A novel medium size lactam ring analoges as antibacterial agents: Synthesis, biological evaluation and molecular docking studies

Authors

  • Putcha A. N. V. Harita Department of Medicinal Chemistry, Guru Nanak Institutions Technical Campus, School of Pharmacy, Jawaharlal Nehru Technological University, Hyderabad-501301, India
  • Putcha Seshi Kumar Shantha Biotechnics private limited. A Sanofi company, Medchal, India-501401
  • Shiva Krishna Reddy Guduru Dr. Reddy's Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad, India-500 046
  • Parameshwar Ravula Department of Medicinal Chemistry, Guru Nanak Institutions Technical Campus, School of Pharmacy, Jawaharlal Nehru Technological University, Hyderabad-501301, India
  • J N Narendra Sharath Chandra Department of Pharmaceutical Chemistry, Bharat Institute of Technology, Mangalpally, Telanagana, India-501510

DOI:

https://doi.org/10.17179/excli2017-193

Keywords:

medium size ring, synthesis, coupling reaction, lactam, bacillus subtilis, anti-bacterial, docking

Abstract

A novel series of medium size (S)-3-alkyl-3,4,6,7-tetrahydro-1H-benzo[e][1,4]diazonine-2,5-dione (6a-f) analogues were synthesized from (E)-3-(2-nitrophenyl)acrylicacid (2) reacting with various amino acid esters using Di-isopropyl Carbodiimide as a coupling agent. The final cyclization is carried out by using reagent 1-Ethyl-3(3-dimethylaminopropyl) Carbodiimide Hydrochloride. The synthesized compounds have been supported by Mass, 1H-NMR and 13C-NMR. Further antibacterial studies were conducted, where some molecules are noticed with potent activity, especially molecule 6d shown highest activity which was also supported by molecular docking studies. All final molecules were docked with enzyme peptide deformylase to determine the probable binding conformation.

Downloads

Published

2017-08-14

How to Cite

Harita, P. A. N. V., Kumar, P. S., Reddy Guduru, S. K., Ravula, P., & Narendra Sharath Chandra, J. N. (2017). A novel medium size lactam ring analoges as antibacterial agents: Synthesis, biological evaluation and molecular docking studies. EXCLI Journal, 16, 1090–1098. https://doi.org/10.17179/excli2017-193

Issue

Vol. 16 (2017)

Section

Original articles

License

Authors who publish in this journal agree to the following terms:

  • The authors keep the copyright and grant the journal the right of first publication under the terms of the Creative Commons Attribution license, CC BY 4.0. This licencse permits unrestricted use, distribution and reproduction in any medium, provided that the original work is properly cited.
  • The use of general descriptive names, trade names, trademarks, and so forth in this publication, even if not specifically identified, does not imply that these names are not protected by the relevant laws and regulations.
  • Because the advice and information in this journal are believed to be true and accurate at the time of publication, neither the authors, the editors, nor the publisher accept any legal responsibility for any errors or omissions presented in the publication. The publisher makes no guarantee, express or implied, with respect to the material contained herein.
  • The authors can enter into additional contracts for the non-exclusive distribution of the journal's published version by citing the initial publication in this journal (e.g. publishing in an institutional repository or in a book).

Most read articles by the same author(s)