Thesis On Coumarins

Thesis On Coumarins-59
Specifically, coumarin-3-sulfonamides and carboxamides were reported to exhibit selective cytotoxicity against mammalian cancer cell lines.

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Therefore, the condensation of pyrazolone with formaldehyde (60%) and various aromatic primary amines resulted in the formation the corresponding Mannich base derivatives.

Antiinflammatory activity was evaluated by carageenan induced paw oedema in albino rats.

The key intermediate was prepared by cyclization of compound with ethyl acetoacetate in presence of glacial acetic acid.

The key intermediate pyrazolone considered as a cyclic amide and hydrogen atom attached to C4 atom should be appreciably labile to participate in the Mannich condensation.

To expand the structural diversity of synthetic courmarins for biological functions, attempts have also been made to attach a chloramphenicol side chain at C-3 position of courmarin.

In addition, the bi- and tri-heterocyclic coumarins and 1-azacoumarins with benzofuran, furan and thiazole ring systems along with biocompatible fragments like vanillin have shown remarkable potency as anti-inflammatory agents in animal models.Some important coumarin members have been isolated from microbial sources e.g. 6 Pharmacological activities: Antimicrobial activity: Coumarin derivatives are having promising antimicrobial activities as per recent literature survey, details of which have been presented as given below: Rama Ganesh by agar cup diffusion method.DMF was used as blank, Streptomycin was used as anti-bacterial standard and Clotrimazole was used as anti-fungal standard drug at concentration of 1000μg/ml.All the synthesized compounds showed activity against both gram positive and gram negative bacteria but lesser activity compared to standard drug. 9 Patel et al synthesized some 4-aryl-2,6-di(coumarin-3-yl)pyridines by the reaction of 3-coumarinoyl methyl pyridinium salts with1-[2H-1-benzopyran-2-on-3-yl]-3-aryl-prop-2-ene-1-ones in the presence of ammonium acetate and acetic acid under the Krohnke reaction conditions (Fig. All the synthesized compounds were screened for antimicrobial activity.None of the compounds showed activity against either in the coumarin nucleus or in the phenyl ring did not affect the antibacterial activity much more and all the compounds have the same activity.Activity of other compounds indicated that the presence of an additional fused benzene ring between the C-5` and C-6` positions inhibited the antibacterial activity towards ) compared to in Potato Dextrose Broth medium (PDB).Appropriate volumes of tested compounds were added to produce concentrations ranging from 10 to 100μg/m L. 12) and (Fig.13) showed good activity as antifungals compared to the antifungal ability of fluconazole, which was used as a standard drugs. 12 FIG.13 4-Heteroaryl-coumarin-3-carbaldehydes Streptomycin was used as standard anti-bacterial drug and ketoconazole was used as standard anti-fungal drug. 17) had activity equal to that of standard drug ketoconazole (31.25 μg/m L) against ntiinflammatory and analgesic activity: Parmar V et al synthesized 4-methyl coumarin derivatives 7,8-dihydroxy-3-ethoxycarbonyl methyl -4-methylcoumarin (DHEMC) and 7,8-diacetoxy-3 - ethoxycarbonylmethyl - 4 - methylcoumarin (DAEMC) (Fig.Photobiological studies on pyridine-fused polycyclic coumarins have highlighted their potential as thymine dimer photosensitisers and the structurally related compounds of both coumarin and carbostyrils have also been found to act via the DNA gyrase pathway in their anti-bacterial activity.Apart from the above works, the present review focuses on the recent research done on coumarins, which basically incudes the synthesis of therapeutically useful coumarins alongwith the SAR, so as to give an overview of essential structural features required for therapeutic activities. They are found at high levels in some essential oils, particularly cinnamon bark oil (7,000 ppm), cassia leaf oil (up to 87,300 ppm) and lavender oil. bilberry, cloudberry), green tea and other foods such as chicory .The synthesized compounds were tested in a standard disk diffusion assay and displayed strong to moderate antimicrobial activity, with a promising new lead prototype compound (7-amino-9-hydroxy-5-oxa-7a,8,11-triazacyclopenta[]phenanthren-6-one (5)) possessing greater activity that the antibiotics Ampicillin and Nystatin.Antioxidant capacities of the compounds, determined spectrophotometrically using a phosphomolybdenum method, were greater, and in the case of compound 5 four times the activity of α-tocopherol acetate.


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