Peptide dendrimers as antifungal agents and carriers for potential antifungal agent— N 3 ‐(4‐methoxyfumaroyl)‐( S )‐2,3‐diaminopropanoic acid—synthesis and antimicrobial activity

2019 ◽  
Vol 26 (1) ◽  
Author(s):  
Magdalena Stolarska ◽  
Katarzyna Gucwa ◽  
Zofia Urbańczyk‐Lipkowska ◽  
Ryszard Andruszkiewicz
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Agent ◽  
Antifungal Agents ◽  
Acid Synthesis ◽  
Peptide Dendrimers ◽  
Diaminopropanoic Acid

scholarly journals Moderate levels of 5-fluorocytosine cause the emergence of high frequency resistance in cryptococci

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Yun C. Chang ◽  
Ami Khanal Lamichhane ◽  
Hongyi Cai ◽  
Peter J. Walter ◽  
John E. Bennett ◽  
...  
Keyword(s):  
Cellular Uptake ◽  
High Frequency ◽  
Antifungal Agent ◽  
Inhibitory Concentration ◽  
Glucuronic Acid ◽  
Rapid Development ◽  
Acid Synthesis ◽  
Transcriptional Factor ◽  
Development Of Resistance ◽  
Acid Accumulation

AbstractThe antifungal agent 5-fluorocytosine (5-FC) is used for the treatment of several mycoses, but is unsuitable for monotherapy due to the rapid development of resistance. Here, we show that cryptococci develop resistance to 5-FC at a high frequency when exposed to concentrations several fold above the minimal inhibitory concentration. The genomes of resistant clones contain alterations in genes relevant as well as irrelevant for 5-FC resistance, suggesting that 5-FC may be mutagenic at moderate concentrations. Mutations in FCY2 (encoding a known permease for 5-FC uptake), FCY1, FUR1, UXS1 (encoding an enzyme that converts UDP-glucuronic acid to UDP-xylose) and URA6 contribute to 5-FC resistance. The uxs1 mutants accumulate UDP-glucuronic acid, which appears to down-regulate expression of permease FCY2 and reduce cellular uptake of the drug. Additional mutations in genes known to be required for UDP-glucuronic acid synthesis (UGD1) or a transcriptional factor NRG1 suppress UDP-glucuronic acid accumulation and 5-FC resistance in the uxs1 mutants.

Esters, amides and substituted derivatives of cinnamic acid: synthesis, antimicrobial activity and QSAR investigations

2004 ◽  
Vol 39 (10) ◽  
pp. 827-834 ◽  
Author(s):  
Balasubramanian Narasimhan ◽  
Deepak Belsare ◽  
Devayani Pharande ◽  
Vishnukant Mourya ◽  
Avinash Dhake
Keyword(s):  
Antimicrobial Activity ◽  
Cinnamic Acid ◽  
Acid Synthesis ◽  
Derivatives Of

scholarly journals Synthesis, Characterization and Antimicrobial Activity of Metal Chelates of 5-[4-Chloro phenyl(1, 3, 4)thiadiazol-2-ylamino methylene]-8-hydroxy quinoline

2009 ◽  
Vol 6 (4) ◽  
pp. 1017-1022 ◽  
Author(s):  
Divyesh K. Patel ◽  
Arun Singh
Keyword(s):  
Antimicrobial Activity ◽  
Magnetic Properties ◽  
Antifungal Activity ◽  
Sodium Bicarbonate ◽  
Antifungal Agents ◽  
Metal Chelates ◽  
Spectral Studies ◽  
Transition Metal Chelates ◽  
Hydroxy Quinoline ◽  
Metal Ligand

5-Chloromethyl-8-quinolinol was condensed stoichiometrically with 5-(4-chlorophenyl)-(1,3,4) thiadiazol-2-ylamine in the presence of sodium bicarbonate. The resulting 5-[4-chlorophenyl-(1,3,4)thiadiazol-2-ylamino methylene]-8-quinolinol (CTAQ) was characterized by elemental analysis and spectral studies. The transition metal chelatesviz. Cu2+, Ni2+, Co2+, Mn2+and Zn2+of CTAQ were prepared and characterized by metal-ligand (M:L) ratio, IR and reflectance spectroscopies and magnetic properties. The antifungal activity of CTAQ and its metal chelates was screened against various fungi. The results show that all these samples are good antifungal agents.

scholarly journals In Vitro Antifungal Activities of a Series of Dication-Substituted Carbazoles, Furans, and Benzimidazoles

1998 ◽  
Vol 42 (10) ◽  
pp. 2503-2510 ◽  
Author(s):  
Maurizio Del Poeta ◽  
Wiley A. Schell ◽  
Christine C. Dykstra ◽  
Susan K. Jones ◽  
Richard R. Tidwell ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Candida Albicans ◽  
Fusarium Solani ◽  
Antifungal Agents ◽  
Antifungal Drugs ◽  
Inhibitory Compounds ◽  
Wide Range ◽  
Fluconazole Resistant ◽  
Resistant Strains

ABSTRACT Aromatic dicationic compounds possess antimicrobial activity against a wide range of eucaryotic pathogens, and in the present study an examination of the structures-functions of a series of compounds against fungi was performed. Sixty-seven dicationic molecules were screened for their inhibitory and fungicidal activities againstCandida albicans and Cryptococcus neoformans. The MICs of a large number of compounds were comparable to those of the standard antifungal drugs amphotericin B and fluconazole. Unlike fluconazole, potent inhibitory compounds in this series were found to have excellent fungicidal activities. The MIC of one of the most potent compounds against C. albicans was 0.39 μg/ml, and it was the most potent compound against C. neoformans (MIC, ≤0.09 μg/ml). Selected compounds were also found to be active againstAspergillus fumigatus, Fusarium solani,Candida species other than C. albicans, and fluconazole-resistant strains of C. albicans and C. neoformans. Since some of these compounds have been safely given to animals, these classes of molecules have the potential to be developed as antifungal agents.

Use of Antifungal Therapy in Hospitalized Patients II. Results after the Marketing of Fluconazole

1994 ◽  
Vol 28 (2) ◽  
pp. 261-270 ◽  
Author(s):  
Thaddeus H. Grasela ◽  
Mary T. Pasko ◽  
S. Diane Goodwin ◽  
Cynthia A. Walawander ◽  
Nicole Blackwelder ◽  
...  
Keyword(s):  
Phase I ◽  
Amphotericin B ◽  
Phase Ii ◽  
Antifungal Therapy ◽  
Antifungal Agent ◽  
Phase I Study ◽  
Antifungal Agents ◽  
Hospitalized Patients ◽  
Prescribing Patterns ◽  
Systemic Antifungal Therapy

OBJECTIVE: To evaluatethe prescribing patternsof antifungal agents in the hospital setting after the introduction of fluconazole, a new broad-spectrum bis-triazole antifungal agent. Also comparedare the prescribing patterns of antifungal agents prior to (phase I) and following (phase II) fluconazole marketing. DESIGN: A prospective cohort of hospitalized patients prescribed topical or systemic antifungal agents. Data were collected from December 1990 to April 1991. SETTING: Fifty-seven hospitals ranging in size from 100 to more than 500 beds. Sixty-three percentare affiliated with medical schools. PATIENTS: Participating pharmacists consecutively identified 15 patients receiving systemic antifungal therapy and 5 patients receiving topical antifungal therapy. INTERVENTIONS: Observational data on patient antifungal therapy, risk factors for fungal infections, comorbidities, concurrent medications, and culture data were collected. MEASURES: Differences in prescribing patterns before and after the marketing of fluconazole were assessed using t-tests and chi-square tests. RESULTS: Of 818 patients studied, 615 (75.2 percent) received systemic antifungal therapy. Five hundred forty-six patients received a single antifungal agent; 348 (63.7 percent) received fluconazole, 105 (19.2 percent) received ketoconazole, 92 (16.8 percent) received amphotericin B, and 1 (0.2 percent) received flucytosine. Sixty-nine patients received two or more systemic agents either concurrently or consecutively. The use of parenteral amphotericin B, alone or in combination with flucytosine and/or an azole, declined from 56.8 percent in the phase I study to 24.2 percent in the current study. The use of parenteral therapy also declined from 56.8 to 40.2 percent. Ketoconazole was used in more than 90 percent of the oral and esophageal infections in the phase I study, but its use declined to only 33 percent in this study. Fluconazole was used most frequently across all sites of presumed or documented infections, with the exception of fungemia. Of the presumed or proven systemic or blood infections, amphotericin B was used alone or in combination in 48.4 percent of the patients and fluconazole was used exclusively in 39.0 percent of the patients. Fluconazole was used more often than amphotericin B (22 vs. 3 patients, respectively) for prophylaxis of systemic infections. The overall use of antifungal prophylaxis also increased from the phase I (9.5 percent) to phase II (13.7 percent). CONCLUSIONS: The introduction of fluconazole had a major impact on the prescribing patterns of antifungal therapy. Although amphotericin B remained the preferred agent for treatment of suspected or proven systemic, central nervous system, or blood infections, use of fluconazole for these indications approached nearly 40 percent. Further studies are needed to address the role of fluconazole in the prophylaxis and treatment of systemic mycoses.

scholarly journals In Vitro Human Onychopharmacokinetic and Pharmacodynamic Analyses of ME1111, a New Topical Agent for Onychomycosis

2017 ◽  
Vol 62 (1) ◽  
Author(s):  
Natsuki Kubota-Ishida ◽  
Naomi Takei-Masuda ◽  
Kaori Kaneda ◽  
Yu Nagira ◽  
Tsubasa Chikada ◽  
...  
Keyword(s):  
Antifungal Agent ◽  
Antifungal Agents ◽  
Nail Plate ◽  
Free Drug ◽  
Content Type ◽  
Clinical Dose ◽  
Drug Concentrations ◽  
Liquid Chromatography Tandem Mass ◽  
Human Nails

ABSTRACT ME1111 is a novel antifungal agent currently under clinical development as a topical onychomycosis treatment. A major challenge in the application of topical onychomycotics is penetration and dissemination of antifungal agent into the infected nail plate and bed. In this study, pharmacokinetic/pharmacodynamic parameters of ME1111 that potentially correlate with clinical efficacy were compared with those of marketed topical onychomycosis antifungal agents: efinaconazole, tavaborole, ciclopirox, and amorolfine. An ME1111 solution and other launched topical formulations were applied to an in vitro dose model for 14 days based on their clinical dose and administration. Drug concentrations in the deep layer of the nail and within the cotton pads beneath the nails were measured using liquid chromatography-tandem mass spectrometry. Concentrations of ME1111 in the nail and cotton pads were much higher than those of efinaconazole, ciclopirox, and amorolfine. Free drug concentrations of ME1111 in deep nail layers and cotton pads were orders of magnitude higher than the MIC90 value against Trichophyton rubrum (n = 30). Unlike other drugs, the in vitro antifungal activity of ME1111 was not affected by 5% human keratin and under a mild acidic condition (pH 5.0). The in vitro antidermatophytic efficacy coefficients (ratio of free drug concentration to MIC90s against T. rubrum) of ME1111, as measured in deep nail layers, were significantly higher than those of efinaconazole, tavaborole, ciclopirox, and amorolfine (P < 0.05). This suggests that ME1111 has excellent permeation of human nails and, consequently, the potential to be an effective topical onychomycosis treatment.

Research on antibacterial and antifungal agents. VIII. synthesis and antimicrobial activity of 1,4-diarylpyrroles

1992 ◽  
Vol 27 (7) ◽  
pp. 717-722 ◽  
Author(s):  
GC Porretta ◽  
M Biava ◽  
R Fioravanti ◽  
M Fischetti ◽  
C Melino ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Agents ◽  
Antibacterial And Antifungal
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