled study of increasing venous tone in primary varicose veins by oral administration of Ruscus aculeatus and trimethylhespiridinchalcone. Zeitschrift fur Hautkrankheiten. 1987;62(1):28-38. PMID: 3554800
25.    Ngameni B. Cedric K. Mbaveng AT. Erdoğan M. Simo I. Kuete V. Daştan A. Design, synthesis, characterization, and anticancer activity of a novel series of O-substituted chalcone derivatives. Bioorganic & Medicinal Chemistry Letters. 2021;35:127827.
26.    Balouiri M. Sadiki M. Ibnsouda SK. Methods for in vitro evaluating antimicrobial activity: A review. Journal of Pharmaceutical Analysis. 2016;6(2):71-79.
27.    Thomsen R. Christensen MH. MolDock: a new technique for high-accuracy molecular docking. Journal of Medicinal Chemistry. 2006;49(11):3315-3321.
28.    Rani N. Kumar P. Singh R. Sharma A. Molecular docking evaluation of imidazole analogues as potent Candida albicans 14α-demethylase inhibitors. Current Computer-Aided Drug Design. 2015;11(1):8-20.
29.    Rani N. Singh R. Molecular modelling investigation of some new 2-mercaptoimidazoles. Current Computer-Aided Drug Design. 2017;13(1):48-56.
30.    Bitencourt-Ferreira G. Azevedo WF. Molegro virtual docker for docking. In Docking screens for drug discovery 2019 (pp. 149-167). Humana, New York, NY.
31.    Qin HL. Zhang ZW. Lekkala R. Alsulami H. Rakesh KP. Chalcone hybrids as privileged scaffolds in antimalarial drug discovery: a key review. European Journal of Medicinal Chemistry. 2020;193:112215.

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