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https://www.readbyqxmd.com/read/28425125/n-methyl-4-pyridinium-tetrazolate-zwitterion-based-photochromic-materials
#1
Xiang-Yi Chen, Ning-Ning Zhang, Li-Zhen Cai, Pei-Xin Li, Ming-Sheng Wang, Guo-Cong Guo
N,N'-disubstituted bipyridinium (viologen) and N-monosubstituted bipyridinium compounds are well known for their electron-transfer (ET) photochromic behavior. The modification of them was exclusively focused on the N-substituents. For the first time, we studied the photochromic behavior when one pyridyl ring of the bipyridinium was substituted with a multi-functional azole group, and revealed that two new coordination compounds based on N-methyl-4-pyridinium tetrazolate (mptz) zwitterion, [Zn(mptz)2Br2] (1) and [Cd3(mptz)2Cl6]n∙4nH2O (2), exhibit typical ET photochromic behavior owing to photoinduced ET from halogen anion to the mptz ligand...
April 20, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28424474/molecular-epidemiology-and-azole-resistance-mechanism-study-of-candida-guilliermondii-from-a-chinese-surveillance-system
#2
Jing-Wei Cheng, Kang Liao, Timothy Kudinha, Shu-Ying Yu, Meng Xiao, He Wang, Fanrong Kong, Ying-Chun Xu
We studied the molecular epidemiology and mechanism of azole resistance of 164 C. guilliermondii isolates from a nationwide multi-center surveillance program. The isolates were identified by ITS gene sequencing, and the in vitro susceptibility to fluconazole and voriconazole was determined by broth microdilution method. The 14-α-demethylase gene ERG11 was amplified and sequenced, and microsatellite analysis was performed to study the genetic relatedness of the isolates. Amongst the 164 C. guilliermondii isolates, 15 (9...
April 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28421758/copper-ii-mediated-chelation-assisted-regioselective-n-naphthylation-of-indoles-pyrazoles-and-pyrrole-through-dehydrogenative-cross-coupling
#3
Sourav Pradhan, Pinaki Bhusan De, Tharmalingam Punniyamurthy
A copper-mediated picolinamide directed regioselective cross-coupling of naphthylamines with azoles is developed via C-H functionalization and C-N bond formation. The reaction of indoles leads to the formation of chiral C-N cross-coupled products with functional group tolerance. These reaction conditions can also be extended to the cross-coupling of pyrazole and pyrrole scaffolds.
April 19, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28417524/biofilms-of-candida-spp-from-the-ocular-conjunctiva-of-horses-with-reduced-azole-susceptibility-a-complicating-factor-for-the-treatment-of-keratomycosis
#4
Raimunda Sâmia Nogueira Brilhante, Paula Vago Bittencourt, Débora de Souza Collares Castelo-Branco, Glaucia Morgana de Melo Guedes, Jonathas Sales de Oliveira, Lucas Pereira Alencar, Rossana de Aguiar Cordeiro, Mariana Pinheiro, Evilázio Fernandes Nogueira-Filho, Waldemiro de Aquino Pereira-Neto, José Júlio Costa Sidrim, Marcos Fábio Gadelha Rocha
OBJECTIVES: This study aimed to assess the biofilm-forming ability of Candida spp. from the ocular conjunctiva of horses and to investigate the antifungal susceptibility of these biofilms. PROCEDURES: Initially, the biofilm-forming ability of 15 strains was assessed by crystal violet staining, which reveals the fungal biomass adhered to the polystyrene plates, and scanning electron microscopy. Then, the minimum inhibitory concentrations (MICs) of amphotericin B, fluconazole, itraconazole, and caspofungin were initially determined against strains in planktonic form...
April 18, 2017: Veterinary Ophthalmology
https://www.readbyqxmd.com/read/28416540/in-vivo-efficacy-of-liposomal-amphotericin-b-against-wild-type-and-azole-resistant-aspergillus-fumigatus-isolates-in-two-different-immunosuppressed-models-of-invasive-aspergillosis
#5
Seyedmojtaba Seyedmousavi, Johan W Mouton, Willem J G Melchers, Paul E Verweij
Using an immunocompetent murine model of invasive aspergillosis (IA), we previously reported (AAC, 2013, 57, 4, 1866-1871) that the efficacy of liposomal amphotericin B (L-AmB) is not hampered by the presence of azole resistance mutations in Aspergillus fumigatus We here investigated the role of immune suppression, i.e. neutropenic and steroid-treated, on L-AmB efficacy in mice infected with a wild type (WT) and azole-resistant Aspergillus fumigatus harboring TR34/L98H mutation in cyp-51A gene.Survival of treated animals at day 14 in both immunosuppressed models was significantly better than that of non-treated controls...
April 17, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28416538/susceptibility-testing-of-common-and-uncommon-aspergillus-species-against-posaconazole-and-other-mold-active-antifungal-azoles-using-the-sensititre-method
#6
Enrica Mello, Brunella Posteraro, Antonietta Vella, Elena De Carolis, Riccardo Torelli, Tiziana D'Inzeo, Paul E Verweij, Maurizio Sanguinetti
We tested 59 common and 27 uncommon Aspergillus species isolates for the susceptibility to the mold-active azole antifungal agents, itraconazole, voriconazole, and posaconazole, using the Sensititre method. The overall essential agreement with the CLSI reference method was 96.5% for itraconazole and posaconazole, and 100% for voriconazole. By Sensititre, as well as CLSI, all of 10 A. fumigatus isolates with a cyp51 mutant genotype were classified as being non-wild-type (MIC > ECV) to triazoles.
April 17, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28409094/successful-treatment-of-azole-resistant-invasive-aspergillosis-in-a-bottlenose-dolphin-with-high-dose-posaconazole
#7
Paulien E Bunskoek, Seyedmojtaba Seyedmousavi, Steven J M Gans, Peter B J van Vierzen, Willem J G Melchers, Cornelis E van Elk, Johan W Mouton, Paul E Verweij
Invasive aspergillosis due to azole-resistant Aspergillus fumigatus is difficult to manage. We describe a case of azole-resistant invasive aspergillosis in a female bottlenose dolphin, who failed to respond to voriconazole and posaconazole therapy. As intravenous therapy was precluded, high dose posaconazole was initiated aimed at achieving trough levels exceeding 3 mg/l. Posaconazole serum levels of 3-9.5 mg/l were achieved without significant side-effects. Follow-up bronchoscopy and computed tomography showed complete resolution of the lesions...
June 2017: Medical Mycology Case Reports
https://www.readbyqxmd.com/read/28404678/antifungal-susceptibility-testing-of-aspergillus-spp-by-using-a-cci-based-maldi-tof-ms-method-appears-to-not-offer-benefit-over-the-traditional-broth-microdilution-testing
#8
Melissa R Gitman, Lisa McTaggart, Joanna Spinato, Rahgavi Poopalarajah, Erin Lister, Shahid Husain, Julianne V Kus
Aspergillus spp. cause serious invasive lung infections and Aspergillus fumigatus is the most commonly encountered clinically significant species. Voriconazole is considered to be the drug of choice for A. fumigatus infections, however rising resistance rates have been reported. We evaluated a MALDI-ToF MS-based method for the differentiation between wild type and non-wild type isolates of 20 Aspergillus spp. (including 3 isolates 2 A. ustus, and 1 A. calidoustus that were used as controls due their intrinsic low azole susceptibility with respect to the in vitro response to voriconazole)...
April 12, 2017: Journal of Clinical Microbiology
https://www.readbyqxmd.com/read/28400291/unmet-clinical-needs-in-the-treatment-of-systemic-fungal-infections-the-role-of-amphotericin-b-and-drug-targeting
#9
Raquel Fernández-García, Esther de Pablo, María Paloma Ballesteros, Dolores R Serrano
Recently an increase in both the prevalence and incidence of invasive fungal infections have been reported. The number of fungal species that can cause systemic mycoses are higher and current antifungal therapies are still far from ideal. The emergence of antifungal resistances has a major clinical impact when using azoles and echinocandins leading to possible treatment failure and ultimately putting the patient's life at risk. Amphotericin B can play a key role in treating severe invasive mycoses as the incidence of antifungal resistance is very low combined with a high efficacy against a wide range of fungi...
April 8, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28395217/novel-alkylated-azoles-as-potent-antifungals
#10
Sanjib K Shrestha, Atefeh Garzan, Sylvie Garneau-Tsodikova
Fluconazole (FLC) is the drug of choice when it comes to treat fungal infections such as invasive candidiasis in humans. However, the widespread use of FLC has resulted in the development of resistance to this drug in various fungal strains and, simultaneously has occasioned the need for new antifungal agents. Herein, we report the synthesis of 27 new FLC derivatives along with their antifungal activity against a panel of 13 clinically relevant fungal strains. We also explore their toxicity against mammalian cells, their hemolytic activity, as well as their mechanism of action...
March 31, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28393697/targeting-malassezia-species-for-novel-synthetic-and-natural-antidandruff-agents
#11
Letizia Angiolella, Simone Carradori, Cristina Maccallini, Gustavo Giusiano, Claudiu T Supuran
Malassezia spp. are lipophilic yeasts not only present in the normal skin microflora, but also responsible of skin-related diseases (pityriasis versicolor, seborrheic/atopic dermatitis and dandruff) as well as systemic fungal infections in humans and animals. Their treatment and eradication are mainly based on old azole drugs, which are characterized by poor compliance, unpredictable clinical efficacy, emerging resistance and several side effects. These drawbacks have prompted the research toward novel synthetic and natural derivatives/nanomaterials targeting other pivotal enzymes/pathways such as carbonic anhydrase (MgCA) and lipases, alone or in combination, in order to improve the eradication rate of this fungus...
April 4, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28387506/interaction-of-azole-based-environmental-pollutants-with-the-coelomic-hemoglobin-from-amphitrite-ornata-a-molecular-basis-for-toxicity
#12
Nikolette L McCombs, Tadeo Moreno-Chicano, Leiah M Carey, Stefan Franzen, Michael A Hough, Reza A Ghiladi
The toxicities of azole pollutants that have widespread agricultural and industrial uses are either poorly understood or unknown, particularly with respect to how infaunal organisms are impacted by this class of persistent organic pollutant. To identify a molecular basis by which azole compounds may have unforeseen toxicity on marine annelids, we examine here their impact on the multifunctional dehaloperoxidase (DHP) hemoglobin from the terebellid polychaete Amphitrite ornata. Ultraviolet-visible and resonance Raman spectroscopic studies showed an increase in the six-coordinate low-spin heme population in DHP isoenzyme B upon binding of imidazole, benzotriazole, and benzimidazole (Kd values of 52, 82, and 110 μM, respectively), suggestive of their direct binding to the heme-Fe...
April 19, 2017: Biochemistry
https://www.readbyqxmd.com/read/28383050/the-global-regulator-ncb2-escapes-from-the-core-promoter-and-impacts-transcription-in-response-to-drug-stress-in-candida-albicans
#13
Mohd Shariq, Sanjiveeni Dhamgaye, Remya Nair, Neha Goyal, Vaibhav Jain, Arnab Mukhopadhyay, Alok K Mondal, Gauranga Mukhopadhyay, Rajendra Prasad
Ncb2, the β subunit of NC2 complex, a heterodimeric regulator of transcription was earlier shown to be involved in the activated transcription of CDR1 gene in azole resistant isolate (AR) of Candida albicans. This study examines its genome-wide role by profiling Ncb2 occupancy between genetically matched pair of azole sensitive (AS) and AR clinical isolates. A comparison of Ncb2 recruitment between the two isolates displayed that 29 genes had higher promoter occupancy of Ncb2 in the AR isolate. Additionally, a host of genes exhibited exclusive occupancy of Ncb2 at promoters of either AR or AS isolate...
April 6, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28382028/notable-increasing-trend-in-azole-non-susceptible-candida-tropicalis-causing-invasive-candidiasis-in-china-august-2009-to-july-2014-molecular-epidemiology-and-clinical-azole-consumption
#14
Xin Fan, Meng Xiao, Kang Liao, Timothy Kudinha, He Wang, Li Zhang, Xin Hou, Fanrong Kong, Ying-Chun Xu
Objectives: To report the notable increasing trends of C. tropicalis antifungal resistance in the past 5 years, and explore molecular epidemiology, and the relationship between clinical azoles consumption and increased resistance rate. Methods: Between August 2009 and July 2014, 507 non-duplicated C. tropicalis isolates causing invasive candidiasis were collected from 10 hospitals in China. The in vitro antifungal susceptibility of nine common agents was determined by Sensititre YeastOne™ using current available species-specific clinical breakpoint (CBPs) or epidemiological cut-off values (ECVs)...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28381607/antifungal-susceptibility-testing-of-malassezia-spp-with-an-optimized-colorimetric-broth-microdilution-method
#15
Cheryl Leong, Antonino Buttafuoco, Martin Glatz, Philipp P Bosshard
Malassezia is a genus of lipid dependent yeasts. It is associated with common skin diseases such as pityriasis versicolor or atopic dermatitis and can cause systemic infections in immunocompromised individuals. Owing to slow growth and lipid requirements of these fastidious yeasts, convenient and reliable antifungal drug susceptibility testing assays for Malassezia spp. are not widely available. We have therefore optimized a broth microdilution assay for the testing of Malassezia that is based on the assays from CLSI and EUCAST for Candida and other yeasts...
April 5, 2017: Journal of Clinical Microbiology
https://www.readbyqxmd.com/read/28379304/changes-in-in-vitro-susceptibility-patterns-of-aspergillus-to-triazoles-and-correlation-with-aspergillosis-outcome-in-a-tertiary-care-cancer-center-1999-2015
#16
Sang Taek Heo, Alexander M Tatara, Cristina Jiménez-Ortigosa, Ying Jiang, Russell E Lewis, Jeffrey Tarrand, Frank Tverdek, Nathaniel D Albert, Paul E Verweij, Jacques F Meis, Antonios G Mikos, David S Perlin, Dimitrios P Kontoyiannis
Background.: Azole-resistant aspergillosis in high risk patients with hematological malignancy or hematopoietic stem cell transplantation (HSCT) is a cause of concern. Methods.: We examined changes over time in triazole MICs (CLSI method) of 290 sequential Aspergillus isolates recovered from respiratory sources from 1999-2002 (before introduction of the Aspergillus-potent triazoles voriconazole and posaconazole) and 2003-2015 at MD Anderson Cancer Center. We also tested for polymorphisms in ergosterol biosynthetic genes (cyp51A, erg3C, erg1) in the 37 A...
March 31, 2017: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/28378358/effects-of-n-oxidation-on-heteroaromatic-macrocycles-synthesis-electronic-structures-and-near-ir-properties-reactivities-of-tetraazaporphyrin-meso-n-oxides
#17
Naoyuki Toriumi, Shunsuke Yanagi, Atsuya Muranaka, Daisuke Hashizume, Masanobu Uchiyama
Heteroaromatic N-oxides such as pyridine and quinoline N-oxides are well studied in organic chemistry, and N-oxide formation has long been utilized for tuning the reactivities of heteroaromatics. However, the scope of aromatic N-oxidation is still restricted to relatively small azine or azole skeletons, and there has been little investigation of the photophysical/chemical effects of N-oxidation on larger heteroaromatic systems. Here, we report synthesis and unique properties of novel macrocyclic heteroaromatic N-oxides, tetraazaporphyrin (TAP) meso-N-oxides...
April 5, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28376640/antimicrobial-activity-of-buchenavia-tetraphylla-against-candida-albicans-strains-isolated-from-vaginal-secretions
#18
José Robson Neves Cavalcanti Filho, Tiago Fonseca Silva, Woah Queiroz Nobre, Larissa Isabela Oliveira de Souza, Cristiane Santos Silva E Silva Figueiredo, Regina Celia Bressan Queiroz de Figueiredo, Norma Buarque de Gusmão, Márcia Vanusa Silva, Luís Cláudio Nascimento da Silva, Maria Tereza Dos Santos Correia
CONTEXT: Buchenavia tetraphylla (Aubl.) RA Howard (Combretaceae: Combretoideae) is an ethnomedicinal plant with reported antifungal action. OBJECTIVE: This study evaluates the antimicrobial activity of B. tetraphylla leaf extracts against clinical isolates of Candida albicans. The morphological alterations, combinatory effects with fluconazole and the cytotoxicity of the active extract were analyzed. MATERIALS AND METHODS: Extracts were obtained using different solvents (hexane: BTHE; chloroform: BTCE; ethyl acetate: BTEE; and methanol: BTME)...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28376618/cage-confinement-pyrolysis-route-to-ultrasmall-tungsten-carbide-nanoparticles-for-efficient-electrocatalytic-hydrogen-evolution
#19
Yan-Tong Xu, Xiaofen Xiao, Zi-Ming Ye, Shenlong Zhao, Rongan Shen, Chun-Ting He, Jie-Peng Zhang, Yadong Li, Xiao-Ming Chen
The size-controlled synthesis of ultrasmall metal-based catalysts is of vital importance for chemical conversion technologies. Here, a cage-confinement pyrolysis strategy is presented for the synthesis of ultrasmall tungsten carbide nanoclusters/nanoparticles. An RHO type zeolitic metal azolate framework MAF-6, possessing large nanocages and small apertures, is selected to confine the metal source W(CO)6. High temperature pyrolysis gives tungsten carbide nanoclusters/nanoparticles with sizes ca. 2 nm, which can serve as an excellent electrocatalyst for the hydrogen evolution reaction...
April 10, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28373148/evaluation-of-the-in-vitro-activity-of-isavuconazole-and-comparator-voriconazole-against-2635-contemporary-clinical-candida-and-aspergillus-isolates
#20
K M T Astvad, R K Hare, M C Arendrup
OBJECTIVE: The in vitro activity of isavuconazole was determined for 1677 Candida and 958 Aspergillus isolates from 2012-2014 with voriconazole as comparator. METHODS: Aspergillus isolates were screened for resistance using azole-agar. Screening positive Aspergillus and all Candida isolates underwent EUCAST broth-microdilution testing. Isolates were categorised as wild-type (wt) or non-wt, adopting EUCAST ECOFFs (where available) or wt upper limits (wtULs; two 2-fold dilutions above the MIC50)...
March 31, 2017: Clinical Microbiology and Infection
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