جستجوی مقالات مرتبط با کلیدواژه "آزول ها" در نشریات گروه "پزشکی"

3,2,1 triazoles are an important class of five-membered heterocyclic compounds whose unique biological properties have made them an important class of chemical compounds. The biological activity of these compounds is known as anti-fungal, anti-bacterial, anti-tumor, anti-inflammatory, anti-depressant, anti-tuberculosis, anti-HIV, etc.  

In this research, first we synthesized new courcomin catalyst. We investigated synthesis of some 1,2,3 triazol derivatives and evaluated their anti-bacterial and anti-fungal effects. After synthesis and purification of some 1,2,3-triazol compound, the inhibitory effect of compounds against fungal (Candida albicans, Aspergillus niger) and against bacterial (Staphylococcus arueus and Escherichia coli) was evaluated.

It was found that compound (3): 1-(4-bromobenzyl)-1H-1,2,3-triazol-4-ol exhibited the best antifungal activities. Also this compound showed good activity against Staphylococcus areus as a Gram-positive bacteria.

According to the results, it seems that the use of recombinant substance 3 as a new compound with acceptable antimicrobial properties can be considered

The management of Candida-related infectious diseases and the recognition of drug susceptibility patterns in each region depend on local epidemiological studies and population structure of each region. The present study was carried out with the aim of identifying the common species associated with VVC and determining their antifungal susceptibility profile.

In this study, 140 clinical isolates of Candida species were collected from people with vaginitis referred to a number of health centers in Zanjan, Iran. Antifungal susceptibility tests for fluconazole, itraconazole and ketoconazole was performed by broth microdilution method, and the results were statistically analyzed using SPSS software.

Overall 41 Candida species were isolated from vaginal discharge samples. C. glabrata was the most frequent with 23 isolates (56.1%). Candida isolates showed high resistance to azoles, so that 11 isolates (26.8%) were resistant to fluconazole. Also, the resistance to itraconazole and ketoconazole was found to be 58.5% and 65.9%, respectively.

In this study C. glabrata had the highest prevalence and it shows the change in the pattern of Candida infections towards non-albicans species. The occurrence of high drug resistance to azoles is one of the problems facing vaginal candidiasis, which leads to recurrent and treatment-resistant infections.

  Azole nucleuses are very important part of antimicrobial, analgesic and anti-inflammatory drugs. The azole class of compounds is the most popular among the antibacterial and antifungal classes because of its lower toxicity, higher efficacy and a broad spectrum of activity. Today, Efforts have focused on the development of new, less toxic and more efficacious antifungal and antibacterial drugs, with the novel mechanism of action. In this study, we tried to investigate the antibacterial and antifungal effects of the new azole derivatives. This research is a descriptive – cross sectional study. The antibacterial and antifungal activity of compounds was evaluated using the minimum inhibitory concentration (MIC) method on a series of gram positive and gram negative bacterial strains and Aspergillus niger, Aspergillus flavus, Candida albicans. The Minimum Inhibitory Concentration from the growth of this bacteria and fung ranges from 12.5 mg/ml to 200 mg/ml. Among the tested compounds, 4- Nitro, 2- methyl imidazole hetrocycle-pathic compound exerted potent in vitro antibacterial activity against Pseudomonas aeruginosa, Escherichia coli, Bacillus subtilis and Staphylococcus aureus while compounds (imidazole, benzimidazole hetrocycle-pathic compound) exhibited potent in vitro antifungal activity against Candida albicans, Aspergillus flavus and Aspergillus niger. Our results indicated that the designed derivatives (4- Nitro, 2- methyl imidazole, imidazole and benzimidazole hetrocycle-pathic compounds) showed effective antibacterial and antifungal activity mainly against a series of gram positive and gram negative bacterial strains. On the other hand, the tested compounds had an appropriate spectrum effect, because they showed antibacterial effect on both positive and negative strains.

The azole class of compounds is the most popular among the antifungal classes because of its lower toxicity, higher efficacy, and a broad spectrum of activity. Ergosterol is the main component of the fungal cell membrane. Inhibition of the 14α-demethylase enzyme will result in decreased ergosterol synthesis. Ergosterol plays a hormone-like role in fungal cells, which stimulates growth. The net effect of azoles is inhibition of fungal growth. In this research, a group of azole derivatives with CYP51 inhibitory activity was subjected to a docking study, followed by toxicity risk assessment.   This research is a descriptive-analytic study. In order to investigate the mode of the benzimidazole oxime ether derivatives coupling with the enzyme active site, at first, the chemical structures of all compounds were designed using the ChemBioDraw Ultra14.0 software. Then to maximize energy efficiency, they were exported into the HyperChem software package. Docking study was performed using the Auto Dock Vina program. Then the results were analyzed utilizing the Molegro Virtual Docking software. At the final stage, the toxicity risk assessment of compounds was performed using the OSIRIS program.   According to docking study results, the main bonds in drug-receptor interactions are azole-heme coordination, the hydrogen bond, and hydrophobic interactions. Among all studied compounds, the best docking results are related to combination No.1 (imidazole heterocycle-pathic compound). In fact, this compound had the most negative ΔGbind (-9.17 Kcal/mol), which indicated favorable interactions with the key amino acid residues at the active site of CYP51.   According to the results of docking studies and the evaluation of toxicity risk, it can be concluded that combination No. 1(imidazole heterocycle-pathic compound) in comparison with fluconazole reference compound might be considered a more effective inhibitor of the CYP51 enzyme.

Leishmaniasis is a group of tropical diseases with high worldwide prevalence and difficulty in management. At present, the development of resistance and the increase of co-infected leishmaniasis with AIDS have become a serious public health problem. Thus, designing and discovery of effective and non-toxic drugs for the treatment of this disease is very urgent. Azole derivatives have displayed a wide range of biological activities. The pharmacological interest of azole compounds has been established to find new antileishmanial agents. The usefulness of some well-known azole antifungals has been also reported previously. Generally, azole antifungals have a common pharmacophoric portion namely N-phenethylazole and act by inhibiting the cytochrome P-450-mediated 14α-demethylation of lanosterol. Apart from azole antifungals with N-phenethylazole structure, a variety of N-aryl azoles and fused azole derivatives have been reported as antileishmanial agents. These compounds possess distinct structure and mechanism of action differing from those of azole antifungals. Thus, in this paper we reviewed the current application of N-aryl azoles and fused azoles for the design and development of new antileishmanial agents.

Invasive fungal infections with high mortality rate are a growing health concern in hospitals and medical centers. The infection usually occurs in people with compromised immune systems. The purpose of this paper is a review of the most commonly prescribed antifungal drugs for invasive fungal diseases. Antifungals consist of the four main groups; polyenes¡ azoles¡ echinocandins and DNA and RNA synthesis inhibitors. Amphotericin B is one of the most significant antifungal agents effective against Aspergillus¡ Candida and Mucor species¡ but due to several side effects¡ it is not used for prophylaxis. Its lipid formulation has lower toxicity. Azoles have an extensive activity against a broad spectrum of filamentous fungi and Candida species. Voriconazole is the drug of choice in the prophylaxis and treatment of the patients susceptible to Aspergillus infections. Posaconazole is an oral azole used to treat mucormycosis.5fluorocytosine is an antifungal drug with intracellular mechanisms that is used routinely for the treatment of cryptococcal meningitis. Echinocandins are the latest family of antifungal agents and include caspofungin¡ anidulafungin and micafungin. They are effective against Candida and can serve as an alternative for azoles. There is a variety of antifungal treatments and monotherapy has been the best; however¡ to prevent side effects of a medicine with high-dose and resistance¡ combination treatments are under investigation.

Oral candidiasis، caused by Candida albicans، is one of the most common infections in immunocompromised patients، especially in HIV+ individuals. The aims of this study were to evaluate the susceptibility of C. albicans isolates to azole drugs and Trachyspermum ammi essential oil. Oral swabs were cultured from 70 HIV+ patients and In order to identify and confirm of C. albicans isolates، Chrom agar، Corn meal agar، germ tube production، carbohydrate assimilation، growth at 45˚C and PCR were performed. Sensivity to fluconazol، ketoconazole and clotrimazol were assessed by disc diffusion and also the effect of T. ammi essential oil was determined by disc diffusion and microdilution broth methods. The causative agent، in 50 patients with oral candidiasis، was C. albicans (71. 4%). In sensivity determination survey to antifungal drugs، the resistance of isolates to fluconazole، ketoconazole and clotrimazole were determined 32%، 28% and 14%، respectively. In disc diffusion، all isolates have an acceptable sensivity at 10 - 20 μL of the oil and 30 μL inhibit the growth completely in plate. Minimum Inhibitory Concentrsation (MIC) by microdilution broth method was 500ppm and 750ppm in 72% and 28% of isolates، respectively، and Minimum Fungicidal Concentration (MFC) in 70% of isolates were 750ppm and for the rest of the isolates (30%) were 1000ppm. We conclude that use of this native plant، as an antifungal compound، could act as a treatment of the patients with mucosal candidiasis، beside of other drugs in to the future.