Development and Applications of a Simple Chalcone- Based Low Molecular Weight Ligand for Treating Nosocomial Infections due to Staphylococcus aureus and Escherichia coli

Authors

  • Kanhaiya M Dadure Department of Chemistry, Bajaj College of Science College, Wardha 442001, Maharashtra, India
  • Animeshchandra G M Haldar Department of Applied Chemistry, Priyadarshini Bhagwati College of Engineering, Nagpur 440009, Maharashtra, India
  • Debarshi Kar Mahapatra Department of Pharmaceutical Chemistry, Dadasaheb Balpande College of Pharmacy, Nagpur 440037, Maharashtra, India

DOI:

https://doi.org/10.37591/rrjom.v10i2.2059

Keywords:

Chalcone, Thiophene, Synthesis, Escherichia coli, Staphylococcus aureus, Anti-microbial

Abstract

Abstract

Inspired from the available biological data of several imperative therapeutic scaffolds in several medicinal chemistry databases, thiophene-containing chalcone compounds were identified and the molecule was designed for treating various nosocomial infections. In one of the recent rational exploration, (E)-3-(4-methoxyphenyl)-1-(thiophen-2-yl)prop-2-en-1-one was synthesized in a single-step reaction, characterized comprehensively by using a few sophisticated spectroscopic instruments such as FT-IR spectroscopy, mass spectroscopy, and 1H-NMR spectroscopy, as well as CHN analyzer, and ultimately screened for its anti-bacterial potentials against gram-negative microbial species (Escherichia coli) and gram-positive microbial species (Staphylococcus aureus) using the conventional procedure. The chemical structure of the proposed molecule was completely recognized by sophisticated spectroscopic instruments. The compound exhibited an incredible anti-bacterial activity against anti-E. coli and expressed a fair bacterial activity against anti-S. aureus in in-vitro anti-microbial screening model, but with a very low potency. The compound was found to be more effective towards gram-negative species. The investigation pointed towards several prospective for the development of broad-spectrum anti-microbial drugs against resistant pathogenic strains by looking insights into the unexplored class of thiophene-containing chalcone compound.

Keywords: Anti-microbial, chalcone, Escherichia coli, Staphylococcus aureus, Thiophene synthesis

Cite this Article

Kanhaiya M. Dadure, Animeshchandra G.M. Haldar, Debarshi Kar Mahapatra. Development and Applications of a Simple Chalcone-Based Low Molecular Weight Ligand for Treating Nosocomial Infections due to Staphylococcus aureus and Escherichia coli. Research & Reviews: Journal of Medicine. 2020; 10(2): 14–18p.


Author Biographies

  • Kanhaiya M Dadure, Department of Chemistry, Bajaj College of Science College, Wardha 442001, Maharashtra, India

    Kanhaiya M. Dadure, PhD

    Assistant Professor,

    Department of Chemistry,

    Bajaj College of Science College,

    Wardha 442001, Maharashtra, India

  • Animeshchandra G M Haldar, Department of Applied Chemistry, Priyadarshini Bhagwati College of Engineering, Nagpur 440009, Maharashtra, India

    Animeshchandra G. M. Haldar, PhD

    Assistant Professor,

    Department of Applied Chemistry,

    Priyadarshini Bhagwati College of Engineering,

    Nagpur 440009, Maharashtra, India

  • Debarshi Kar Mahapatra, Department of Pharmaceutical Chemistry, Dadasaheb Balpande College of Pharmacy, Nagpur 440037, Maharashtra, India

    Debarshi Kar Mahapatra, PhD

    Assistant Professor,

    Department of Pharmaceutical Chemistry,

    Dadasaheb Balpande College of Pharmacy,

    Nagpur 440037, Maharashtra, India

References

Mahapatra DK, Bharti SK, Asati V. Chalcone derivatives: Anti-inflammatory potential and molecular targets perspectives. Curr Top Med Chem. 2017;17(28):3146-3169p.

Mahapatra DK, Bharti SK, Asati V. Anti-cancer Chalcones: Structural and molecular targets perspectives. Eur J Med Chem. 2015;98:69-114p.

Mahapatra DK, Bharti SK, Asati V. Chalcone scaffolds as anti-infective agents: Structural and molecular target perspectives. Eur J Med Chem. 2015;101:496-524p.

Mahapatra DK, Asati V, Bharti SK. Chalcones and their role in management of diabetes mellitus: Structural and pharmacological perspectives. Eur J Med Chem. 2015;92:839-865p.

Mahapatra DK, Bharti SK. Therapeutic Potential of chalcones as cardiovascular agents. Life Sci. 2016;148:154-172p.

Mahapatra DK, Bharti SK, Asati V, Singh SK. Perspectives of medicinally privileged chalcone based metal coordination compounds for biomedical applications. Eur J Med Chem. 2019;174:142-158p.

Mahapatra DK, Asati V, Bharti SK. An updated patent review of therapeutic applications of chalcone derivatives (2014-present). Exp Opin Therapeut Pat. 2019;29(5):385-406p.

Mahapatra DK, Asati V, Bharti SK. Recent therapeutic progress of chalcone scaffold bearing compounds as prospective anti-gout candidates. J Crit Rev. 2019;6(1):1-5p.

Mahapatra DK, Shivhare RS, Kumar P. Murrayanine-chalcone transformed into novel pyrimidine compounds demonstrated promising anti-inflammatory activity. Asian J Pharm Res. 2018;8(1):6-10p.

Mahapatra DK, Shivhare RS, Bharti SK. Novel Murrayanine based Pyrazole analogs as emerging anti-fungal candidates: Design, synthesis, characterization, and in vitro evaluation. Res Pharm. 2017;1(1):1-5p.

Mahapatra DK, Chhajed SS, Shivhare RS. Development of Murrayanine-Chalcone hybrids: An effort to combine two privilege scaffolds for enhancing hypoglycemic activity. Int J Pharm Chem Anal. 2017;4(2):30-34p.

Mahapatra DK, Shivhare RS. 3′,4′-Methylenedioxy Moiety Containing Murrayanine Based Chalcone as Emerging Anti-inflammatory Agent. J Mod Chem Chem Technol. 2018;9(1):12-16p.

Mahapatra DK, Shivhare RS, Asati V. Locomotor inhibitory activity of some Murrayanine-Chalcone based 2,3-dihydrobenzo[b][1,4]thiazepine derivatives: Exploring Anxiolytic potentials. Chron Pharm Sci. 2018;2(1):462-468p.

Mahapatra DK, Shivhare RS, Dadure KM. Transforming Murrayanine-Chalcone into corresponding 3H-benzo[b][1,4]diazepine derivatives: Accessing the anti-anxiety effect by inhibition of locomotor activity. Acta Scientific Pharm Sci. 2018;2(5):40-44p.

Mahapatra DK, Shivhare RS, Joseph TM. Design and characterization of Murrayanine linked Isoxazole derivatives: Novel class of bacteriocidal agents. Int J Res Drug Pharm Sci. 2017;1(1):11-15p.

Mahapatra DK, Shivhare RS. Anti-microbial Perspective of a Chalcone, (E)-1-(1-methoxy-9H-carbazol-3-yl)-3-(4-(methylsulfonyl)phenyl)prop-2-en-1-one: Fabrication of a Hybrid by Unification of a Natural Product with a Synthetic Component. Int J Agri Life Sci. 2018;4(2):236-240p.

Downloads

Published

2020-09-18

Issue

Vol. 10 No. 2 (2020)

Section

Research Article

License

Declaration and Copyright Transfer Form

(to be completed by authors)

I/ We, the undersigned author(s) of the submitted manuscript, hereby declare, that the above manuscript which is submitted for publication in the STM Journals(s), is not published already in part or whole (except in the form of abstract) in any journal or magazine for private or public circulation, and, is not under consideration of publication elsewhere.

  • I/We will not withdraw the manuscript after 1 week of submission as I have read the Author Guidelines and will adhere to the guidelines.
  • I/We Author(s ) have niether given nor will give this manuscript elsewhere for publishing after submitting in STM Journal(s).
  • I/ We have read the original version of the manuscript and am/ are responsible for the thought contents embodied in it. The work dealt in the manuscript is my/ our own, and my/ our individual contribution to this work is significant enough to qualify for authorship.
  •  I/We also agree to the authorship of the article in the following order:

Author’s name                                    

 

1. ________________

2. ________________

3. ________________

4. ________________

 

We  Author(s) tick this box and would request you to consider it as our signature as we agree to the terms of this Copyright Notice, which will apply to this submission if and when it is published by this journal.