Synthesis, in silico Profiling, in vitro Anthelmintic and Antibacterial Activities of Novel 6-Bromo-2-Phenyl-3-Substituted Quinazolin-4(3H)-ones

Bhargavi Posinasetty1,2,, Kishore Bandarapalle3,, Nihar Pillarikuppam4,, Rajasekhar Komarla Kumarachari4,*,, Geetha Birudala5, and Aruga Chandrakala6,

1Senior Clinical Data Manager, PROMETRIKA LLC, Cambridge, MA-02140, U.S.A.

2Government Dental College and Research Institute, Bellary-583104, India

3Department of Pharmaceutics, Sri Padmavathi School of Pharmacy, Tiruchanur, Tirupati-517503, India

4Department of Pharmaceutical Chemistry, Sri Padmavathi School of Pharmacy, Tiruchanur, Tirupati-517503, India

5Faculty of Pharmacy, Dr. M.G.R. Educational and Research Institute, Velappanchavadi, Chennai-600077, India

6Department of Pharmacology, S.V.U. College of Pharmaceutical Sciences, S.V. University, Tirupati-517501, India

*Corresponding author: Fax: +91 877 2237732; E-mail: komarla.research@gmail.com

Abstract

In this study, eight novel derivatives of 6-bromo-2-phenyl-3-substituted quinazolin-4(3H)-ones were synthesized, which was achieved through the use of bromoanthranilic acid, benzoyl chloride, and different substituted amino synthons. The chemical structures of these compounds through IR spectroscopy, 1H NMR spectroscopy, and mass spectrometry were successfully characterized. By employing computational tools like PASS, Molinspiration, Osiris, and Swiss ADME, we made predictions about the properties of these molecules. These predictions encompassed factors such as anthelmintic and antibacterial traits, drug-likeness, bioactivity scores, toxicity, and potential molecular targets. Furthermore, we performed in vitro assays to evaluate the bioactivities of the synthesized compounds. For anthelmintic effectiveness, the conventional method of assessing paralysis and mortality in earthworms for each compound was followed. The antibacterial efficacy was tested against both Gram-positive and Gram-negative bacterial strains, using the agar cup plate technique. The results of these assays provide valuable insights into the potential of these compounds as agents with anthelmintic and antibacterial properties.

Keywords

Bromo quinazolinones, Toxicity, Biological activity, Anthelmintic acitivity, Antibacterial activities.

   View Article PDF File Creative Commons License
This work is licensed under a Creative Commons Attribution 4.0 International License.