Barringtonia acutangula (L.) Gaertn belonging to family Barringtoniaceae was investigated to evaluate In vitro antibacterial activity of aqueous, ethanolic, petroleum ether and chloroform extracts against Staphylococcus aureus, Pseudomonas aeruginosa, Klebsiella pneumoniae, Enterococcus faecalis and Escherichia coli the major urinary tract infection causing pathogens were tested by disc diffusion assay method and the minimum inhibitory concentration was evaluated. Ethanol (95%) extract exhibited broader spectrum of inhibition followed by chloroform, petroleum ether and aqueous extracts against the urinary tract pathogens under test. An attempt has been made to compare the activity of extracts with standard antibiotics against selected urinary tract infection causing pathogens.

Antibacterial activity of Barringtonia acutangula against selected urinary tract pathogens

The hydroalcoholic extracts prepared from leaves of Rungia pectinata and Rungia repens were investigated for antiinflammatory and diuretic activity in wistar rats. The results obtained were compared with that of standard drug aspirin and frusemide for their antiinflammatory and diuretic activity respectively. The acute toxicity study was also carried out using adult swiss albino mice of either sex which indicates the safety of the extracts even at a dose of 4000 mg/kg. R. pectinata showed better anti-inflammatory activity than R. repens. In the present study, it was demonstrated that hydroalcoholic extracts of both R. repens and R. pectinata produce diuretic effect by increasing the excretion of Na(+), K(+) and Cl(-). Results showed that R. repens is most effective in increasing urinary electrolyte concentration of Na(+) and K(+) ions. The antimicrobial potency of the aerial parts of Rungia pectinata and Rungia repens have been studied using the petroleum ether, benzene, chloroform, acetone and ethanol extract against a wide number of bacteria and fungi by disc diffusion method. The ethanol extract at a concentration of 30 to 60 μg/disc showed significant activity against the bacteria and fungus investigated. All the extracts of R. pectinata and R. repens have got moderate action but chloroform and acetone extracts of R. repens and ethanol extract of R. pectinata have got significant activity against Trichophyton mentagrophytes.

/pdf/antiinflammatory-diuretic-and-antimicrobial-activities-of-1whw6yt37z.pdf

Antiinflammatory, diuretic and antimicrobial activities of Rungia pectinata linn. and Rungia repens nees

Anti-Inflammatory Effects of Coumarin–Selenophene Derivatives on LPS-Stimulated RAW 264.7 Macrophage Cells

Coumarins (2H-chromen-2-ones), also known as benzopyran-2-ones, are a family of naturally occurring heterocyclic ring systems that contain a lactone moiety. Coumarins exhibit a wide range of well-s...

Medicinal applications of coumarins bearing azetidinone and thiazolidinone moieties.

Background Piperine or piperic acid was isolated from fruits of Piper nigrum and had been reported as pharmacological valuable bioactive constituents. Keeping in view, a series of piperic acid-based N heterocyclic's derivatives were synthesized and evaluated for antibacterial activity. All these prepared ligands were docked to study the molecular interactions and binding affinities against the protein PDB ID: 5 CDP. Objective To meet the real need of newer antibacterials, we designed and synthesized scaffolds with good antibacterial activity. The obtained antibacterials have been validated in terms of ligand-protein interaction and thus prove to build up as good drug candidates. Methods Antibacterial activity of the compounds were carried out against bacterial strains; three Grampositive and three Gram-negative bacterial strains using agar well diffusion method. In silico molecular docking studies were carried out using Glide (grid-based ligand docking) program incorporated in the Schrodinger molecular modeling package by Maestro 11.0. Results Compounds BC 28, BC 32, and BC 33 exhibits antibacterial activity along with Glide docking score of -8.580, -9.753 kcal/mol, and -8.813 kcal/mol, respectively. Docking studies explained hydrogen bonding, pi-pi, and hydrophobic interactions with amino acid residues which explain the binding affinity of the most docked ligand with protein. Conclusion In the present study, substituted piperic acid was synthesized and evaluated as antibacterial compared with standard drug ciprofloxacin and results interpret that having nitrogen as heteroatom in the heterocyclic nucleus found to be more potent than the standard drug ciprofloxacin. On comparing, substitution with electron-donating groups generates excellent antibacterial potential against the bacterial strains. It was also proved that having substitution with electron-donating groups on meta and para position with triazoline ring system exhibits greater potential while compounds which have a meta- electron-donating substituent showed lesser activity with thiazole nucleus. In addition, structure-based activities of the prepared analogs were discussed under Structure-Activity Relationship (SAR) section.

Synthesis and In Silico Molecular Docking Studies on Substituted Piperic Acid Derivatives as Inhibitors of Bacterial DNA Gyrase.

Keeping in view the pharmacological potential of azetidinones, thiazolidinones and coumarins, the title compounds containing these nuclei were synthesized. The 4-methyl -7-hydroxy coumarin (1) on treatment with hydrazine hydrate affords 2-hydrazo- 4-methyl -7-hydroxy coumarin (2). The N- (2’-imino-4’-methyl-7’-hydroxy coummarinyl)-imino substituted benzene (3) was synthesized by reaction of compound 2 with various aromatic aldehydes. Condensation of compound 3 with chloroacetyl chloride in presence of 1,4-dioxan and triethyl amine yields the 3-chloro-4- (substituted)-1-(2’-imino-4’-methyl-7’-hydroxy coumarinyl) azetidin-2-one (4a-d). Further more condensation of 3 with thioglycollic acid in presence of 1,4-dioxan and anhydrous aluminium chloride gives 2-(substituted phenyl)-3-(2’-imino-4’-methyl-7’-hydroxy coumarinyl)-1,3-thiazolidinone (4’a-d). Elemental and spectral characterization established the identity of these compounds. All the products were screened in vitro for their anti microbial activity against different strains of urinary tract pathogens. All compounds exhibited significant antimicrobial activity compared to the standard drug nitrofurantoin.

 Key words: Azetidinones, thiazolidinone, coumarin, nitrofurantoin, E. coli, P. auregenosa, K. pneumoniae, P. mirabilis E. faecalis , and S.aureus .

Dhaka Univ. J. Pharm. Sci. Vol.4(2) 2005

The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

Synthesis and Biological Activity Evaluation of Some Azetidinone and Thiazolidinone Derivatives of Coumarins

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Synthesis and Biological Activity Evaluation of Some Azetidinone and Thiazolidinone Derivatives of Coumarins