Posted by admin on Jun 30, 2017 in |
Acid amine coupling of 1H-indol-6-yl(piperazin-1-yl) methanone with different acids has been synthesized in presence of HATU reagent, DIPEA base with DMF solvent at 45 °C 30 mins to yield Indole piperzine derivatives 3a-j. The structures of all the synthesized compounds have been characterised by elemental analysis and spectral studies like 1H-NMR and LCMS. Some selected Indole piperazine derivatives have been tested for antimicrobial activity using by Disc diffusion method and in vitro antioxidant activity using DPPH Assay method. Three compounds 3a, 3f and 3h have shown significant antimicrobial and one compound 3b have shown in vitro antioxidant...
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Posted by admin on May 31, 2017 in |
Flavanoids are plant secondary metabolites, synthesized by microwave assisted synthesis and green chemistry approach since, the conventional method of synthesis uses various organic solvents, hazardous by product, tedious work that requires more reaction time. Flavonoids have general structure of 15-carbon skeleton which consists of two phenyl ring (A and B) and heterocyclic pyran ring(C). Flavones are one of the important class of flavanoids acquires a broad spectrum of activity. Chalcone (1, 3-diaryl-2-propen-1-ones), is a privileged structure, demonstrating promising anti-microbial, anti-inflammatory and anticancer activities. The basic moiety of flavanoids gives numerous biological activities henceforth; flavanoid and chalcone derivatives were synthesized and confirmed by physiochemical and spectral data. Biological screening was done for antibacterial especially for anti-methicillin resistant Staphylococcus aureus and antifungal screening with using standard drug Ofloxacin and Griseofulvin respectively. Compound NKP-3, NKP-4, NKP-8a, NKP- 9a and NKP-10a are more active and other compounds are less active against bacteria and...
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Posted by admin on May 31, 2017 in |
The present investigation evaluates preliminary phytochemical screening and antimicrobial activity of aerial parts of Alternanthera bettzickiana (Regel) G. nicholson an edible green medicinal herb tested against various Gram positive, Gram negative bacteria and fungi. The plants were evaluated against two Gram positive bacterial species such as Staphylococcus aureus and Enterococcus faecalis; two Gram negative bacterial species such as Escherichia coli and Klebsiella pneumoniae; and fungi such as Aspergillus niger, Epidermophyton floccosum and Candida albicans were tested. Preliminary phytochemical screening was performed with ethanol, petroleum ether, acetone, chloroform and aqueous extracts of Alternanthera bettzickiana (Regel) G. nicholson that showed the alkaloids, carbohydrates, saponins, phenols, flavonoids, diterpenes, tannin, terpenoids, steroid, oxalate, anthocyanin, leucoanthocyanin, Xanthoprotein, coumarin and glycosides in the ethanol extract. The ethanol extract showed higher phytoconstituents when compared to the other extracts. The extracts were compared with standards like Amoxicillin and Ketoconazole for antibacterial and antifungal activity respectively. The extracts showed greatest antimicrobial activity as measured from the zone of inhibition and results were comparable with that of standard drugs...
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Posted by admin on Apr 30, 2017 in |
In this study, a novel series of heterocyclic compounds containing pyrazolidine-3, 5-dione nucleus has been synthesized. The compounds were synthesized in four steps; esterification of 2-mercaptobenzoic acid in an acidic medium to yield 2-mercapto-benzoic acid ethyl ester which was cyclized using ethyl acetoacetate to form 2-methyl-4-oxo-4H-thiochromene-8-carboxylic acid ethyl ester. These were reacted phenyl hydrazine derivatives to give corresponding thiochromene derivatives, which were cyclized using diethylmalonate to obtain pyrazolidine-3, 5-dione derivatives. All the synthesized compounds were characterized by spectral (IR, NMR and MS) and elemental analysis. The compounds were screened for their antibacterial activity against Gram-positive bacteria (B. subtilis, S. epidermidis, M. luteus, S. aureus, B. pumilis, and B. cereus), Gram-negative bacteria (K. pneumonia, E. coli, and P. aeroginosa) and for antifungal activity against (A. niger, C. albicans and F. solani) by agar-diffusion method. The minimum inhibitory concentrations (MICs) of these compounds were also determined by tube dilution method. The antimicrobial effectiveness of all the compounds was found to be concentration dependent. Two compounds- 1-(3-chlorophenyl)-2-(2-methyl-4-oxo-4H-thiochromene-8- carbonyl) pyrazolidine-3, 5-dione (5a) and...
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Posted by admin on Apr 30, 2017 in |
Acinetobacter baumanniiis typically coccobacillus Gram-Negative bacterium, resists almost all antibiotics in use. Synthetic antimicrobial peptides (AMPs) against this bacterium were designed with the aid of computational software and databases to be with the accepted models. Antimicrobial peptides (AMPs) might be the candidate solution for the this problems. Four peptides designated MY1, MY2, MY3 and MY4 were synthesized with length 11-14 amino acids, they were rich in Arginine and Tryptophan. The MICs of the peptides against colistin sensitive A. baumannii were 2.4, 6.2, 6.9, 6.6 µg/ml (mean for 10 strains) respectively vs Mastoparan as control was 10.4 µg/ml, whereas the MICs of peptides against colistin resistant A. baumannii were 3.8, 6.2, 6.8, 6.4 µg/ml (mean for 10 strains) respectively vs Mastoparan 13.6 µg/ml. The designed peptides showed no hemolytic activity at effective MICs. The practical calculated Therapeutic Index were 141.7, 67.7, 60.9, 77.3 vs 7.7 for Mastoparan (Colistin sensitive strains) and for resistant strains were 89.5, 67.7, 61.8, 79.7 vs Mastoparan...
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