2H/4H-Chromenes—A Versatile Biologically Attractive Scaffold

Abstract

2H/4H-chromene (2H/4H-ch) is an important class of heterocyclic compounds with versatile biological profiles, a simple structure, and mild adverse effects. Researchers discovered several routes for the synthesis of a variety of 2H/4H-ch analogs that exhibited unusual activities by multiple mechanisms. The direct assessment of activities with the parent 2H/4H-ch derivative enables an orderly analysis of the structure-activity relationship (SAR) among the series. Additionally, 2H/4H-ch have numerous exciting biological activities, such as anticancer, anticonvulsant, antimicrobial, anticholinesterase, antituberculosis, and antidiabetic activities. This review is consequently an endeavor to highlight the diverse synthetic strategies, synthetic mechanism, various biological profiles, and SARs regarding the bioactive heterocycle, 2H/4H-ch. The presented scaffold work compiled in this article will be helpful to the scientific community for designing and developing potent leads of 2H/4H-ch analogs for their promising biological activities.

Search for Antimicrobial Activity Among Fifty-Two Natural and Synthetic Compounds Identifies Anthraquinone and Polyacetylene Classes That Inhibit Mycobacterium tuberculosis

“…This compound, prepared for a previous study, demonstrated anti-parasitic action against both T. cruzi and L. amazonensis ( Martin et al, 2018 ). Chromene derivatives bearing trisubstituted amines were previously reported as antimycobacterial against M. tuberculosis H37Rv ( Raj and Lee, 2020 ). C10, the most active compound among the pyranocoumarin derivatives, differs from the others with the substituent group on the aryl moiety and the ester function on the pyran ring.…”

Chromanone-A Prerogative Therapeutic Scaffold: An Overview

“…Generally, cancer can be measured by assessing the degree of mitochondrial impairment and metabolic dysfunctions such as cellular energy supply, cell death signaling, irregulation of metabolic pathways, formation of reactive oxygen species (ROS), compromised enzyme actions, aerobic glycolysis augmented in tumor cells, alterations in lipid metabolism and unbalanced pH [ 6 ]. Therefore, to cure such metabolic dysfunctions, naturally occurring flavonoids, flavonols, flavanones (2-phenyl chroman-4-one derivatives) and homoisoflavanones exhibit good anticancer potential along with other pharmacological activities such as anti-inflammatory, antioxidative, antidiabetic, antibacterial, antimicrobial, antifungal, antimutagenic, antiparasitic and anti-HIV [ 7 , 8 ]. In this regard, the following naturally occurring flavanones such as naringenin [ 9 ], naringin [ 9 ], sakuranetin [ 10 ], eriodictyol [ 11 ], calyxin G, deguelin [ 12 ] and sterubin [ 13 ] have been reported (Figs.…”

New Insights Into the Promising Antibacterial Activity of Thiophene or Chromene Moiety Containing Aryl Sulfonamide

“…Chromene moieties play a signi cant role with structural aryl sulfonamide scaffold which can be easily transformed into functionalized diverse biologically active molecules. 124 Naturally occurring 125 and synthetic chromene compounds possess antibacterial properties. 126 A number of pathways are available for their synthesis, but there is a signi cant need for approaches that include chromenes from precursors that are readily available.…”