Pharmacological Studies on Novel Triazino Quinolines

Namitha R,Selvi G,G Sathya Priyadarshini

doi:10.13189/app.2021.090401

Abstract

Pharmacological importance of the nitrogen heterocycles is countless. The triazines are found to possess exceptional biological antitumor, anti-HIV, antiviral, antimalarial, antimicrobial, cytotoxic activities. The current investigation attempts to evaluate invitro antibacterial, antifungal, antioxidant potential, and cytotoxicity of newly synthesized substituted 4'-methyl-3-thioxo-1,2,4-triazinoquinolin-5-one. The antimicrobial activity was done by Agar Well Diffusion Method and the MIC of the compound was found using the Broth dilution assay method. The compounds showed excellent antibacterial activity against selected bacterial strains, including Gram-positive S. aureus, S. pyogens, and Gram-negative bacteria P. aeroginosa, E. coli, K. peumoniae, Pseudomonas Sp with the zones of inhibition 9 to 19nm. The standard drug Ampicillin showed a maximum inhibitory zone 18 nm. Among all the screened compounds, sample exhibited good activity. Similarly, the compounds were screened for antifungal properties, which showed an excellent reduction in the growth of selected fungal strain for Candida albicans. The compounds were also screened for 1,1-diphenyl-2-picrylhydrazyl (DPPH) activity. Cytotoxicity was done in Dalton's Lymphoma Ascites (DLA) cells which were obtained from Amala Cancer Research Center. The tested compounds exhibited significant antioxidant activity in a concentration-dependent manner.

Highlights

The compounds with quinoline moiety are well branded due to their extensive biological activity [1]
8-hydroxyquinoline and its derivatives were established into antifungal clinical use and novel compounds of this type are still investigated [2,3,4]
Dalton’s Lymphoma Ascites (DLA) cells were obtained from Amala Cancer Research Center

Summary

Introduction

The compounds with quinoline moiety are well branded due to their extensive biological activity [1]. 8-hydroxyquinoline and its derivatives were established into antifungal clinical use and novel compounds of this type are still investigated [2,3,4]. The utility of quinoline derivatives in the areas of medicine [5] is well established. These compounds are found to possess various bioactivities such as anti-malarial [6,7,8], anti-bacterial [9,10,11,12], anti-fungal [13,14,15], and anti-cancer agents [16,17,18,19]. There is an urgent need for new antifungal remedies with novel modes of action due to a decreased antifungal susceptibility of newly emerging fungi in the growing set of immune compromised patients [20,21,22]

Methods

Results

Conclusion