Docking Related Survey on Heterocyclic Compounds Based on Glucosamine-6- Phosphate Synthase Inhibitors and their Antimicrobial Potential

Abstract

<jats:sec> <jats:title>:</jats:title> <jats:p>The synthetic heterocyclic compounds have their importance due to their wide applications in various fields of science. The heterocyclic compounds have been reported for their anticancer, antitubercular, insecticides, analeptics, analgesic, anti-bacterial, anti-viral, anti-fungal, and weedicidal activity. Researchers have tried various newer targets in search of better antimicrobials acting via novel mechanisms. Glucosamine-6-Phosphate synthase is an enzyme present in microbial cells. The inactivation of G-6-P synthase may serve as a novel approach to find better antimicrobials. The increasing demands development of newer and effective antimicrobial drugs has reported in search of newer techniques for the generation of new drugs. Hence, the molecular docking technique shall be explored to find or investigate the newer target finding the novel compounds which can be an active antimicrobial compound. The present review has focused on the reported heterocyclic compounds which have been evaluated for their antimicrobial potential using G-6-P synthase as a target. The results of in silico methods and in vitro methods have been compared and critically discussed.</jats:p> </jats:sec>

Preferential Synthesis and Pharmacological Evaluation of Mono‐ and Di‐substituted Benzimidazole Derivatives

“…Glucosamine-6-phosphate synthase is an enzyme present in nearly every microbial cells and inactivation of this enzyme is being researched as a novel therapeutic approach for designing newer antimicrobial drugs. [38,39] On the other hand, some anthelmintic drugs bind to ChemistrySelect the tubulin subunit of helminth's microtubules, thus disrupting their structure and function. Drug-tubulin interaction results in the loss of various vital functions of the helminth, such as mitosis, motility and transport, which is why it is an important target for predicting anthelmintic potential.…”

“…Table 7 summarizes the interaction of the synthesized compounds with glucosamine 6‐phosphate synthase (PDB: 1XFF) for predicting anti‐bacterial activity and tubulin (PDB: 1SA0) for predicting anthelmintic activity. Glucosamine‐6‐phosphate synthase is an enzyme present in nearly every microbial cells and inactivation of this enzyme is being researched as a novel therapeutic approach for designing newer antimicrobial drugs [38,39] . On the other hand, some anthelmintic drugs bind to the tubulin subunit of helminth's microtubules, thus disrupting their structure and function.…”

In Silico Studies of N-(Phenyl Substituted) 2-([Phenyl Substituted) Methylidene] Amino)-N,4- Diphenyl-6h-1,3-Oxazin-6-Amine Derivatives as Potential Antibacterial Agents

“…Glucosamine -6-phosphate synthase enzyme catalyzes the first step in hexosamine biosynthesis, converting D-fructose 6phosphate into D-glucosamine-6-phosphate (GlcN-6-P) using glutamine as the ammonia source and leading to the eventual formation of uridine-5-diphospho-N-acetyl-D-glucosamine, the important point of metabolic control in the biosynthesis of amino sugar containing macromolecules which is necessary for the cell wall assembly in bacteria and fungi 16,17 . Inhibition of this enzyme will restrain the cell membrane production and thereby significantly reduces the population of bacteria.…”

Regioselective synthesis of heterocyclic N-sulfonyl amidines from heteroaromatic thioamides and sulfonyl azides

“…The biological activity, rich chemistry and technically useful properties of heterocyclic compounds have made them a focal point of science and industry over the years. Heterocyclic compounds including azoles and azines have been found in natural products, and they are included in the structures of nucleic acids, vitamins, antibiotics and in many types of synthetic drugs [1][2][3][4][5][6][7][8][9][10][11][12]. N-Sulfonyl amidines have received considerable attention because they exhibit various types of pharmaceutical properties and biological activities [13][14][15][16][17][18][19][20][21] and also have been used as interesting building blocks in organic synthesis [17][18][19][20] (Figure 1).…”