Synthesis of Coumarin Derivatives with Cytotoxic, Antibacterial and Antifungal Activity

Abstract

The synthesis and selective biological screening of 7-hydroxy-4-methyl-2H-chromen-2-one (2), 7-hydroxy-4,5-dimethyl-2H-chromen-2-one (15) and some of their derivatives were carried out. Compound 13 was found to be most potent cytotoxic agent with LD50 = 126.69 microg/ml. In antibacterial assay the compounds showed a broad spectrum of activities. Compound 11 exhibited a very high degree of plant growth inhibition at three levels of concentration. Compound 4 showed very promising antifungal activity against Candida albicans. Compounds 12 and 13 demonstrated excellent antioxidant activity.

In vitro inhibition of cytosolic carbonic anhydrases I and II by some new dihydroxycoumarin compounds

“…There have also been very interesting studies of the synthesis and selective biological properties of 7-hydroxy-4-methyl-2H-chromen-2-one (2), 7-hydroxy-4,5-dimethyl-2H-chromen-2-one (15) and some of their derivatives [10]. These stimulated us to synthesize a number of new dihydroxy coumarin compounds for testing against hCA-I and -II isozymes.…”

“…A wide spectrum of pharmacological activities are displayed by coumarins and their derivatives [10,11]. Coumarin derivatives are used widely as anticoagulants (such as warfarin, -OH group is attached at 4-position) for the treatment of disorders in which there is excessive or undesirable clotting, such as thrombophlebitis, pulmonary embolism, and certain cardiac conditions.…”

Microwave-Assisted Synthesis of Bioactive Six-Membered Heterocycles and Their Fused Analogues

“…Benzopyrones are an important class of oxygenated heterocycles, widely distributed in plants, including edible vegetables and fruits [79] and many of them have broad and interesting ranges of biological activities [80][81][82][83]. The two more important benzopyrone derivatives are the chromones and coumarins.…”

Synthesis and Characterization of Some Novel Coumarin Based 2-Pyridone Heterocycles with their Broad Spectrum Antimicrobial Potency

“…It is well known that coumarin derivatives possess a wide range of medicinal indications, such as anthelmintic, anticoagulant, hypnotic and insecticidal properties [2]. The antimicrobial activity of coumarin derivatives is reported in the literature [3,4,5,6,7]. Potential of various natural and synthetic coumarin derivatives proved its importance as anti-inflammatory [8] antioxidant properties [9] anticancer [10,11] and monoamine oxidase inhibitors [12].…”