Posted by admin on Nov 30, 2018 in |
In the field of the preparation of chemotherapeutic agents with new mechanism distinct from currently approved drugs is important. However, the clinically effective approved small inhibitor molecule is still lacking. Previous reports indicated that 4-aryl-2-hydrazinothiazole derivatives provided a useful start point to develop HAT inhibitors (histone acetyltransferase). Consequently, preparation and biological evaluation of a focused library of 4-aryl-2-hydrazinothiazole based derivatives as useful as anti-cancer agents. Synthesis of 4-aryl-2-hydrazinothiazoles (1a-d), (2a-d), (3a-c), (4a-b), (5a-b), (6a-b) studied by either conventional method and free solvent microwave one-pot method, and the synthesized compounds were proved by spectroscopic methods (IR, 1HNMR, 13CNMR, GC-Ms, and elemental analysis). The activity against different cancer cell lines and the antimicrobial activities different organisms also studied, and all of the synthesized compounds were of high activity as an antibacterial for gram positive and gram negative; however, it showed also an antifungal activity were the most active compounds were 4a, 4b, 5b, 6a. It was found that all of the prepared thiazoles derivatives were active toward many cell lines (breast,...
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Posted by admin on Nov 30, 2018 in |
Quinolones are the organic compounds that act against the DNA-gyrase enzyme, a type II topoisomerase. Norfloxacin is one such quinolone which is characterized by a piperazinemoiety at C-7 position. This moiety plays a significant role in determining the antibacterial spectrum and potency and serves as a site amenable to significant modification. N-Mannich bases have proved to be potential prodrug candidates for amides, urea derivatives, imides and amines. It has proved to be a versatile base in current applications of organic chemistry. Mannich bases with N-4 substituted piperazine containing moieties were biologically active. We designed and synthesized new series of Mannich bases of Norfloxacin by conventional as well as microwave method by reacting them with isatin and various aromatic aldehydes. Their chemical structures have been confirmed by IR, 1H NMR and 13C NMR spectroscopy and evaluated for antibacterial activity by Agar well diffusion method. Antimicrobial evaluation was done against gram positive bacteria B. subtilis and gram negative bacteria E. coli. Among the compounds tested, 7a (i) and 7b (i) showed...
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Posted by admin on Oct 31, 2018 in |
Encapsulation of thymol is important for its volatile nature, taste, and antispasmodic, antioxidant, antimicrobial, anticancer and anti-inflammatory properties. This review provides a summary of thymol encapsulation in different biodegradable polymers along with the methods of encapsulation and control release in various parts of the body. Biodegradability of shell material along with its health compatibility and the half life of the core material and knowledge of microstructure are some of the main issues that must be addressed while studying encapsulation of Pharmaceutically Active Ingredients (PAI). Different biodegradable polymers used for the encapsulation of thymol are xanthum gum, poly vinyl alcohol (PVA), gelatine, starch, sodium alginate and ethyl cellulose. Preparative conditions, such as concentration ratios, temperature, stirring speed, and nature of solvent used, have deterministic effect on the polymer shell formed around the core material. Purposes for encapsulation of PAI may be numerous, such as controlled release, targeted controlled release, protection/preservation, economic utilization, convenient packaging, and clever option for storage, easy portability and formulation, modification/ hiding undesirable property such as taste,...
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Posted by admin on Oct 31, 2018 in |
Plants are an important source of substances which are claimed to induce biological activities. Although there are a few studies on antimicrobial and antioxidant activities of this plant, antimutagenic activity has not been studied and there is no study in Turkey. Antibacterial activities of Syzygium aromaticum against oral pathogens have not been reported until today. The scope of this work was to investigate the biological activities of S. aromaticum different extracts. The various extracts were screened for antibacterial activity. The bacteria were isolated from oral flora by traditional methods. The plant extracts were tested by Kirby-Bauer method. Other antibacterial activities tests are MIC (minimum inhibitory concentration) and MBC (minimum bactericidal concentration). In addition to, the antioxidant activities of plant extracts were screened by the stable DPPH (2, 2-diphenyl- 1-picrylhydrazyl hydrate) free-radical. The antimutagenicity of the plant extracts were determined by Ames test using Salmonella typimurium strains. The highest antibacterial activity was determined as 20 mm inhibition zone from methanol extracts. The highest DPPH scavenging activity was found as 82%...
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Posted by admin on Oct 31, 2018 in |
Investigation of antioxidant, anti-inflammatory and antimicrobial activity of a dental film, which easily reabsorbs with applied phytocomplex of Geranium palustre, has been performed to use it for the treatment of oral mucosa diseases. To get the extract, the dried material was grounded, extracted and lyophilized. Quantitative determination of biologically active substances in lyophilized phytocomplex was performed on spectrophotometer and high performance liquid chromatograph. For investigation of antioxidant properties of the extract, the method, based on the interaction with stable chromogen-radical DPPH, was used. Investigation of anti-inflammatory activity of a dental film with extract of Geranium palustre herb was carried out based on carrageenin model of inflammatory. The study of antimicrobial properties of extract was performed using laboratory strains of microorganisms as a test-culture. The obtained qualitative indices of biologically active substances of the investigated phytocomplex showed high content of tannins, polyphenol compounds, polysaccharides, phenolcarboxylic acids, organic acids, ascorbic acid, free amino acids and other compounds, due to which lyophilized extract possesses a wide range of properties, important for treatment:...
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