Pharmacological report of recently designed multifunctional coumarin and coumarin–heterocycle derivatives

Abstract

Coumarin is a naturally available molecule and has been identified as a potent pharmacophore due to its pharmacological activity. Because of this, coumarin has been exploited synthetically to prepare a wide range of derivatives. In fact, most coumarin derivatives have been found to be less toxic, which is the most essential property for a drug molecule. Such molecules are being prepared for therapeutic use as broad‐spectrum pharmacological agents. Microbial diseases including viral diseases have become very common and are responsible for many deaths worldwide. In particular, microbial drug resistance is a problem that needs to be tackled in an effective manner. Also, for Alzheimer's disease, which affects most elderly persons, no efficient chemotherapy exists. In addition, although diabetes, a metabolic syndrome, can be treated with many drugs, there is no complete cure. Thus, more potent antidiabetic agents are required for the management of diabetes. Likewise, for the treatment of a wide range of ailments caused by microbes, genetic factors, or lifestyle‐related factors, an efficient drug regimen is needed. In view of this, coumarin derivatives are designed and evaluated. Here, coumarin derivatives that have been reported recently are compiled, classified and evaluated critically. This study briefly takes the structure–activity relationship into consideration and suggests the next suitable step. With a focus on the most potent molecules, the pharmacological activity of the evaluated molecules is described.

Cytogenotoxicity assessment of 3‐(3,4‐dihydroxyphenyl)‐7,8‐dihydroxycoumarin on HepG2/C3A cells and leukocytes

“…Coumarins are produced by plants as secondary metabolites. These compounds occur in low concentrations, and many of them proved to have pharmacological effects (Dorababu, 2022; Hussain et al, 2012; Leitzmann, 2016; Xia et al, 2022). Coumarins are found mainly in fruits and flowers, and also in other sources, as olive oil, coffee, wine, black or green tea, citrus fruits, cinnamon, and essential oils such as cinnamon bark and lavender oils (Heghes et al, 2022; Matos et al, 2015).…”

Computational Drug Designing, Synthesis, Characterization and Anti-bacterial Activity Evaluation of Some Mixed Ligand–Metal Complexes of 2-hydroxybenzaldehydethiosemicarbazone as Primary Ligand

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Fig. 6 RMSD (root mean deviation square) plot of Asp kinase complex bound with ligand [Cu(L)(im) 2 (SO 4 )]

The radius of gyration (Rg) reflects the compactness, folding, and stability of the complex [ 79 ] as well as the mass-weighted root mean square distance of the atoms from the centre of mass. The Rg plot displays the folding, compactness, and target structure fitness during the 20 ns simulation time (Fig.…”

Coumarins Synthesis and Transformation via C–H Bond Activation—A Review

“…The wide and diverse area of application for coumarins in medical sciences, biomedical research, and in many industries, including perfumery, is impressive. The pharmacological profile of these phytochemicals includes antibacterial (agasyllin, felamidin, and armillarisin A) [8,9], anti-inflammatory (coumarin and esculetin) [10], anticancer [11][12][13][14], antiviral [15,16], antioxidant (Esculetin) [17][18][19][20], antifungal [21], anticoagulant (warfarin) [22,23], anti-HIV (inophyllums and calanolides) [24][25][26], and other activities [27]. Coumarins also act as selective enzyme inhibitors; they are able to interact with targets in the treatment of diseases such as Parkinson's and Alzheimer's [28,29] and, more recently, they have been widely adopted in the design of small-molecule fluorescent chemosensors [30].…”