Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:Q29983 (MIC)
 21,138 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

1-[(2-Fluorophenyl)(4-fluorophenyl)phenylmethyl]-1H-imidazole (flutrimazole, UR-4056, CAS 119006-77-8) is a new topical imidazole antifungal agent which displays potent broad-spectrum in vitro activity against dermatophytes, filamentous fungi and yeasts, saprophytic and pathogenic to animals and humans (MIC = 0.025-5.0 micrograms/ml). In most of these studies the activity of flutrimazole was comparable to that of clotrimazole and markedly higher than that of bifonazole (MIC differences of greater than or equal to 1 order of magnitude). Tested against Scopulariopsis brevicaulis (8 strains), both flutrimazole and clotrimazole exhibited fungistatic and fungicidal activity, and clotrimazole appeared something less active (MIC = 0.3-2.5 micrograms/ml) than flutrimazole (MIC = 0.15-0.6 micrograms/ml). In animal experiments, topical application of 1% and 2% flutrimazole, as a cream or solution, was highly effective in models of rat vaginal candidiasis and guinea-pig trichophytosis, giving a rate of cured or cured plus markedly improved animals higher than 80%. Flutrimazole shares the mode of action of other imidazole or triazole-containing antifungals, i.e. inhibition of fungal lanosterol 14 alpha-demethylase, as it strongly inhibits ergosterol biosynthesis in a cell-free homogenate of Candida albicans, with an IC50 value of 0.071 mumol/l.
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PMID:In vitro and in vivo studies with flutrimazole, a new imidazole derivative with antifungal activity. 141 42

The antimicrobial activity of taurolidine (Taurolin, CAS 19388-87-5), a synthetic broad-spectrum antimicrobial agent and anti-toxin, and two conventional antiseptics, chlorophenol-camphor-menthol (CCM) and chlorhexidine digluconate (CHX) were compared using the serial dilution test on 10 potential oral pathogenic bacterial species. The minimum inhibitory and minimum bactericidal concentrations were lowest for CHX (MIC 0.03-0.12 mg/ml), followed by taurolidine (MIC 0.12-0.5 mg/ml) and CCM (MIC 0.5-2.0 mg/ml). However, if both bacterial efficacy and cytotoxicity are considered, only taurolidine achieves extensive bactericidal activity with tissue tolerability.
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PMID:In vitro activity of taurolidine, chlorophenol-camphor-menthol and chlorhexidine against oral pathogenic microorganisms. 144 86

At present, only a limited number of studies of the effects of sub-inhibitory antifungal agents on the adherence of Candida to epithelial (buccal and vaginal) host cells are available. The adherence of Candida albicans to the epithelial cell surface is accepted as an important first step in persistent colonization and in the following symptomatic or asymptomatic infection of mucosal surface. Ciclopirox (ciclopiroxolamine, CAS 29342-05-0) is a substituted pyridone antimycotic drug, unrelated to the imidazole derivatives and its topical application ensures maximum local bioavailability. The present study was done to investigate the effects of sub-inhibitory concentrations of ciclopirox on the adherence of Candida albicans to human buccal and vaginal epithelial cells. The findings on the adherence of different strains of Candida indicate that the drug caused a significant reduction in the mean number of Candida adhering to both buccal and vaginal cells. This reduction was maximal at concentration of 1/2 MIC and still significant at 1/4, 1/8, 1/16 MIC, but with progressive return to mean control values at 1/32 MIC. Ciclopirox acts on fungi by inhibiting the intracellular uptake of essential substrates and ions and this probably acts on the Candida ability to express its adherence mechanisms.
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PMID:Effects of subinhibitory concentrations of ciclopirox on the adherence of Candida albicans to human buccal and vaginal epithelial cells. 149 54

The activity of 7-chloro-3-[1-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl) ethoxy-methyl]benzo[b]thiophene (sertaconazole, FI 7045, CAS 99592-32-2), a new topical antifungal, was studied in vitro against several infecting organisms. The results obtained show that sertaconazole is a broad-spectrum antifungal against yeasts (C. albicans, C. tropicalis, C. pseudotropicalis, C. krusei, Trichosporon and Cryptococcus), dermatophytes (Microsporum, Trichophyton and Epidermophyton), opportunistic filamentous fungi (Aspergillus) and Gram-positive bacteria. The MIC (minimum inhibitory concentration) values for the fungistatic activity were between 0.35 and 5.04 micrograms/ml for yeasts and between 0.24 and 2 micrograms/ml for dermatophytes; even partial activities (IC25) against these organisms were obtained at concentrations 10 times lower than those mentioned. At concentrations superior to MIC (MFC between 0.5 and 16 micrograms/ml), sertaconazole exhibited fungicidal activity.
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PMID:In vitro activity of sertaconazole. 162 86

The antifungal activity of 7-chloro-3-[1-(2,4-dichlorophenyl)-2-(1H- imidazol-1-yl)ethoxy-methyl]benzo[b]thiophene (sertaconazole, FI-7045, CAS 99592-32-2) versus miconazole has been studied in vitro against yeast-like fungi, dermatophytes and other filamentous fungi. Candida albicans was very sensitive to sertaconazole both in serotype A and serotype B strains (MIC = 0.21 micrograms/ml). Sensitivity of Candida non albicans species (MIC = 0.17 microgram/ml), Torulopsis (MIC = 0.09 microgram/ml) and Trichosporon (MIC = 0.09 microgram/ml) was also remarkable. For dermatophytes, partial inhibitions were observed at concentrations of 0.04 and 0.09 microgram/ml, the 50% inhibition ranging between 0.36 and 12.56 micrograms/ml for most strains. Filamentous opportunistic fungi were less sensitive to azoles, although sertaconazole MICs were lower than those of miconazole. Sertaconazole also proved to possess a remarkable fungicidal activity on all strains of Candida albicans under study.
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PMID:In vitro antifungal activity of sertaconazole. 162 87

The fungistatic and fungicidal activity of 7-chloro-3-[1-(2, 4-dichlorophenyl)-2-(1H-imidazol-1-yl)ethoxy-methyl]benzo[b]thiophene (sertaconazole, FI-7045, CAS 99592-32-2) against Candida albicans was determined and compared with that obtained for other antifungals. The fungistatic activity of sertaconazole, evaluated through the MIC obtained in Sabouraud and YNB media, gave results comparable to those obtained with miconazole and clotrimazole, and superior to those presented by bifonazole and ketoconazole. The fungicidal activity, evaluated by means of the 90% reduction in viable cells, took place at a concentration of 8 micrograms/ml for sertaconazole and at higher concentrations for the other drugs studied.
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PMID:In vitro comparative study of the fungistatic and fungicidal activity of sertaconazole and other antifungals against Candida albicans. 162 88

The in vitro activity of mezlocillin (MZL, CAS 51481-65-3), piperacillin (PIP, CAS 61477-96-1) and cefotaxim (CTX, CAS 63527-52-6) alone and in combination with sulbactam (SBT; CAS 68373-14-8) against mezlocillin-resistant pathogens was determined in a multicenter study. A total of 870 strains were investigated (481 Enterobacteriaceae, 57 Pseudomonas aeruginos, 41 Acinetobaster spp., 194 Bacteroides fragilis, and 97 Staphylococcus spp.). Determinations of MIC were performed according to DIN-guidelines (agar-dilution method for aerobes and microbroth-dilution method for anaerobes). Sulbactam was added in fixed concentrations of 5 mg/l and 10 mg/l. In all sulbactam-combinations examined mean MIC as well as MIC50 and MIC90 were reduced compared to the respective values for the antibiotics alone. Consequently, percentages of susceptible strains increased significantly: i.e. for Enterobacteriaceae: MZL 1% vs. MZL + 10 mg/l SBT 53%; PIP 4% vs. PIP + 10 mg/l SBT 54%; CTX 52% vs. CTX + 10 mg/l SBT 68%. The effect of sulbactam was most pronounced in Bacteroides spp. with an increase in susceptible strains from 2% to 97% for MZL, from 6% to 95% for PIP and from 7% to 98% for CTX. The results indicate that by adding sulbactam the in vitro activity of mezlocillin, piperacillin and cefotaxim against resistant pathogens is augmented significantly. In addition, the spectrum of antibacterial activity is extended to anaerobic pathogens such as Bacteroides spp. The availability of sulbactam as a monosubstance for combination with various beta-lactam-antibiotics thus represents a useful improvement of therapeutic options in bacterial infections.
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PMID:[The effect of sulbactam on the in vitro activity of mezlocillin, piperacillin and cefotaxime]. 178 6

The in vitro effects of the single agents, and the synergistic/antagonistic action of three different combinations of ampicillin (AMP, CAS 69-53-4), cefotaxime (CTX, CAS 63527-52-6), mezlocillin (MEZ, CAS 51481-65-3), and piperacillin (PIP, CAS 61477-96-1) with the beta-lactamase inhibitor sulbactam (SUL, CAS 68373-14-8) were determined against 675 gram-positive and gram-negative, both aerobic and anaerobic bacteria. All the combinations of sulbactam and the antibiotics (1: 1, 1:2 and 1:4) exhibited very similar synergistic action. The percentage of the total strains tested for which synergistic activity was found was 51% with SUL + AMP (1:1), 24% with SUL + CTX (1:1), 31% with SUL + MEZ (1:1), and 28% with SUL + PIP (1:1). A fourfold or greater reduction of MIC's in the comparison with the antibiotics alone was found with 23% of the total strains tested for the SUL + AMP, with 9% of the strains tested with SUL + CTX, with 11% of the strains tested with SUL + MEZ, and with 15% of the strains tested with the SUL + PIP-combination. In the presence of sulbactam, 18% of the strains tested showed a significant reduction in the number of resistant strains with ampicillin, 7% with cefotaxime, 16% with mezlocillin, 14% with piperacillin, and in parallel there was an increase in the number of fully susceptible strains (shift from resistant or moderately sensitive to sensitive) by about 14%. In comparison with the antibiotic alone, the most marked reductions in the number of resistant strains on combination with sulbactam were as follows (the percentage of reduction is shown in brackets): for SUL + AMP and Acine-tobacter spp. (39% fewer resistant strains). Citrobacter spp. (-60%), Enterobacter aerogenes (-48%), Klebsiella oxytoca (-49%), Klebsiella pneumoniae (-63%), Morganella morganii (-74%), and Proteus vulgaris (-55%); for SUL + CTX and Acinetobacter spp. (-38%), Enterobacter cloacae (-6%), Klebsiella pneumoniae (-16%), Serratia marcescens (-9%), and Bacteroides fragilis (-31%); for SUL + MEZ and Acinetobacter spp. (-68%), Citrobacter spp. (-27%), Enterobacter spp. (-23%), Klebsiella pneumoniae (-32%), and Serratia marcescens (-19%); for SUL + PIP and Acinetobacter spp. (-41%), Citrobacter spp. (-30%), Klebsiella spp. (-30%), and Serratia marcescens (-33%).
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PMID:In vitro activity against clinically important gram-positive and gram-negative bacteria of sulbactam, alone and in combination with ampicillin, cefotaxime, mezlocillin, and piperacillin. 229 54

Candida albicans is an opportunistic dimorphic pathogenic yeast which is present on the human mucosal epithelial cell surface. Its adhesion is considered to be an important first step in colonization and in the subsequent symptomatic or asymptomatic infection of buccal or vaginal mucosa. Because the ability to adhere is an important element of the pathogenicity of Candida we investigated in this study the compared effects of sub-inhibitory concentrations (sub-MICs) of rilopirox (CAS 104153-37-9) with those of ciclopirox olamine (CAS 41621-49-2) in inhibiting Candida adhesion to human buccal (BEC) and vaginal cells (VEC). Rilopirox is a new hydroxypyridone antimycotic agent with strong activity, especially against Candida albicans. There was a significant reduction in the mean number of Candida adhering to both buccal and vaginal cells with up to 1/8 MIC rilopirox for buccal and 1/16 MIC for vaginal cells, while for ciclopirox olamine reduction was significant up to 1/16 MIC for buccal and 1/8 MIC for vaginal cells. There were no significant differences in the dose-effect curves for BEC and VEC with either rilopirox and ciclopirox olamine, but on a molar basis, rilopirox was more active than ciclopirox olamine. The present in-vitro results support the developmental concept of an oropharyngeal and vaginal preparation of rilopirox. It can be expected that even sub-inhibitory concentrations of rilopirox exert an important additional effect in the treatment of oral and vaginal candidosis by impairing the pathogenic adhesion process of the fungus.
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PMID:Inhibition of Candida albicans adhesiveness to human buccal and vaginal cells by sub-inhibitory concentrations of rilopirox. 789 77

The postantibiotic effect and postantibiotic sub-MIC effect of ofloxacin (CAS 82419-36-1), tobramycin (CAS 32986-56-4) and ceftriaxone (CAS 73384-59-5) on two salmonella serotypes (S. typhimurium and S. enteritidis) were studied. The influence of postantibiotic effect and postantibiotic sub-MIC effect of the antibiotics on prophage induction of the lysogenic S. typhimurium strain and on Congo red binding by both serovars as indicator of their invasive ability was examined. The postantibiotic effect was induced by exposure of the bacteria to the 2x and 4x MIC concentrations of antibiotics studied for 0.5 h. The postantibiotic effects were different; ceftriaxone induced the longest postantibiotic effect against S. enteritidis, and the 4x MIC of tobramycin induced the longest postantibiotic effect against S. typhimurium. The postantibiotic sub-MIC effects lasted longer and in the case of subinhibitory concentrations of tobramycin on S. typhimurium and ceftriaxone on S. enteritidis did not allow any regrowth. The results showed that the postantibiotic effect and postantibiotic sub-MIC effect of ofloxacin induced a prophage of a lysogenic S. typhimurium strain, and the postantibiotic sub-MIC effects of tobramycin influenced Congo red binding by S. enteritidis cells.
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PMID:Pharmacodynamic parameters of ofloxacin, tobramycin and ceftriaxone and their effect on the biological properties of salmonellae. 934 22


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