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antifungal agents

Alex G Baldwin, Jonathan Bevan, David Brough, Ruth Ledder, Sally Freeman
Dehydroacetic acid is a common pyrone derivative used commercially as an antibacterial and antifungal agent. Based on the synthesis of dehydroacetic acid ( 1 ) from N -hydroxysuccinimdyl acetoacetate, a novel series of enamine-based derivatives were synthesised in order to improve the antibacterial activity of dehydroacetic acid. The antibacterial activities of the synthesised analogues were evaluated against Escherichia coli and Staphylococcus aureus . Derivative 4d (N-Ph) was identified as the most potent inhibitor of S...
2018: Medicinal Chemistry Research
Ju-Hyun Kim, Won-Gu Choi, Ju-Yeon Moon, Joo Young Lee, Sangkyu Lee, Hye Suk Lee
Itraconazole (ITZ) is a first-generation triazole-containing antifungal agent that effectively treats various fungal infections. As ITZ has a better safety profile than that of ketoconazole (KCZ), ITZ has been used worldwide for over 25 years. However, few reports have explored the metabolic profile of ITZ, and the underlying mechanism of ITZ-induced liver injury is not clearly understood. In the present study, we revisited ITZ metabolism in humans, using a non-targeted metabolomics approach, and identified several novel metabolic pathways including O-dearylation, piperazine oxidation, and piperazine-N,N'-deethylation...
March 7, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Tânia Raquel Rodrigues Grainha, Paula Alexandra da Silva Jorge, Martín Pérez-Pérez, Gael Pérez Rodríguez, Maria Olívia Baptista Oliveira Pereira, Anália Maria Garcia Lourenço
The complex virulence attributes of Candida albicans are an attractive target to exploit in the development of new antifungals and anti-virulence strategies to combat C. albicans infections. Particularly, quorum-sensing (QS) has been reported as critical for virulence regulation in C. albicans. This work presents two knowledge networks with up-to-date information about QS regulation and experimentally tested anti-QS and anti-virulence agents for C. albicans. A semi-automatic bioinformatics workflow that combines literature mining and expert curation was used to retrieve otherwise scattered information from the scientific literature...
March 6, 2018: FEMS Yeast Research
Enea Gino Di Domenico, Ilaria Cavallo, Maria Guembe, Grazia Prignano, Maria Teresa Gallo, Valentina Bordignon, Giovanna D'Agosto, Isabella Sperduti, Luigi Toma, Fabrizio Ensoli
Candida species are opportunistic pathogens responsible for a variety of diseases, ranging from skin and mucosal lesions to severe systemic, life-threatening infections. Candida albicans accounts for more than 70% of all Candida infections, however, the clinical relevance of other species such as Candida parapsilosis and Candida krusei are being increasingly recognized. Biofilm-producing yeasts cells acquire an increased resistance to antifungal agents, often leading to therapeutic failure and chronic infection...
March 6, 2018: FEMS Yeast Research
Lígia de Souza Fernandes, Yuri Martins Amorim, Elton Libério da Silva, Samuel Calixto Silva, Alécia Junia Aparecida Santos, Franciele Natália Peixoto, Luara Moniele Neves Pires, Raquel Yumi Sakamoto, Flávia do Carmo Horta Pinto, Maria Virgínia Costa Scarpa, Marcelo Gonzaga de Freitas Araújo
Owing to the growing resistance among isolates of Candida species to usual antifungal agents and the well-known therapeutic potential of curcumin, the purpose of this study was to develop and validate a vaginal formulation containing this substance and to evaluating its effectiveness in the treatment of experimental vulvovaginal candidiasis METHODS: Curcumin was incorporated in a vaginal cream in three concentrations (0.01, 0.1 and 1.0%). The different concentrations of the cream and its controls were intravaginally administered in an immunosuppressed rat model to evaluate the efficacy in the treatment of experimental vulvovaginal candidiasis...
March 8, 2018: Mycoses
Laura Reisfeld, Cássia Yumi Ikuta, Laura Ippolito, Bruna Silvatti, José Soares Ferreira Neto, José Luiz Catão-Dias, Fernando C W Rosas, José Anselmo Neto, Vera M F da Silva
An adult male Amazonian manatee Trichechus inunguis under human care presented with 3 circular cutaneous lesions on the dorsal aspect of the rostrum and between the nostrils (plenum). Initially these lesions were superficial, hypopigmented, without warmth and non-painful. Microbiological cultures of skin swabs isolated Candida sp. and Pseudomonas aeruginosa, and topical treatment with antiseptic, antifungal, anti-inflammatory and antibiotic medication was instituted. This treatment strategy did not lead to any clinical improvement, and after 6 mo, the lesions progressed to a confluent abscess (5...
March 5, 2018: Diseases of Aquatic Organisms
Vanessa Andreu, Annabel Levert, Anaïs Amiot, Anaïs Cousin, Nicolas Aveline, Cédric Bertrand
Five plant extracts traditionally used in organic and biodynamic farming for pest control and antifungal (downy mildew) disease management were selected after a farmer survey and analyzed for their chemical composition in LC-PDA-MS-MS and using adapted analytical method from food chemistry for determination of class of component (e.g., protein, sugar, lipids…). Their antifungal activity against Penicillium expansum, Botrytis cinerea, Botrytis allii, brown rot causing agents (Monilinia laxa and Monilinia fructigena), and grape downy mildew (Plasmopara viticola) was examined in vitro...
March 7, 2018: Environmental Science and Pollution Research International
Hebat-Allah S Abbas, Somaia S Abd El-Karim, Nayera A M Abdelwahed
The present study investigates, the synthesis of new derivatives of benzenesulfonamide nucleus hybridized with various substituted pyrazole 4, 8 and thiazole ring 6 using 4-amino-N-butylbenzenesulfonamide 1 as the key starting compound. Furthermore, 3,5-diaminopyrazole derivative 10 was allowed to react with different reagents such as an active methylene compounds, ketone dithioacetal, ethoxymethylene malononitrile and cyanoguanidine for a preparation of new benzenesulfonamide derivatives 11-18 conjugated with different substituted hetero-bicyclic ring systems...
May 2017: Acta Poloniae Pharmaceutica
Eman M Mohi El-Deen, Eman K Abd El-Hameed
Synthesis of a series of novel 10-substituted-pyrido[3',2':4,5]thieno[3,2-b] quinoline derivatives 3-15, which contain a planar tetracyclic heteroring system, has been accomplished. The synthetic approaches for the target compounds included, condensation reaction of 10-amino derivatives 2 with triethyl orthoformate to give ethyl N-formimidate derivatives 3, which in turn reacted with different amines to give N-substituted formimidamide derivatives 4a,b. In addition, N-mustard derivative 6 was synthesized via treatment of 2,2'- azanediylbis(ethan-1-ol) derivative 5 with thionyl chloride...
May 2017: Acta Poloniae Pharmaceutica
Ahmad Mourad, John R Perfect
Cryptococcal meningitis is the most common central nervous system infection in the world today. It occurs primarily, but not exclusively, in immunocompromised individuals and despite substantial improvement in management of clinical events like AIDS, the numbers of cases of cryptococcosis remain very high. Unfortunately, despite several antifungal agents available for treatment, morbidity and mortality rates remain high with this fungal infection. In this Review, we will describe the treatments and strategies for success, identify the failures, and provide insights into the future developments / improvements for management...
2018: Memórias do Instituto Oswaldo Cruz
Jennifer E McGill, Andrew S Hanzlicek, Kate S Kukanich, Gary D Norsworthy, Audrey K Cook
Objectives The objective of this study was to determine if urine Histoplasma antigen ( HAg) enzyme immunoassay (EIA) concentrations at the time of diagnosis and prior to the administration of antifungal agents are predictive of outcome for cats infected with Histoplasma capsulatum and to determine if compromised renal function affects urine HAg EIA measurements. Methods Medical records at four institutions were searched to identify cats diagnosed with histoplasmosis between April 2012 and December 2015. Pretreatment urine Histoplasma EIA values were recorded, along with patient signalment, serum creatinine concentration, urine specific gravity, site(s) of infection and survival data...
March 1, 2018: Journal of Feline Medicine and Surgery
Cheng-He Zhou, Ya-Nan Wang, Rammohan R Yadav Bheemanaboina, Wei-Wei Gao, Jie Kang, Gui-Xin Cai
A series of benzimidazole quinolone hybrids as new potential antimicrobial agents were designed and synthesized, and their bioactive assay indicated that some prepared compounds exhibited potent antibacterial and antifungal activities. Notably, 2-fluorobenzyl derivative 5b showed remarkable antimicrobial activities against the resistant P. aeruginosa and C. tropicalis isolated from infected patients. The active molecule 5b could not only rapidly kill the tested strains, but also exhibit low toxicity towards Hep-2 cells...
March 7, 2018: ChemMedChem
Anuoluwa Abimbola Akinsiku, Enock Olugbenga Dare, Kolawole Oluseyi Ajanaku, Olayinka Oyewale Ajani, Joseph Adebisi O Olugbuyiro, Tolutope Oluwasegun Siyanbola, Oluwaseun Ejilude, Moses Eterigho Emetere
In the quest for environmental remediation which involves eco-friendly synthetic routes, we herein report synthesis and modeling of silver nanoparticles (Ag NPs) and silver/nickel allied bimetallic nanoparticles (Ag/Ni NPs) using plant-extract reduction method. Secondary metabolites in the leaf extract of Canna indica acted as reducing agent. Electronic transitions resulted in emergence of surface plasmon resonance in the regions of 416 nm (Ag NPs) and 421 nm (Ag/Ni NPs) during optical measurements. Further characterizations were done using TEM and EDX...
2018: International Journal of Biomaterials
Xiaodong Cui, Jingjing Du, Jiao Li, Zhuanhua Wang
Antimicrobial peptides (AMPs) are known to play important roles in the innate host defense mechanisms of most living organisms. Protease inhibitors from plants potently inhibit the growth of a variety of pathogenic bacteria and fungi. Therefore, there are excellent candidates for the development of novel antimicrobial agents. In this study, an antimicrobial peptide derived from tartary buckwheat seeds (FtAMP) was obtained by gene cloning, expression and purification, which exhibited inhibitory activity toward trypsin...
March 2, 2018: Acta Biochimica et Biophysica Sinica
Yukun Qin, Weixiang Liu, Ronge Xing, Song Liu, Kecheng Li, Pengcheng Li
In this study, 3-methyl-1,2,4-triazolyl chitosan (MTACS) and 3-chloromethyl-1,2,4-triazolyl chitosan (CMTACS) were prepared via cyclization of acyl thiourea chitosan (TUCS). Their structures were confirmed by FT-IR, ¹H-NMR, elemental analysis, DSC, XRD, and SEM. The conformations were predicted using the Gaussian 09 program. Additionally, the antifungal properties of MTACS and CMTACS against Stemphylium solani weber ( S. solani ), Alternaria porri ( A. porri ), and Gloeosporium theae-sinensis ( G. theae-sinensis ) were assayed in vitro and ranged from 250 μg/mL to 1000 μg/mL...
March 6, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Sarah G Whaley, Kelly E Caudle, Lucia Simonicova, Qing Zhang, W Scott Moye-Rowley, P David Rogers
The high prevalence of fluconazole resistance among clinical isolates of Candida glabrata has greatly hampered the utility of fluconazole for the treatment of invasive candidiasis. Fluconazole resistance in this yeast is almost exclusively due to activating mutations in the transcription factor Pdr1, which result in upregulation of the ABC transporter genes CDR1 , PDH1 , and SNQ2 and therefore increased fluconazole efflux. However, the regulation of Pdr1 is poorly understood. In order to identify genes that interact with the Pdr1 transcriptional pathway and influence the susceptibility of C...
January 2018: MSphere
Cristina Lazzarini, Krupanandan Haranahalli, Robert Rieger, Hari Krishna Ananthula, Pankaj B Desai, Alan Ashbaugh, Michael J Linke, Melanie T Cushion, Bela Ruzsicska, John Haley, Iwao Ojima, Maurizio Del Poeta
The incidence of invasive fungal infections has risen dramatically in the past decades. Current antifungal drugs are either toxic, likely to interact with other drugs, have a narrow spectrum of activity or induce fungal resistance. Hence, there is a great need for new antifungals, possibly with novel mechanisms of action. Previously our group reported an acylhydrazone called BHBM that targeted the sphingolipid pathway, and showed strong antifungal activity against several fungi. In this study, we screened 19 derivatives of BHBM...
March 5, 2018: Antimicrobial Agents and Chemotherapy
Rafika Brakni, Monia Ali Ahmed, Pauline Burger, Aurélie Schwing, Grégory Michel, Christelle Pomares, Lillia Hasseine, Laurent Boyer, Xavier Fernandez, Anne Landreau, Thomas Michel
Lichens are complex symbiotic organisms able to produce a vast array of compounds. The Algerian lichen diversity has only prompted little interest even given the 1085 species listed. Herein, the chemodiversity of four Algerian lichens including Cladonia rangiformis, Ramalina farinaceae, R. fastigiata and Roccella phycopsis was investigated. A dereplication strategy, using ultra high performance liquid chromatography-electrospray ionization-high resolution mass-spectrometry (UHPLC-ESI-HRMS/MS), was carried out for a comprehensive characterization of their substances including phenolics, depsides, depsidones, depsones, dibenzofurans and aliphatic acids...
March 5, 2018: Chemistry & Biodiversity
R Biczak, M Turek, B Pawłowska, E Różycka-Sokołowska, B Marciniak, M Deska, P Krupa, I Jatulewicz, J Skalik, P Bałczewski
2,2'-Thiodiacetates with their excellent complexing properties may be used as metal extraction agents, fluorescent and superparamagnetic materials, antibacterial and anticancer medical agents, however there are no data concerning the environmental impact of 2,2'-thiodiacetates derivatives and data definying the potential hazard connected with their use. This study describes the ecotoxicity assessment of seven 2,2'-thiodiacetates with non-metallic, alkyl and aryl ammonium cations, which were obtained in an environmentally friendly, solvent-free syntheses...
February 28, 2018: Ecotoxicology and Environmental Safety
Ferdows Atiq, Edon Hameli, Annoek E C Broers, Jeanette K Doorduijn, Teun Van Gelder, Louise M Andrews, Birgit C P Koch, Jorie Versmissen, Brenda C M de Winter
PURPOSE: Cyclosporine A (CsA) is the most widely used immunosuppressive agent after a hematopoietic stem cell transplantation (HSCT). Although recommendations for CsA dose conversion from intravenous to oral administration differ from 1:1 to 1:3, most studies did not consider the role of azole antifungals as an important confounder. Therefore, we assess the optimal conversion rate of CsA from intravenous to oral administration in HSCT recipients, taking into account the concomitant use of azole antifungals...
March 2, 2018: European Journal of Clinical Pharmacology
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