In order to develop new antifungal agents effective against two species of Candida, we have designed a series of dihydrofolate reductase (DHFR) inhibitors. Here, we explore the structure-activity relationships of these inhibitors toward Candida albicans DHFR by evaluating enzyme inhibition, antifungal activity and toxicity to mammalian cells. Analysis of docked complexes of the enzyme and inhibitors yields the structural basis of relative potency. The meta-biphenyl series of this class exhibits the greatest enzyme inhibition, selectivity and antifungal activity.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2724765 | PMC |
| http://dx.doi.org/10.1016/j.bmc.2009.06.021 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
A Novel and Robust Method for Investigating Fungal Biofilm.
Bio Protoc
January 2025
Laboratory of Protein Translation and Fungal Pathogenesis, Regional Centre for Biotechnology, Faridabad, India.
, labeled an urgent threat by the CDC, shows significant resilience to treatments and disinfectants via biofilm formation, complicating treatment/disease management. The inconsistencies in biofilm architecture observed across studies hinder the understanding of its role in pathogenesis. Our novel in vitro technique cultivates biofilms on gelatin-coated coverslips, reliably producing multilayer biofilms with extracellular polymeric substances (EPS).
View Article and Find Full Text PDFConcomitant Inhibition and Collaring of Dual-Species Biofilms Formed by and by Triazole Based Small Molecule Inhibitors.
Pharmaceutics
December 2024
Department of Chemistry, College of Science, University of Jeddah, Jeddah 21589, Saudi Arabia.
Background/objectives: Biofilm-associated infections, particularly those involving Candida auris and Staphylococcus aureus, pose significant challenges in clinical settings due to their resilience and resistance to conventional treatments. This study aimed to synthesize novel triazole derivatives containing a piperazine ring via click chemistry and evaluate their efficacy in disrupting biofilms formed by these pathogens.
Methods: Triazole derivatives were synthesized using click chemistry techniques.
Virtual screening assisted identification of a phytocompound as potent inhibitor against Candida lusitaniae; an in-silico study.
BMC Infect Dis
January 2025
Department of Clinical Laboratory Sciences, College of Applied Medical Science, King Khalid University, Abha, Saudi Arabia.
Candida lusitaniae is one of the fungal species which causes serious health illnesses including peritonitis, vaginitis and fungemia, among others. Several antifungal drugs have been designed to tackle its infections but their efficacy is still questionable due to their associated side effects. Hence, there is a need to design those drugs which possess comparatively higher degree of therapeutic potential.
View Article and Find Full Text PDF[Septic musculoskeletal complications under immunomodulating treatment].
Z Rheumatol
January 2025
Rheumatologische Facharztpraxis Schwerin, Schwerin, Deutschland.
Infections are an important cause of morbidity and mortality in patients with inflammatory rheumatic diseases. Among these, musculoskeletal infections represent a relevant proportion as patients with rheumatoid arthritis face an increased risk of developing septic arthritis and prosthesis infections. The causes are multifactorial.
View Article and Find Full Text PDF[Updates in General Management and Frequent Complications Following Adult Liver Transplant].
Rev Med Chil
June 2024
Departamento de Gastroenterología, Escuela de Medicina, Pontificia Universidad Católica de Chile, Santiago, Chile.
Liver transplantation (LT) is a cost-effective therapy for advanced liver disease. Although LT significantly improves long-term survival, it requires strict control of immunosuppressants and their potential complications. Several available immunosuppressive drugs include glucocorticoids, calcineurin inhibitors, mycophenolate, mTOR inhibitors, and anti-CD25 antibodies.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!