Synthesis and antimicrobial evaluation of 2-(p-substituted phenyl)-5-[(4-substituted piperazin-l-yl)acetamido]-benzoxazoles.

A series of 2-(p-substituted phenyl)-5-(2-{4-[(p-chloro-fluorophenyl)/phenyl] piperazin-1-yl}acetamido)-benzoxazoles were synthesized and tested for their antimicrobial activities. The structures of the new derivatives were elucidated by spectral techniques. The minimum inhibitory concentrations (MIC) of the new benzoxazoles, along with those of previously synthesized analogues, were determined against standard bacterial and fungal strains and drug-resistant isolates, and compared with those of several reference drugs. The new benzoxazole derivatives were found to possess a broad spectrum of antimicrobial activity with MIC values of 32-1024 µg/ml. Although the standard drugs were more active against the tested pathogens, the activities of the new benzoxazoles and the reference drugs were largely similar against the drug-resistant isolates.

Synthesis and different biological activities of novel benzoxazoles.

A series of 2-[4-(4-substitutedbenzamido/phenylacetamido/butanamido)phenyl]-5-ethylsulphonyl-benzoxazole derivatives were synthesized and biologically evaluated as possible antimicrobial agents and inhibitors of tyrosinase, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE). The results demonstrated that the synthesized compounds exhibited a broad spectrum of activity with minimum inhibitory concentration (MIC) values of 128-16 µg/ml against some Gram-positive, Gram-negative bacteria as well as Candida albicans and C. krusei. The compound 10 displayed higher activity in this series against methicilline resistant Staphylococcus aureus (MRSA) with a MIC value of 16 µg/ml than the compared control drugs ampicillin and ceftriaxone. Compound 14 showed moderate tyrosinase inhibition, however, none of the compounds showed effect as inhibitor of AChE and BChE.

Novel benzoxazoles: synthesis and antibacterial, antifungal, and antitubercular activity against antibiotic-resistant and -sensitive microbes.

A new series of 5-(p-substituted benzamido/phenylacetamido)-2-(p-tert-butylphenyl)benzoxazole derivatives were synthesized and evaluated for their antibacterial, antifungal, and antimycobacterial activities against antibiotic-resistant and -sensitive Staphylococcus aureus, Enterococcus faecalis, Escherichia coli, Klebsiella pneumoniae, and Mycobacterium tuberculosis as well as against Candida albicans and Candida krusei. The compounds possessed broad-spectrum activity against all of the tested Gram-positive and Gram-negative bacteria and yeasts, their minimum inhibitory concentrations (MICs) ranging between 16-128 microg/ml. One compound exhibited significant antibacterial activity (16 microg/ml) against an antibiotic-resistant Enterococcus faecalis isolate, having twice the potency of the compared standard drugs vancomycin and gentamycin sulfate. The compounds also showed moderate antitubercular activity with MIC values between 8-128 microg/ml against Mycobacterium tuberculosis and its clinical isolate.

Synthesis and antimicrobial activity of novel benzoxazoles.

A series of 2-(p-substituted-benzyl)-5-[[4-(p-chloro/fluoro-phenyl)piperazin-1-yl]acetamido]-benzoxazoles were synthesized in need of new compounds for the fight against microbial pathogens. Their structures were elucidated by spectral techniques. These new derivatives, along with previously synthesized 2-(p-substituted-benzyl)-5-substituted-benzoxazoles, were evaluated for their antibacterial and antifungal activities against standard strains and drug-resistant isolates in comparison with ampicillin, gentamicin sulfate, ofloxacin, vancomycin, fluconazole, and amphotericin B trihydrate. The minimum inhibitory concentration (MIC) of each compound was determined by a two-fold serial dilution technique. The compounds were found to possess a broad spectrum of antimicrobial activities with MIC values of 32-256 microg/ml. Although standard drugs were more active against the pathogenes employed in this study, the activities of the new benzoxazoles and reference drugs against drug-resistant isolates of the microorganisms were largely similar.

Candida albicans and Pseudomonas aeruginosa adhesion on soft contact lenses.

BACKGROUND: In this study it was aimed to determine the adherence of Pseudomonas and Candida to contact lens surfaces, and to determine the difference in adherence between five contact lens types. Biofilm-negative control strains were also used to emphasize the difference between biofilm-positive and biofilm-negative strains in adherence. METHODS: Five different soft contact lenses were used to investigate the adherence of Pseudomonas aeruginosa and Candida albicans strains. P. aeruginosa ATCC 27853, P. aeruginosa ATCC 10145, C.albicans ATCC 10231 standard strains and C. albicans clinical isolate were included in the study. Slime formation was investigated by two methods; modified Christensen macrotube method, and a modified microtiter plate test. P. aeruginosa and C. albicans slime formation on soft contact lenses was studied in adherence and separation phases. Pseudomonas and Candida suspensions were serially diluted and inoculated to blood agar and sabouraud dextrose agar surfaces respectively. After overnight incubation, the colonies were counted. Sterile unworn contact lenses were used as negative controls, and bacterial and fungal culture suspensions were used as positive controls. The experiments were conducted in three parallel series. RESULTS: The number of adherent Pseudomonas was as follows from high to low in polymacon, etafilcon A, hilafilcon, ocufilcon and lotrafilcon contact lenses respectively. However, the number of adherent yeast were determined higher in lotrafilcon and ocufilcon contact lenses, followed by hilafilcon, etafilcon A and polymacon contact lenses. Biofilm-negative Pseudomonas ATCC standard strain and Candida clinical isolate were used to confirm that the number of adherent cells were lower than the biofilm-positive ones. CONCLUSIONS: This study demonstrates that in addition to the contact lens properties, the microorganisms themselves and their interactions with the lens material also play an important role in adherence.

[Comparison of two different methods for the investigation of in vitro susceptibilities of planktonic and biofilm forming Candida species to antifungal agents]. / Candida türlerinin biyofilm olusturan ve planktonik formlarinin antifungal ajanlara karsi in vitro duyarliliklarinin arastirilmasinda iki farkli yöntemin karsilastirilmasi

Microdilution method that determines the minimum inhibitory concentrations (MIC) of antifungal agents against Candida spp. is still the only method used in laboratories for both biofilm and planktonic forms. However, it was determined in several studies that there were susceptibility differences between the biofilm and planktonic forms of the same microorganism. The aims of this study were the determination of in vitro susceptibilities of planktonic and biofilm forms of Candida strains against antifungal agents, the comparison of the data obtained from planktonic and biofilm forms and the evaluation of two different methods used for the detection of susceptibilities of biofilm forms. Candida albicans ATCC 10231, Candida parapsilosis ATCC 90028 and Candida krusei ATCC 6258 were used as reference strains together with clinical isolates of one of each C.albicans, C.parapsilosis and Candida tropicalis. Microdilution method was used to determine the susceptibilities of planktonic forms of the strains according to CLSI M27-A3 standards, and MIC values of fluconazole, itraconazole, flucytosine, amphotericin B and nystatin were determined. For the detection of antifungal susceptibilities of Candida spp. biofilm forms, Calgary biofilm method (CBM) and BioTimer assay (BTA) were used, and minimum biofilm eradication concentration (MBEC) and minimum biofilm inhibition concentration (MBIC) values of the same antifungals were determined. The difference between MIC and CBM-MBEC, CBM-MBEC and BTA-MBEC, CBM-MBEC and BTAMBIC values were found statistically significant (p < 0.05). In general CBM-MBEC values were found to be higher than MIC values. However, MBEC values were not always very reliable since the exact number of the microorganisms in biofilm can not be determined. BTA-MBIC values were also generally lower than the MBEC values and higher than the MIC values. Statistically significant difference between two methods was determined only for the MBEC values of flucytosine (p= 0.002) and itraconazole (p = 0.025). For flucytosine (p = 0.001) and itraconazole (p = 0.001), there was also a significant difference between CBM-MBEC and BTA-MBIC values, however, the difference was not significant (p > 0.05) for the other antifungal agents. These findings supported that antifungal susceptibilities of biofilm forming Candida strains should also be investigated. However, MBEC and MBIC of the antifungal agents should not always be expected to be higher than the MIC values since the mechanism of action of the specific antifungal agents and the first inoculum concentration of the microorganisms might differ.

Antibacterial, antifungal, and antiviral activities of some flavonoids.

Antibacterial and antifungal activities of six plant-derived flavonoids representing two different structural groups were evaluated against standard strains of Escherichia coli, Pseudomonas aeruginosa, Proteus mirabilis, Klebsiella pneumoniae, Acinetobacter baumannii, Staphylococcus aureus, Enterococcus faecalis, Bacillus subtilis and their drug-resistant isolates, as well as fungi (Candida albicans, C. krusei) using the microdilution broth method. Herpes simplex virus Type-1 and Parainfluenza-3 virus were employed for antiviral assessment of the flavonoids using Madin-Darby bovine kidney and Vero cell lines. Ampicillin, gentamycin, ofloxacin, levofloxacin, fluconazole, ketoconazole, acyclovir, and oseltamivir were used as the control agents. All tested compounds (32-128 microg/ml) showed strong antimicrobial and antifungal activities against isolated strains of P. aeruginosa, A. baumanni, S. aureus, and C. krusei. Rutin, 5,7-dimethoxyflavanone-4'-O-beta-D-glucopyranoside and 5,7,3'-trihydroxy-flavanone-4'-O-beta-D-glucopyranoside (0.2-0.05 microg/ml) were active against PI-3, while 5,7-dimethoxyflavanone-4'-O-[2''-O-(5'''-O-trans-cinnamoyl)-beta-D-apiofuranosyl]-beta-D-glucopyranoside (0.16-0.2 microg/ml) inhibited potently HSV-1.

Comparison of olive oil and dry-clean keeping methods in umbilical cord care as microbiological.

The application of olive oil is one of the traditional practices used in umbilical cord care in Turkey. The study was conducted experimentally, so as to compare microbiologically the efficacy of olive oil use and keeping the stump dry. Data were obtained using a personal information form and an omphalitis follow-up form, as well as from cultures taken from the infants' umbilical cords. Cultures were taken from the neonates' umbilical cords at three different times. The Pearson chi-square test, student t test, percentages, and averages were used for statistical data analysis. The average time for separation is 9.46 days. For the control group, this period is 9.8 days, while for the study group, it is 9.1, lacking a statistically significant difference between the two groups (P > 0.05). However, when the cut-off point for umbilical cord detachment is set at 10 days, the cords of 71.6% of the neonates in the study group, compared with 55.6% of the control group, are observed to have separated before 10 days, representing a significant difference between the groups (P < 0.05). In all of the cultures collected, growth was noted in 35.9% of the study group and 33.3% of the control group. The correlation between the method used for the care of the cord and the total culture results was not statistically significant (P > 0.05). Olive oil can be used in the umbilical cord care of neonates under appropriate conditions; we recommended that this investigation be repeated on expanded sample groups.