Thia-Michael addition of 2-[(4-hydroxy-3,5-dimethoxyphenyl)methylidene]hydrazine-1-carbothioamide (1) with maleic anhydride results in the formation of the title compound 2-{[(4-hydroxy-3,5-dimethoxyphenyl)methylidene]hydrazinylidene}-4-oxo-1,3-thiazolidin-5-yl acetic acid 2. The precursor 1 is synthesized by the reaction of 4-hydroxy-3,5-dimethoxybenzaldehyde and thiosemicarbazide in the presence of glacial acetic acid as the catalyst. The structure of the title compound is determined by elemental analysis, FT-IR, 1H-NMR, 13C-NMR and mass spectral data. In order to determine the molecular interactions with the bacterial enzyme, the title compound is further docked into the active site of the MurB protein of Staphylococcus aureus (PDB ID: 1HSK). The in vitro antibacterial and antifungal activity of the title compound is carried out in order to appraise its antimicrobial efficacy by determination of zone of inhibition and minimal inhibitory concentration. The compound is also evaluated for its antioxidant property by 2,2-diphenyl-1-picryl-hydrazyl (DPPH) radical scavenging assay.
A study has been conducted to assess the role of vermicomposting and carrying out plant nutrients analysis of composts delivered from food waste at Mangalagangothri campus, Dakshina Kannada District, Karnataka-India. Wastes were collected and subjected to pit- and vermi-composting using an exotic species of earthworm (Eudriluseugeniae). The composts were harvested and analyzed for macro-nutrients (N, P, K, Mg, Ca, S) by employing the standard methods. The Bioassay was conducted using PisumsativumL. plant and the data wereanalyzed statistically using SPSS. 20.Results revealed that there was highly reduction in the volume of the wastes equivalent to 30% and 20% for vermi- and pit-composting respectively. The macro-nutrients analysis showed that vermicompost had more nutrientsthan pit-compost. Based on bioassay test, the vermicompost had the potential for improving plant growth and yield compared to pit-compost and garden soil (control). Thus, vermicompost was found to be cost-effective methods, helps in reducing food waste disposals and supplied soil with a lot of macro-nutrients compared to that of the pit-compost based on results of bioassay and nutritional parameters. Keywords:Bioassay; Eudriluseugeniae; Food waste, Pisumsativum, Vermicompost.
Background: Development of potential antimicrobial agents is a main aim in the drug discovery process to overcome the drug resistant problems. Pyrazolines and thiazolinones are extensively used as building blocks for the synthesis of diverse medicinally important compounds. Method: In this present work, a new series of functionalized pyrazolinyl-thiazolinone biheterocycles is designed and synthesized from N-pyrazolinecarbothioamide. Antimicrobial screening is carried out in order to discover their potential towards six bacterial and four fungal strains. The zone of inhibition (ZI in mm) was determined by disc diffusion method and minimum inhibitory concentration (MIC in μg/mL) by macro dilution method. The druggability of these new entities is done through in silico pharmacokinetic profiling using Maestro 2017-1 interface of Schrӧdinger software. Result: The compounds 4c and 4e with chloro and iodo substituents on N-phenylacetamide ring displayed good inhibitory antibacterial activity against tested bacterial strains with minimum MIC values when compared to the reference drug tetracycline. The compound 3 with an acetic acid derivative showed high antifungal activity among all the tested derivatives. The compound 3 not only showed antifungal activity but also qualified druggability test with no violation of Lipinski rule of five. Conclusion: The capability of the synthesized pyrazolinyl-thiazolinone derivatives was performed to efficiently inhibit the growth of microorganisms against selected bacterial and fungal strains. Further, these compounds are found to be effectively bound to the active sites of attractive target Escherichia coli FabH.
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