New Benzothiazole-based Thiazolidinones as Potent Antimicrobial Agents. Design, synthesis and Biological Evaluation

Abstract

The twelve new compounds were synthesized and studied for their antimicrobial activity. The compounds appeared to be promising antimicrobial agents and could be the lead compounds for new, more potent drugs. According to the docking prediction, the compounds could be MurB inhibitors.

Theoretical investigations on the HOMO–LUMO gap and global reactivity descriptor studies, natural bond orbital, and nucleus-independent chemical shifts analyses of 3-phenylbenzo[d]thiazole-2(3H)-imine and its para-substituted derivatives: Solvent and substituent effects

“…The values of the LUMO-HOMO energy gap reflect the chemical activity of the molecule. The decrease in the HOMO-LUMO energy gap explains the eventual charge transfer interaction taking place within the studied compounds [1][2][3][4][5][6] because of the strong electron-accepting ability of the electron acceptor group (Table 4). As a result, the stability of the studied compounds is 1 > 3 > 2 > 4 > 5 > 6.…”

“…Such compounds are used as building blocks in organic synthesis due to their wide range of biological activities, and they form core in various drugs such as anticancer, antimicrobial, antiasthmatic, antitumor, antibacterial, antitubercular, anticonvulsant, anti-HIV, anti-inflammatory, antifungal, antiproliferative, antiviral, anti-Alzheimer, antimalarial, and anti-diabetic, agents. [4][5][6][7][8][9][10][11][12][13] Herein, we report a facile, environmentally friendly method for intramolecular cyclization under solvent-free conditions. The reaction occurs in two steps in the presence of sodium tertbutoxide as a strong base.…”

Therapeutic advancement of benzothiazole derivatives in the last decennial period

“…Among the Gram‐negative bacteria, the most sensitive to the tested compounds was Salmonella typhimurium , while Escherichia coli was the most resistant one. As for the Gram‐positive bacteria, the most sensitive was Bacillus cereus , while Mariniluteicoccus flavus was found to be the most resistant …”

NEW ROUTE FOR THE SYNTHESES OF SOME NOVEL DERIVATIVES OF 3-ARYL BENZO[d] THIAZOLE-2(3H)-IMINE FROM HIGH SUBSTITUTED THIOUREAS

“…Benzothiazole is an organosulfur, as well as organonitrogen heterocyclic compound was a which benzene ring is fused with thiazole [4][5][6][7][8][9][10][11][12][13]. Benzothiazoles are an important class of heterocyclic compounds that act as core nucleus in various drugs such as anticancer [5,14], antileishmanial [15], antimicrobial [9,16], anti-asthmatic [11], antitumor [6], antibacterial [17,18], anti-tubercular, [19] anticonvulsant [4,20], anti-HIV [15,21], anti-inflammatory [5,7], antifungal [9,13], antiproliferative [6,14,21,22], antiviral [23], anti-Alzheimer [10,14], antimalarial [15], and antidiabetic [24][25][26] effects. The related research and developments in BTA-based medicinal chemistry have become a rapidly developing and increasingly active topic [6,19].…”