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https://www.readbyqxmd.com/read/28637041/the-effects-of-fungicides-on-human-3%C3%AE-hydroxysteroid-dehydrogenase-1-and-aromatase-in-human-placental-cell-line-jeg-3
#1
Shuyan Cao, Leping Ye, Ying Wu, Baiping Mao, Lanlan Chen, Xiudi Wang, Ping Huang, Ying Su, Ren-Shan Ge
Placenta secretes a large amount of progesterone and estradiol, which are critical for maintaining pregnancy. In human placenta, 3β-hydroxysteroid dehydrogenase 1 (HSD3B1) catalyzes pregnenolone to form progesterone, and aromatase (CYP19A1) catalyzes testosterone into estradiol. Fungicides display antifungal activities and are widely used to prevent fungal infections in agricultural plants. These chemicals include azoles, such as tebuconazole (TEB), triadimefon (TRI), and vinclozolin (VCZ) or organotins, such as tributyltin (TBT) and tetrabutyltin (TTBT)...
June 22, 2017: Pharmacology
https://www.readbyqxmd.com/read/28636889/complications-of-hematopoietic-stem-transplantation-fungal-infections
#2
REVIEW
Ali S Omrani, Reem S Almaghrabi
Patients undergoing allogeneic hematopoietic stem cell transplantation (HSCT) are at increased risk of invasive fungal infections, especially during the early neutropenic phase and severe graft-versus-host disease. Mold-active prophylaxis should be limited to the highest risk groups. Empiric antifungal therapy for HSCT with persistent febrile neutropenia is associated with unacceptable response rates, unnecessary antifungal therapy, increased risk of toxicity, and inflated costs. Empiric therapy should not be a substitute for detailed work up to identify the cause of fever in such patients...
June 13, 2017: Hematology/oncology and Stem Cell Therapy
https://www.readbyqxmd.com/read/28630940/fluconazole-induced-ploidy-change-in-cryptococcus-neoformans-results-from-the-uncoupling-of-cell-growth-and-nuclear-division
#3
Sophie Altamirano, Diana Fang, Charles Simmons, Shreyas Sridhar, Peipei Wu, Kaustuv Sanyal, Lukasz Kozubowski
Cryptococcus neoformans is a pathogenic yeast that causes lethal cryptococcal meningitis in immunocompromised patients. One of the challenges in treating cryptococcosis is the development of resistance to azole antifungals. Previous studies linked azole resistance to elevated numbers of copies of critical resistance genes in aneuploid cells. However, how aneuploidy is formed in the presence of azole drugs remains unclear. This study showed that treatment with inhibitory concentrations of an azole drug, fluconazole (FLC), resulted in a significant population of cells with increased DNA content, through the following defects: inhibition of budding, premature mitosis, and inhibition of cytokinesis followed by replication in the mother cell...
May 2017: MSphere
https://www.readbyqxmd.com/read/28630186/loss-of-c-5-sterol-desaturase-activity-results-in-increased-resistance-to-azole-and-echinocandin-antifungals-in-a-clinical-isolate-of-candida-parapsilosis
#4
Jeffrey M Rybak, C Michael Dickens, Josie E Parker, Kelly Caudle, Kayihura Manigaba, Sarah G Whaley, Andrew Nishimoto, Arturo Luna-Tapia, Sujoy Roy, Qing Zhang, Katherine S Barker, Glen E Palmer, Thomas R Sutter, Ramin Homayouni, Nathan P Wiederhold, Steven L Kelly, P David Rogers
Among emerging non-albicans Candida species, C. parapsilosis is of particular concern as a cause of nosocomial bloodstream infections in neonatal and intensive care unit patients. While fluconazole and echinocandins are considered effective treatment of such infections, recent reports of fluconazole and echinocandin resistance in C. parapsilosis indicate a growing problem. The present study describes a novel mechanism of antifungal resistance in this organism affecting the susceptibility of azole and echinocandin antifungals in a clinical isolate obtained from a patient with prosthetic valve endocarditis...
June 19, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28626746/frequency-of-cutaneous-fungal-infections-and-azole-resistance-of-the-isolates-in-patients-with-diabetes-mellitus
#5
Omid Raiesi, Mansour Siavash, Faezeh Mohammadi, Javaher Chabavizadeh, Behzad Mahaki, Mehrnoush Maherolnaghsh, Parvin Dehghan
BACKGROUND: Diabetic patients are more susceptible to cutaneous fungal infections. The higher blood sugar levels cause increasing the cutaneous fungal infections in these patients. The main objective of this study was to find the frequency of fungal infections among cutaneous lesions of diabetic patients and to investigate azole antifungal agent susceptibility of the isolates. MATERIALS AND METHODS: In this study, type 1diabetes (n = 78) and type 2 diabetes (n = 44) comprised 47 cases (38...
2017: Advanced Biomedical Research
https://www.readbyqxmd.com/read/28622580/combating-breast-cancer-with-non-steroidal-aromatase-inhibitors-nsais-understanding-the-chemico-biological-interactions-through-comparative-sar-qsar-study
#6
REVIEW
Nilanjan Adhikari, Sk Abdul Amin, Achintya Saha, Tarun Jha
It is a challenging task to design target-specific and less toxic non-steroidal aromatase inhibitors (NSAIs) though the modeling studies for designing anti-aromatase molecules have been continuing for more than two decades to fight the dreaded estrogen-dependent breast cancer. In this article, different validated QSAR models are developed and analyzed to understand important physicochemical and structural parameters modulating the aromatase inhibitory activity of NSAIs. Physicochemical properties such as molar refractivity and dipole moment are found to be the most important parameters for controlling aromatase inhibition...
May 30, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28620958/a-network-meta-analysis-of-primary-prophylaxis-for-invasive-fungal-infection-in-haematological-patients
#7
REVIEW
L P Leonart, F S Tonin, V L Ferreira, S T S Penteado, A Wiens, F A Motta, R Pontarolo
WHAT IS KNOWN AND OBJECTIVE: Antifungal prophylaxis is an option to reduce the incidence of invasive fungal infection (IFI) in haematological patients. To date, no network meta-analysis (NMA) of high-quality evidence (double-blind randomized controlled trials) has been performed on this subject. This systematic review and NMA aimed to evaluate the safety and efficacy of different antifungal agents used for prophylaxis of IFI in patients with haematological disorders. METHODS: A systematic review was performed according to PRISMA and Cochrane recommendations...
June 15, 2017: Journal of Clinical Pharmacy and Therapeutics
https://www.readbyqxmd.com/read/28620845/cross-resistance-between-voriconazole-and-fluconazole-for-non-albicans-candida-infection-a-case-case-control-study
#8
Y Wang, Q Yang, L Chen, L Liu, R Hao, T Zhang, X Wang, J Lei, J Xie, Y Dong
Cross-resistance (CR) between voriconazole and fluconazole for non-albicans Candida (NAC) species is not uncommon, but little is known about the risk factors and clinical consequences associated with this resistance phenotype. A case-case-control study was performed at a university-affiliated hospital in China between November 2012 and April 2016. The two case groups respectively comprised patients with a mono-resistance (MR) NAC infection (fluconazole or voriconazole resistance) and patients with a CR NAC infection (fluconazole and voriconazole resistance)...
June 15, 2017: European Journal of Clinical Microbiology & Infectious Diseases
https://www.readbyqxmd.com/read/28618155/clinical-outcome-of-cystic-fibrosis-patients-colonized-by-scedosporium-species-following-lung-transplantation-a-single-center-15-year-experience
#9
Perrine Parize, Veronique Boussaud, Vianney Poinsignon, Emilie Sitterlé, Francoise Botterel, Sandrine Lefeuvre, Romain Guillemain, Eric Dannaoui, Elaine M Billaud
BACKGROUND: Fungi of the genus Scedosporium are emerging pathogens responsible for severe infections in lung transplant recipients. These infections are associated with poor prognosis and some centers consider now Scedosporium species colonization as a contraindication to lung transplantation (LT) even though no published evidence demonstrates that Scedosporium species colonization is associated with higher morbidity or mortality after LT. METHODS: Here we aim to describe characteristics and outcome of cystic fibrosis (CF) lung transplant recipients colonized with Scedosporium species in a single center over a 15-year period...
June 15, 2017: Transplant Infectious Disease: An Official Journal of the Transplantation Society
https://www.readbyqxmd.com/read/28613342/a-novel-metal-free-amidosulfenylation-of-alkenes-leading-to-%C3%AE-azolyl-sulfides
#10
Kai Sun, Yunhe Lv, Zuodong Shi, Shiqiang Mu, Changhao Li, Xin Wang
A novel and environmentally benign method for C-S and C-N bond formation by the direct amidosulfenylation of alkenes has been developed under metal-free conditions. Various alkenes and azoles were transformed into the corresponding β-azolyl sulfides in ionic liquids. The wide substrate scope, good functional group tolerance, and ease of operation make this reaction attractive for the synthesis of nitrogen- and sulfur-containing molecules.
June 14, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28613336/visible-light-mediated-c3-azolylation-of-imidazo-1-2-a-pyridines-with-2-bromoazoles
#11
Qing Chang, Zhongjie Wu, Lu Yu, Ping Liu, Peipei Sun
The C3-azolylation of imidazo[1,2-a]pyridines was developed via a visible light-mediated reaction of imidazopyridines with 2-bromoazoles catalyzed by Ir(ppy)2(dtbbpy)PF6 under mild conditions. For the imidazo[1,2-a]pyridines with various substituents on benzene or the pyridine ring and a variety of azoles, the reaction proceeded smoothly to give 3-(azol-2-yl)imidazo[1,2-a]pyridines in moderate to good yields.
June 14, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28612071/palladium-catalyzed-intermolecular-carbonylative-cross-coupling-of-heteroaryl-c-sp-2-h-bonds-with-amines-an-efficient-strategy-for-oxidative-aminocarbonylation-of-azoles
#12
Qi Xing, Hui Lv, Chungu Xia, Fuwei Li
An efficient palladium-catalyzed oxidative aminocarbonylation of azoles has been developed. This system allows for intermolecular carbonylative cross-coupling of aromatic C(sp(2))-H bonds with simple amines, which has often been asked for, but has not been realized so far. It provides a straightforward approach to a variety of azol-2-amides.
June 14, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28607016/drug-sensitivity-and-resistance-mechanism-in-aspergillus-section-nigri-strains-from-japan
#13
Aki Hashimoto, Daisuke Hagiwara, Akira Watanabe, Maki Yahiro, Alimu Yikelamu, Takashi Yaguchi, Katsuhiko Kamei
Aspergillus niger and its related species, known as Aspergillus section Nigri, are ubiquitously distributed across the globe and are often isolated from clinical specimens. In Japan, Aspergillus section Nigri is the second-most often isolated from clinical specimens following A. fumigatus. We determined the species of Aspergillus section Nigri isolated in Japan by DNA sequencing of partial β-tubulin genes and investigated drug susceptibility by CLSI M38-A2 method. The collection contained 20 A. niger, 59 A...
June 12, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28605488/in-vitro-activity-of-the-novel-antifungal-compound-f901318-against-difficult-to-treat-aspergillus-isolates
#14
J B Buil, A J M M Rijs, J F Meis, M Birch, D Law, W J G Melchers, P E Verweij
Background: F901318 is a new antifungal agent with a novel mechanism of action with activity against Aspergillus species. We investigated the in vitro activity of F901318 against a collection of Aspergillus isolates. Methods: A total of 213 Aspergillus isolates were used in this study. A total of 143 Aspergillus fumigatus sensu stricto isolates were used, of which 133 were azole resistant [25 TR 34 /L98H; 25 TR 46 /Y121F/T289A; 33 A. fumigatus with cyp51A -associated point mutations (25 G54, 1 G432 and 7 M220); and 50 azole-resistant A...
June 10, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28597967/anidulafungin-for-the-treatment-of-candidaemia-caused-by-candida-parapsilosis-analysis-of-pooled-data-from-six-prospective-clinical-studies
#15
Dimitrios P Kontoyiannis, Matteo Bassetti, Marcio Nucci, Maria Rita Capparella, Jean L Yan, Jalal Aram, Patricia A Hogan
Concerns with echinocandin use for infections caused by Candida parapsilosis complex species have driven the need for data to support echinocandin clinical efficacy in such patients. Data from six prospective studies were pooled to assess efficacy and safety of anidulafungin in patients with candidaemia caused by C. parapsilosis. Patient-level data were pooled from patients with microbiologically confirmed candidaemia due to C. parapsilosis treated with anidulafungin. Patients received a 200 mg intravenous (IV) loading dose of anidulafungin (day 1) and 100 mg daily thereafter...
June 9, 2017: Mycoses
https://www.readbyqxmd.com/read/28595940/glabridin-triggers-over-expression-of-mca1-and-nuc1-genes-in-candida-glabrata-is-it-an-apoptosis-inducer
#16
M Moazeni, M T Hedayati, M Nabili, S J Mousavi, A Abdollahi Gohar, S Gholami
The growing trends of emergence of antifungal-resistant Candida strains has recently been inspired the researchers to design new antifungal agents with novel mechanisms of action. Glabridin is an originally natural substrate with multiple biological activities which propose it as a novel anticancer, antimicrobial and antifungal agent. In the present study, the antifungal effect of glabridin against Candida glabrata isolates and its possible mechanism of action were investigated. The minimum inhibitory concentrations (MIC) for glabridin against fluconazole-resistant and fluconazole-SDD strains of C...
June 5, 2017: Journal de Mycologie Médicale
https://www.readbyqxmd.com/read/28593476/synergy-between-azoles-and-1-4-dihydropyridine-derivative-as-an-option-to-control-fungal-infections
#17
Zuzana Ježíková, Tomáš Pagáč, Barbora Pfeiferová, Helena Bujdáková, Stanislava Dižová, Iva Jančíková, Dana Gášková, Petra Olejníková
With emerging fungal infections and developing resistance, there is a need for understanding the mechanisms of resistance as well as its clinical impact while planning the treatment strategies. Several approaches could be taken to overcome the problems arising from the management of fungal diseases. Besides the discovery of novel effective agents, one realistic alternative is to enhance the activity of existing agents. This strategy could be achieved by combining existing antifungal agents with other bioactive substances with known activity profiles (combination therapy)...
June 7, 2017: Antonie Van Leeuwenhoek
https://www.readbyqxmd.com/read/28591186/increasing-incidence-of-mucormycosis-in-a-large-spanish-hospital-from-2007-to-2015-epidemiology-and-microbiological-characterization-of-the-isolates
#18
Jesús Guinea, Pilar Escribano, Antonio Vena, Patricia Muñoz, María Del Carmen Martínez-Jiménez, Belén Padilla, Emilio Bouza
We studied 19 cases of proven/probable mucormycosis diagnosed from 2007 to 2015 in our hospital and assessed the microbiological characteristics of the isolates. We recorded the incidence of mucormycosis and clinical and microbiological data of infected patients. Isolates were identified to molecular level and tested for their antifungal susceptibility to azoles, amphotericin B, and liposomal amphotericin B according to the CLSI M-38 A2 procedure. The incidence of mucormycosis in cases/100,000 hospital admissions during 2007-2015 increased significantly with respect to that reported in 1988-2006 (3...
2017: PloS One
https://www.readbyqxmd.com/read/28590071/synthesis-and-characterization-of-nitro-trinitromethyl-and-fluorodinitromethyl-substituted-triazolyl-and-tetrazolyl-trihydridoborate-anions
#19
Guillaume Belanger-Chabot, Max Kaplan, Piyush Deokar, Norbert Szimhardt, Ralf Haiges, Karl O Christe
The problem of preparing energetic, exclusively mono-azolyl substituted hydridoborate anions in high yield and purity from [BH4]- and nitroazoles by hydrogen elimination was overcome by reacting the corresponding nitroazolate anions with the BH3 adducts BH3·S(CH3)2 or BH3·THF. The highly-energetic, nitro-, trinitromethyl-, and fluorodinitromethyl- substituted triazolyl- and tetrazolyl-trihydridoborate anions were synthesized in this manner and characterized by vibrational and multinuclear NMR spectroscopy and their crystal structures...
June 7, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28589197/coordination-strategy-induced-selective-c-h-amination-of-8-aminoquinolines
#20
Hong Yi, Hong Chen, Changliang Bian, Zilu Tang, Atul K Singh, Xiaotian Qi, Xiaoyu Yue, Yu Lan, Jyh-Fu Lee, Aiwen Lei
In this study, we broke through the directing function of the amide group. The coordination interaction between metal and directing-group enhanced the reactivity of the substrate. Using this strategy, we realized the selective amination of 8-aminoquinolines at the C5 position via employing azoles as the source of amine. Various kinds of 8-aminoquinolines and different substituted azoles were compatible to afford the corresponding C-N coupling products.
June 7, 2017: Chemical Communications: Chem Comm
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