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European Journal of Medicinal Chemistry Jul 2020Herein, based on the theory of bioisosterism, a series of novel miconazole analogues containing selenium were designed, synthesized and their inhibitory effects on...
Herein, based on the theory of bioisosterism, a series of novel miconazole analogues containing selenium were designed, synthesized and their inhibitory effects on thirteen strains of pathogenic fungi were evaluated. It is especially encouraging that all the novel target compounds displayed significant antifungal activities against all tested strains. Furthermore, all the target compounds showed excellent inhibitory effects on fluconazole-resistant fungi. Subsequently, preliminary mechanistic studies indicated that the representative compound A03 had a strong inhibitory effect on C.alb. CYP51. Moreover, the target compounds could prevent the formation of fungi biofilms. Further hemolysis test verified that potential compounds had higher safety than miconazole. In addition, molecular docking study provided the interaction modes between the target compounds and C.alb. CYP51. These results strongly suggested that some target compounds are promising as novel antifungal drugs.
Topics: Antifungal Agents; Biofilms; Drug Design; Drug Resistance, Multiple, Fungal; Fluconazole; Fungi; Humans; Miconazole; Microbial Sensitivity Tests; Molecular Docking Simulation; Organoselenium Compounds; Structure-Activity Relationship
PubMed: 32403018
DOI: 10.1016/j.ejmech.2020.112360 -
Mykosen Mar 1978
Topics: Drug Tolerance; Humans; Imidazoles; Miconazole; Time Factors; Tinea Versicolor
PubMed: 642972
DOI: 10.1111/j.1439-0507.1978.tb01618.x -
Drug and Therapeutics Bulletin Sep 1975
Topics: Candidiasis; Dermatomycoses; Female; Humans; Imidazoles; Miconazole; Vaginal Creams, Foams, and Jellies; Vaginal Diseases
PubMed: 1183317
DOI: No ID Found -
Journal of Drugs in Dermatology : JDD Jun 2016Present research work was aimed at formulation and evaluation of antifungal activity of miconazole nitrate (MN) vesicles vs C. albicans spp.
OBJECTIVE
Present research work was aimed at formulation and evaluation of antifungal activity of miconazole nitrate (MN) vesicles vs C. albicans spp.
METHODS
Miconazole loaded vesicles were prepared by coacervation phase separation technique using nonionic surfactants and stabilizers. The antimycological activity of vesicles was performed using agar disc diffusion technique.
RESULTS
The miconazole nitrate lipid vesicles F5A and F5B showed maximum activity with higher zones of inhibition ie, 13.95+1.54 mm and 13.64+0.65 mm, respectively, after 3 days (For all comparisons, P<.05 was considered significant).
CONCLUSION
The findings of this study suggest antifungal potential of a novel preparation of miconazole nitrate vesicles vs Candida albicans in the treatment of mycoses in dermatological practice.
J Drugs Dermatol. 2016;15(6):734-737.Topics: Antifungal Agents; Candida albicans; Drug Carriers; Drug Compounding; Humans; Miconazole; Nanoparticles
PubMed: 27272081
DOI: No ID Found -
Journal of Drugs in Dermatology : JDD May 2007The potential for toxicity from systemic absorption of topical miconazole in infants is a concern. (Clinical Trial)
Clinical Trial
BACKGROUND
The potential for toxicity from systemic absorption of topical miconazole in infants is a concern.
OBJECTIVE
To assess the relative safety of 0.25% miconazole based on the amount absorbed through the skin of infants with diaper dermatitis after multiple applications.
METHODS
Of 24 infants with moderate to severe diaper dermatitis, 19 received 0.25% miconazole nitrate ointment and 5 received 2% miconazole nitrate cream for 7 days at each diaper change and after bathing. Blood samples were collected prior to treatment and after 7 days.
RESULTS
In the 0.25% treatment group, blood concentrations of miconazole were nondetectable (< 1 ng/mL) in 83% (15/18) and minimal (3.0 to 3.8 ng/mL) in 17% (3/18). Samples were missing for one patient. For the 5 infants in the 2% treatment group, miconazole concentration was nondetectable in 20% (1/5) and less than 7.4 ng/mL in 4 infants. No adverse events were noted.
CONCLUSIONS
Systemic absorption of 0.25% miconazole nitrate ointment was minimal, demonstrating its safety in the treatment of moderate to severe diaper dermatitis.
Topics: Antifungal Agents; Diaper Rash; Female; Gastrointestinal Diseases; Humans; Infant; Male; Miconazole; Ointments; Severity of Illness Index; Skin Absorption; Treatment Outcome
PubMed: 17679187
DOI: No ID Found -
Journal of Oral Rehabilitation May 2006The feasibility of using collagen as the base of miconazole was investigated. The addition of 33% collagen to a miconazole solution did not affect the minimal inhibitory...
The feasibility of using collagen as the base of miconazole was investigated. The addition of 33% collagen to a miconazole solution did not affect the minimal inhibitory concentration (MIC80) of the miconazole solution for Candida albicans. When 1 microg mL(-1) of miconazole in 33% collagen solution was plated on resin discs and dried to yield a thin membrane, the growth of C. albicans on the resin discs was nearly completely inhibited. In addition, we compared the antifungal effect of this collagen solution that contained 1 microg mL(-1) miconazole, with the antifungal effect of miconazole gel that had been diluted with glycerol (the main component of miconazole gel) to yield a final concentration of 1 microg mL(-1) of miconazole; as a result, we found that the collagen solution containing 1 microg mL(-1) miconazole had a stronger antifungal effect. In conclusion, our results demonstrated that it may be feasible to use collagen as the base of miconazole instead of glycerol, and suggest that a collagen-based miconazole solution would have a stronger antifungal effect than commercially available miconazole gel. Collagen-based miconazole solution may be useful for the treatment of Candida-associated denture stomatitis.
Topics: Antifungal Agents; Candida albicans; Collagen; Colony Count, Microbial; Drug Carriers; Drug Evaluation, Preclinical; Feasibility Studies; Humans; Miconazole; Microbial Sensitivity Tests
PubMed: 16629895
DOI: 10.1111/j.1365-2842.2005.01568.x -
Antimicrobial Agents and Chemotherapy Dec 1979The effectiveness of miconazole was evaluated in 37 documented fungal infections, 32 of which were major infections. All patients were receiving therapy for advanced...
The effectiveness of miconazole was evaluated in 37 documented fungal infections, 32 of which were major infections. All patients were receiving therapy for advanced malignancy, with 28 patients having acute leukemia. The overall cure rate was 41% and it was also 41% for major fungal infections. Nine of 22 patients with Candida albicans infections were cured, and 3 of 11 patients with Candida tropicalis infections were cured. A total of 183 patients who received miconazole for presumed or documented fungal infection were evaluated for toxicity. Nausea and vomiting and central nervous system toxicity were the most common side effects, occurring in 25 and 16% of the patients, respectively. Overall, the drug was tolerated well, with only four patients requiring the drug to be permanently discontinued because of toxicity.
Topics: Adolescent; Adult; Aged; Candida; Candidiasis; Female; Humans; Imidazoles; Male; Miconazole; Middle Aged; Mycoses; Neoplasms; Time Factors
PubMed: 575281
DOI: 10.1128/AAC.16.6.792 -
Archives of Internal Medicine Jul 1979The efficacy and safety of intravenously administered miconazole nitrate was examined in eight patients with the following infections: cutaneous North American...
The efficacy and safety of intravenously administered miconazole nitrate was examined in eight patients with the following infections: cutaneous North American blastomycosis (one), extensive dermatophytosis(one), and chronic mucocutaneous candidiasis (six). Mycologic assessment included direct examination for fungal elements, fungal culture, and histopathology. Laboratory evaluations were performed before and at regular intervals during the study. The total miconazole nitrate dosage, which was administered over a seven- to 32-day period, ranged from 4.0 to 46.8 g. Follow-up examinations extended from two to 15 months. Excellent results were obtained in five patients and fair results in three. No renal, cardiac, hepatic, or hematopoietic toxicity was observed. Other side effects, however, necessitated premature cessation of therapy in four patients. Overall, intravenously administered miconazole is an effective antifungal agent for these cutaneous infections.
Topics: Adolescent; Adult; Child; Dermatomycoses; Female; Humans; Imidazoles; Injections, Intravenous; Male; Miconazole; Middle Aged; Phlebitis
PubMed: 454066
DOI: No ID Found -
Antimicrobial Agents and Chemotherapy Mar 1998
Topics: Antifungal Agents; Helicobacter pylori; Miconazole
PubMed: 9517964
DOI: 10.1128/AAC.42.3.725 -
The American Review of Respiratory... Nov 1977
Topics: Adolescent; Adult; Aged; Child; Coccidioidomycosis; Drug Resistance, Microbial; Humans; Imidazoles; Miconazole; Middle Aged; Mycoses; Paracoccidioidomycosis; Recurrence
PubMed: 921060
DOI: 10.1164/arrd.1977.116.5.801