Abstract
The novel coumarin derivatives (2,3,4,5,6,7) have been synthesized from the reaction of o-acetyloxy benzoic acid with thionyl chloride yielding 2-acetoxy benzoyl chloride, which on further treatment with ethylacetoacetate gave 4-hydroxycoumarin. Substituted pyrazolones and thiazoles reacted with 4-hydroxy coumarin to give pyrazolones and methyl thiazoles related coumarin derivatives. The newly synthesized products were characterized with IR, 1H and 13C NMR, mass spectroscopic techniques and elemental analysis. The synthesized compounds were screened for their antibacterial and antifungal activity. All the compounds were found to have significant activity against the tested microorganisms. Keywords: Coumarin, thiazole, pyrazolone, antibacterial activity, antifungal activity.
Highlights
Coumarin derivatives are present in significant quantities and more than 1300 coumarins were identified from natural sources
The synthesis of coumarin and its derivatives have attracted considerable attention from organic and medicinal chemists for many years, as large numbers of natural products contain this heterocyclic nucleus.3. They are widely used as optical brighteners4 and dispersed fluorescent and laser dyes,5 additives in food,6 perfumes,7 cosmetics8 and pharmaceuticals9 so the synthesis of this heterocyclic nucleus is of much interest
The reaction of o-acetyloxy benzoic acid and thionyl chloride to give 2-acetoxy benzoyl chloride, which reacts with ethylacetoacetate to yield hydroxycoumarin
Summary
Coumarin derivatives are present in significant quantities and more than 1300 coumarins were identified from natural sources. ThIS family of compounds serve as an important model for the advanced design and synthesis of more active analogous coumarins, since natural compounds possess potent antioxidants and radical-scavenging properties as reportedin various experimental models. The synthesis of coumarin and its derivatives have attracted considerable attention from organic and medicinal chemists for many years, as large numbers of natural products contain this heterocyclic nucleus. They are widely used as optical brighteners and dispersed fluorescent and laser dyes, additives in food, perfumes, cosmetics and pharmaceuticals so the synthesis of this heterocyclic nucleus is of much interest. ThIS family of compounds serve as an important model for the advanced design and synthesis of more active analogous coumarins, since natural compounds possess potent antioxidants and radical-scavenging properties as reportedin various experimental models.. The synthesis of coumarin and its derivatives have attracted considerable attention from organic and medicinal chemists for many years, as large numbers of natural products contain this heterocyclic nucleus.. The synthesis of coumarin and its derivatives have attracted considerable attention from organic and medicinal chemists for many years, as large numbers of natural products contain this heterocyclic nucleus.3 They are widely used as optical brighteners and dispersed fluorescent and laser dyes, additives in food, perfumes, cosmetics and pharmaceuticals so the synthesis of this heterocyclic nucleus is of much interest. We report the design and synthesis of pyrazolone and methyl thiazole related coumarins derivatives with significant biological importance Warfarin and acenocomarol, which are coumarin derivatives, exhibit anticoagulant activity. Coumarin derivatives are used to synthesize fluorescent polymers and fluorescent chemosensors for Mg+2 ion. We report the design and synthesis of pyrazolone and methyl thiazole related coumarins derivatives with significant biological importance
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