Enzyme inhibition and antibacterial potential of 4-Hydroxycoumarin derivatives

Abstract

The 4-Hydroxycoumarin derivatives are known to show a broad spectrum of pharmacological applications. In this paper we are reporting the synthesis of a new series of 4-Hydroxycoumarin derivatives synthesized through Knovenegal condensation; they were characterized by using UV-Vis, FT-IR, NMR spectroscopies. The synthesized compounds were evaluated for antibacterial activity against Staphylococcus aureus and Salmonella typhimurium strains. The compounds (2), (3) and (8) showed favorable antibacterial activity with zone of inhibitions 26.5± 0.84, 26.0 ± 0.56 and 26.0 ± 0.26 against Staphylococcus aureus (Gram-positive) respectively. However, the compounds (5) and (9) were found more active with 19.5 ± 0.59 and 19.5 ± 0.32 zone of inhibitions against Salmonella typhimurium (Gram-negative). Whereas, in urease inhibition assay, none of the synthesized derivatives showed significant anti-urease activity; although, in carbonic anhydrase-II inhibition assay, the compound (2) and (6) showed enzyme inhibition activity with IC 50 values 263±0.3 and 456±0.1, respectively.

Testing for the ability to modify antibiotics of Panus tigrinus 8/18 Lentinus strigosus 1566 laccase

“…Usage of enzymes to produce new compounds or modify antibacterial compounds is important (Zengin et al, 2018;Saleem et al, 2020;Zhao et al, 2020;Tukenova et al, 2021). Fungal laccases are an inexpensive and readily accessible enzyme for earning reaction components.…”

Extending the Library of 4‐Hydroxycoumarin Derivatives with Potential Pharmacological Activity by a Catalyst‐Free and Purification‐Free Method

“…Although multiple sites can be targeted to functionalize 4‐hydroxycoumarin, position 3‐substituted derivatives are subject of interest for pharmacological use [14–16] . The nucleophilic carbon in position 3 leads to the creation of a new carbon‐carbon bond, which is one of the main pillars of organic synthesis.…”

“…Although multiple sites can be targeted to functionalize 4hydroxycoumarin, position 3-substituted derivatives are subject of interest for pharmacological use. [14][15][16] The nucleophilic carbon in position 3 leads to the creation of a new carboncarbon bond, which is one of the main pillars of organic synthesis. Several synthetic techniques are employed to make a new carbon-carbon bond, however, the multicomponent reactions such as Mannich reaction is considered one of the most important high-atom economic carbon-carbon bond forming strategy to produce β-amino carbonyl compounds referred to as the Mannich base.…”