• Archives of Pharmacal Research
• /
• 제12권2호
• /
• pp.119-124
• /
• 1989

Cotton xanthate, which was obtained by treating cotton with carbon disulfide in alkaline solution, was treated with the solution of polyvalent metal ions to produce cotton xanthate-metal chelates. This chelation reaction was readily and simply achieved, and antimicrobial agents with suitable structures could subsequently be coupled to the chelate with ease at moderate pH values and in aqueous solution. Metal ions used in present work include Cu(II), Zn(II) and Fe(III). Tetracycline, streptomycin, neomycin and pyrithion were used as antimicrobial/antifungal agents. Antibacterial activities were measured employing ditch plate method against G(+) Staphylococcus aureus, Streptococus faecalis, and G(-) Escherichia coli, Enterobacter aerogenes, and the fungus, Aspergillus niger. All the cotton xanthate-metal-antimicrobial agent chelates exhibited activities whereas the cotton xanthate-metal chelates themselves were inactive. Considering the extensive washing procedures and results from control experiments, possibility of the involvement of physical adsorption for the binding of drugs could be excluded.

• Genomics & Informatics
• /
• 제6권4호
• /
• pp.227-230
• /
• 2008

Compounds of polyketide origin possess a wealth of pharmacological effects, including antibacterial, antifungal, antiparasitic, anticancer and immunosuppressive activities. Many of these compounds and their semisynthetic derivatives are used today in the clinic. Most of the gene clusters encoding commercially important drugs have also been cloned and sequenced and their biosynthetic mechanisms studied in great detail. The area of biosynthetic engineering of the enzymes involved in polyketide biosynthesis has recently advanced and been transferred into the industrial arena. In this work, we introduce a computational system to provide the user with a wealth of information that can be utilized for biosynthetic engineering of enzymes involved in post-PKS tailoring steps. Post-PKS tailoring steps are necessary to add functional groups essential for the biological activity and are therefore important in polyketide biosynthesis.

• Mycobiology
• /
• 제31권2호
• /
• pp.99-104
• /
• 2003

Bee propolis ethanolic extract with some plant essential oils was investigated for its antidermatophytic properties. The tested plant essential oils included jasmine, clove, lemon, Arabian jasmine, mint, rosa, olive and basil. The antidermatophytic activity has been compared to Naftifine-HCl and Clotrimazole used for dermatophyte treatment. Experimental model has been tested using sheep hoof plate for the in vitro tests to stimulate human nails. Mint, clove and basil with 4 mg/ml of bee propolis have a comparable efficacy to those of Naftifine-HCl and Clotrimazole. There is a great necessity for new effective low price and safe antidermatophyte agents to avoid recurrent infection. Propolis synergistic could be of great importance with essential oils of plants in dermatophyte therapy.

• Bulletin of the Korean Chemical Society
• /
• 제32권5호
• /
• pp.1511-1518
• /
• 2011

A series of 1,4-disubstituted octahydroquinoxaline-2,3-dione derivatives was prepared through two steps reaction. The latter involves the formation of N,N-disubstituted cyclohexane-1,2-diamine derivatives (la-j) through reductive alkylation of 1,2-cyclohexanediamine with different aldehydes in presence of sodium cyanoborohydride. Fusion of compounds (1a-j) with diethyl oxalate affording the target compounds (2a-j). Elucidation of structures of compounds (2a-j) was based upon different spectral data as well as the elemental methods of analyses. In addition, mass spectrometry and X-ray diffraction analyses were carried out. Moreover, the lipophilicity of the target compounds as expressed from the Clog P. Most of the test compounds (2a-j) showed weak to moderate antibacterial and antifungal activities against most of the used bacterial and fungal strains in comparison to chloramphenicol and clotrimazole as reference drugs respectively.

• Bulletin of the Korean Chemical Society
• /
• 제32권11호
• /
• pp.3996-4000
• /
• 2011

In an attempt to find a new class of anti microbial agents, a series of thiazolidinone and their 5-arylidene derivatives containing 4-(4-methyl benzamido)-benzoyl moiety were synthesized via the reaction of benzocaine with appropriate chemical reagents. These compounds were screened for their antibacterial activity against Gram-positive bacteria (Bacillus subtilis and Bacillus thuringiensis), Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa) and antifungal activity against Botrytis fabae, Fusarium oxysporan and Candida albicans. On the other hand the synthesized compounds were also screened for their anti tubercular activity. IR, $^1H$ NMR, $^{13}C$ NMR and MS spectral analyses established the structures of the newly synthesized compounds. The results revealed that some of these compounds have shown promising antimicrobial and anti tubercular activity in comparison with standard drugs.

• Pediatric Infection and Vaccine
• /
• 제18권1호
• /
• pp.15-22
• /
• 2011

Invasive Candida infections (ICI) have become the third most common cause of late-onset infection among premature infants in the neonatal intensive care unit (NICU). Risk factors include birth weight less than 1,000 g, exposure to more than two antimicrobials, third generation cephalosporin exposure, parenteral nutrition including lipid emulsion, central venous catheter, and abdominal surgery. Candida colonization of the skin and gastrointestinal tract is an important first step in the pathogenesis of invasive disease. Strict infection control measures against the infection should be done in the NICU. The following practices are likely to contribute to reducing the rate of ICI: (1) restriction of broad-spectrum antibiotics, antacids and steroid; (2) introduction of early feeding and promoting breast milk. Fluconazole prophylaxis may be an effective control measure to prevent Candida colonization and infections in individual units with high incidence of fungal infection. In addition, there is a need of further data including the development of resistant strains and the effect on long-term neurodevelopmental outcomes of infants exposed to drugs before the initiation of routine application of antifungal prophylaxis in the NICU.

• Journal of Microbiology and Biotechnology
• /
• 제27권3호
• /
• pp.429-438
• /
• 2017

For centuries, plants have been used for a wide variety of purposes, from treating infectious diseases to food preservation and perfume production. Presently, the increasing resistance of microorganisms to currently used antimicrobials in combination with the appearance of emerging diseases requires the urgent development of new, more effective drugs. Plants, due to the large biological and structural diversity of their components, constitute a unique and renewable source for the discovery of new antibacterial, antifungal, and antiparasitic compounds. In the present paper, the history, composition, and antimicrobial activities of the basil, oregano, and thyme essential oils are reviewed.

• Mycobiology
• /
• 제36권1호
• /
• pp.70-73
• /
• 2008

The antibacterial and antifungal activities of three schiff bases were evaluated against some pathogenic bacteria and fungi. Parallel experiments were also carried out with standard drugs (Kanamycin for bacteria and Nystatin for fungi). Two compounds [N-(1-phenyl-2-hydroxy-2phenylethylidine)-2',4' dinitrophenyl hydrazine, abbreviated as PDH and N-(2-hydroxy benzylidine)-2'-hydroxy imine, abbreviated as HHP] showed significant antimicrobial activities. The rest one [N-(l-phenyl 2-hydroxy-2 phenyl ethylidine) 2'-hydroxy phenyl imine, abbreviated as PHP] showed moderate activity. All these three compounds were found to possess pronounced cytotoxic effect. These compounds can be considered as potent antimicrobial agents.

• Mycobiology
• /
• 제45권4호
• /
• pp.426-429
• /
• 2017

A yeast-like organism was isolated from a urine sample of a 6-year-old neutered male miniature poodle dog with urinary tract infection, diabetes ketoacidosis, and acute pancreatitis. We identified the yeast-like organism to be Candida glabrata and found that this fungus was highly resistant to azole antifungal drugs. To understand the mechanism of azole resistance in this isolate, the sequences and expression levels of the genes involved in drug resistance were analyzed. The results of our analysis showed that increased drug efflux, mediated by overexpression of ATP transporter genes CDR1 and PDH1, is the main cause of azole resistance of the C. glabrata isolated here.

• Archives of Pharmacal Research
• /
• 제29권1호
• /
• pp.26-33
• /
• 2006

Some new derivatives of 1,2,4-triazolo[2,3-a]benzimidazoles were synthesized through the reaction of 1,2-diaminobenzimidazole with carbon disulfide. The resulting 1,2,4-triazolo-[2,3a]benzimidazole-2-thione intermediate was reacted with one equivalent of alkyl halides to give the corresponding 2-alkylthio derivatives, which were further alkylated through the reaction with another one equivalent of different alkyl halides to afford the target compounds; 1-alkyl-2alkylthio-1,2,4-traizolo[2,3-a]benzimidazoles. On the other hand, the 1,2-disubstituted derivatives with two identical alkyl substituents were prepared by the reaction of 1,2,4-triazolo[2,3-a]benzimidazole-2-thione with two equivalents of the alkyl halides. The structures of the new compounds were assigned by spectral and elemental methods of analyses. The synthesized compounds were tested for their antibacterial and antifungal activities. Most of the tested compounds proved comparable results with those of ampicillin and fluconazole reference drugs. The study indicated that, the antibacterial as well as the antifungal activities of the test compounds were improved with increase in the bulkiness of the introduced alkyl groups. Also, some active antibacterial compounds were tested for their antimycobacterial activity. All the test compounds showed equipotent antitubercular activity as that of INH as a reference drug.