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https://www.readbyqxmd.com/read/29784014/unintentional-sulfonylurea-toxicity-due-to-a-drug-drug-interaction-a-case-report
#1
Keith Gunaratne, Emily Austin, Peter E Wu
BACKGROUND: Sulfonylureas are widely used for type 2 diabetes mellitus, but these medications carry a risk of hypoglycemia. Drug-drug interactions that inhibit sulfonylurea metabolism and thus increase systemic exposure can cause unintentional sulfonylurea toxicity. CASE PRESENTATION: A 56-year-old man presented with severe, recurrent hypoglycemia. He had a history of type 2 diabetes mellitus and was taking the sulfonylurea gliclazide with no prior episodes of hypoglycemia...
May 21, 2018: BMC Research Notes
https://www.readbyqxmd.com/read/29783634/novel-structural-insight-into-inhibitors-of-heme-oxygenase-1-ho-1-by-new-imidazole-based-compounds-biochemical-and-in-vitro-anticancer-activity-evaluation
#2
Khaled F Greish, Loredana Salerno, Reem Al Zahrani, Emanuele Amata, Maria N Modica, Giuseppe Romeo, Agostino Marrazzo, Orazio Prezzavento, Valeria Sorrenti, Antonio Rescifina, Giuseppe Floresta, Sebastiano Intagliata, Valeria Pittalà
In this paper, the design, synthesis, and molecular modeling of a new azole-based HO-1 inhibitors was reported, using compound 1 as a lead compound, in which an imidazole moiety is linked to a hydrophobic group by means of an ethanolic spacer. The tested compounds showed a good inhibitor activity and possessed IC50 values in the micromolar range. These results were obtained by targeting the hydrophobic western region. Molecular modeling studies confirmed a consolidated binding mode in which the nitrogen of the imidazolyl moiety coordinated the heme ferrous iron, meanwhile the hydrophobic groups were located in the western region of HO-1 binding pocket...
May 18, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29780467/computational-evaluation-of-metal-pentazolate-frameworks-inorganic-analogues-of-azolate-metal-organic-frameworks
#3
Mihails Arhangelskis, Athanassios D Katsenis, Andrew J Morris, Tomislav Friščić
Pentazolate is the ultimate all-nitrogen, inorganic member of the azolate series of aromatic 5-membered ring anions. As an azolate ligand, it has the potential to form open framework structures with metal ions, that would be inorganic analogues of azolate metal-organic frameworks formed by its congeners. However, while the low stability and elusive nature of the pentazolate ion have so far prevented the synthesis of such frameworks, computational studies have focused on pentazolate exclusively as a ligand that would form discrete metallocene structures...
April 7, 2018: Chemical Science
https://www.readbyqxmd.com/read/29778564/simultaneous-quantification-of-systemic-azoles-and-their-major-metabolites-in-human-serum-by-hplc-pda-role-of-azole-metabolic-rate
#4
Alicia Gomez-Lopez, Laura Alcazar-Fuoli, Leticia Bernal-Martínez
We describe the development and validation of a novel liquid chromatography assay (HPLC/PDA) for simultaneous quantification of voriconazole, itraconazole, and posaconazole, as well as some of their major metabolites, voriconazole N-oxide and hydroxy-itraconazole, in human serum. Analytes were detected using a PDA system that allows the characterization of the specific UV spectra of each compound. The assay exhibited linearity between 0.25-16 mg/L for all the compounds tested. The accuracy and within- and between-day precision of the assay were in acceptable ranges...
April 14, 2018: Diagnostic Microbiology and Infectious Disease
https://www.readbyqxmd.com/read/29775209/comparative-studies-of-immobilized-chiral-stationary-phases-based-on-polysaccharide-derivatives-for-enantiomeric-separation-of-fifteen-azole-compounds
#5
Bolin Zhu, Miaoduo Deng, Yaqi Yao, Jia Yu, Qing Li
Immobilized polysaccharide-based columns showed excellent enantioselectivity in normal phase separation mode. In this work, enantioseparation abilities of four immobilized polysaccharide-derived chiral stationary phases (Chiralpak IA, Chiralpak IB, Chiralpak IC and Chiralpak ID) toward fifteen azole compounds were evaluated. Separation was carried out using n-hexane as mobile phase with ethanol, 1-propanol, 1-butanol and 2-propanol as modifiers. And twelve compounds have achieved baseline separation with the resolutions ranging between 2...
May 18, 2018: Electrophoresis
https://www.readbyqxmd.com/read/29773744/worldwide-emergence-of-resistance-to-antifungal-drugs-challenges-human-health-and-food-security
#6
REVIEW
Matthew C Fisher, Nichola J Hawkins, Dominique Sanglard, Sarah J Gurr
The recent rate of emergence of pathogenic fungi that are resistant to the limited number of commonly used antifungal agents is unprecedented. The azoles, for example, are used not only for human and animal health care and crop protection but also in antifouling coatings and timber preservation. The ubiquity and multiple uses of azoles have hastened the independent evolution of resistance in many environments. One consequence is an increasing risk in human health care from naturally occurring opportunistic fungal pathogens that have acquired resistance to this broad class of chemicals...
May 18, 2018: Science
https://www.readbyqxmd.com/read/29771861/vincristine-associated-neuropathy-with-antifungal-usage-a-kaiser-northern-california-experience
#7
Mina Nikanjam, Aida Sun, Mark Albers, Kristine Mangalindin, Eyun Song, Hyma Vempaty, Danny Sam, Edmund V Capparelli
The dose-limiting toxicity for vincristine is peripheral neuropathy which can be potentiated with concurrent usage of azole antifungals. The current retrospective study assessed the incidence of concurrent vincristine and azole antifungal usage to determine if it led to increased neurotoxicity for the Kaiser Northern California pediatric acute lymphoblastic leukemia (ALL) and Hodgkin lymphoma patient population. Data were obtained from the electronic medical record (2007 to 2014). In total, 130 subjects received at least one dose of vincristine for ALL or Hodgkin lymphoma (median age 9, 88% ALL, 58% male, 47% Caucasian)...
May 16, 2018: Journal of Pediatric Hematology/oncology
https://www.readbyqxmd.com/read/29770723/the-impact-of-azole-antifungal-drugs-on-imatinib-metabolism-in-human-liver-microsomes
#8
Xingxian Luo, Taifeng Li, Ze Yu, Xuecai Xue, Haiyang Zhao, Na Li, Liping Ma, Changqing Yang, Lin Huanglin, Wangyu Feng
1. Imatinib is widely used for the treatment of hematologic malignancies. It is common that imatinib is clinically co-prescribed with azole antifungal agents since these patients are more prone to invasive antifungal infection. The present study was to investigate the effects of azole antifungal drugs, including ketoconazole, fluconazole, voriconazole, itraconazole and posaconazole on imatinib metabolism. 2. The main metabolites, 1-OH midazolam and N-desmethyl imatinib, were determined in the absence and in the presence of various levels of ketoconazole, fluconazole, voriconazole, itraconazole and posaconazole...
May 17, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29766819/synthesis-in-silico-molecular-docking-and-pharmacokinetic-studies-in-vitro-antimycobacterial-and-antimicrobial-studies-of-new-imidozolones-clubbed-with-thiazolidinedione
#9
Imran H Khan, Navin B Patel, Vatsal M Patel
BACKGROUND: A series of (E)-5-(4-((Z)-4-substitutedbenzylidene/2-thienylmethylene-5-oxo-2-phenyl-4,5-dihydro-1H-imidazol-1-yl) benzylidene)thiazolidine-2,4-dione were synthesized and evaluated for antimycobacterial and antimicrobial activity. All these ligands were docked against protein (InhA) Enoyl-ACP reductase of the type II fatty acid syntase (FAS-II) system, (PDB ID: 4COD). OBJECTIVE: In this report we have designed and synthesized azole scaffolds with good antitubercular activities as there is a real need to develop new candidates with less toxicity and more efficient toward pathogen...
May 15, 2018: Current Computer-aided Drug Design
https://www.readbyqxmd.com/read/29763525/-bis-imidazolyl-bh%C3%A2-bis-triazolyl-bh%C3%A2-ionic-liquids-with-high-density-and-energy-capacity
#10
Nianming Jiao, Hao Li, Yanqiang Zhang, Long Liu, Suojiang Zhang
[Bis(imidazolyl)-BH₂]+[bis(triazolyl)-BH₂]- and [bis- (imidazolyl)-BH₂]+[tris(triazolyl)-BH]- were first synthesized, whose cations and anions were all functionalized with B-H groups and azoles. As B-H groups contributing to hypergolic activity and azole groups improving the energy outputs, the resulting ionic liquids exhibited ignition delay time as low as 20 ms and energy output as high as 461.1 kJ mol-1. Besides, densities (1.07-1.22 g∙cm-3) and density-specific impulse (ρIsp, ~ 360 s g cm-3) reach to relatively high level...
May 15, 2018: Chemistry, An Asian Journal
https://www.readbyqxmd.com/read/29754833/discovery-of-benzimidazole-derivatives-as-orally-active-renin-inhibitors-optimization-of-3-5-disubstituted-piperidine-to-improve-pharmacokinetic-profile
#11
Hidekazu Tokuhara, Yasuhiro Imaeda, Yoshiyuki Fukase, Koichi Iwanaga, Naohiro Taya, Koji Watanabe, Ray Kanagawa, Keisuke Matsuda, Yumiko Kajimoto, Keiji Kusumoto, Mitsuyo Kondo, Gyorgy Snell, Craig A Behnke, Takanobu Kuroita
We previously identified 2-tert-butyl-4-[(3-methoxypropyl)amino]-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholin-4-ylcarbonyl)piperidin-3-yl]pyrimidine-5-carboxamide 3 as a potent renin inhibitor. Since 3 showed unacceptably low bioavailability (BA) in rats, structural modification, using SBDD and focused on physicochemical properties was conducted to improve its PK profile while maintaining renin inhibitory activity. Conversion of the amino group attached at the 4-position of pyrimidine to methylene group improved PK profile and decreased renin inhibitory activity...
April 27, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29749387/invasive-candidiasis
#12
REVIEW
Peter G Pappas, Michail S Lionakis, Maiken Cavling Arendrup, Luis Ostrosky-Zeichner, Bart Jan Kullberg
Invasive candidiasis is an important health-care-associated fungal infection that can be caused by several Candida spp.; the most common species is Candida albicans, but the prevalence of these organisms varies considerably depending on geographical location. The spectrum of disease of invasive candidiasis ranges from minimally symptomatic candidaemia to fulminant sepsis with an associated mortality exceeding 70%. Candida spp. are common commensal organisms in the skin and gut microbiota, and disruptions in the cutaneous and gastrointestinal barriers (for example, owing to gastrointestinal perforation) promote invasive disease...
May 11, 2018: Nature Reviews. Disease Primers
https://www.readbyqxmd.com/read/29747479/synthesis-and-biological-evaluation-of-bisthiazoles-and-polythiazoles
#13
Mohammed A Al-Omair, Abdelwahed R Sayed, Magdy M Youssef
Small heterocyclic compounds containing nitrogen and sulfur atoms, such as thiazole derivatives, represent a significant class of organic azoles that exhibit promising bioactivities and have a great potential in medicinal and agricultural fields. A convenient and high-yielding synthetic approach for a range of organic molecules is presented. The nuclease-like activities of compounds were studied with the aid of E. coli AB1157 DNA and agarose gel electrophoresis. The antioxidant evaluation of the compounds was carried out with different antioxidant techniques, such as ABTS and NO scavenging efficiency...
May 10, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29747400/in-vitro-anticandidal-activity-and-mechanism-of-a-polyoxovanadate-functionalized-by-zn-fluconazole-complexes
#14
Shuanli Guo, Wei Yang, Mingming Zhao, Rui Tian, Boyu Zhang, Yanfei Qi
The rise in the number of fungal infections is requiring the rapid development of novel antifungal agents. A new polyoxovanadate functionalized by Zn-fluconazole coordination complexes, Zn₃(FLC)₆V10 O28 ·10H₂O (ZnFLC) (FLC = fluconazole) has been synthesized and evaluated for in vitro antifungal against Candida species. The identity of ZnFLC were confirmed by elemental analysis, IR spectrum, and single-crystal X-ray diffraction. The antifungal activities of ZnFLC was screened in 19 Candida species strains using the microdilution checkerboard technique...
May 9, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29746950/candida-periprosthetic-joint-infection-a-rare-and-difficult-to-treat-infection
#15
Laura Escolà-Vergé, Dolors Rodríguez-Pardo, Jaime Lora-Tamayo, Laura Morata, Oscar Murillo, Helem Vilchez, Luisa Sorli, Laura Guío Carrión, José Mª Barbero, Julián Palomino-Nicás, Alberto Bahamonde, Alfredo Jover-Sáenz, Natividad Benito, Rosa Escudero, Marta Fernandez- Sampedro, Rafael Pérez Vidal, Lucía Gómez, Pablo S Corona, Benito Almirante, Javier Ariza, Carles Pigrau
BACKGROUND: Candida periprosthetic joint infection (CPJI) is a rare, difficult-to-treat disease. The purpose of this study was to evaluate the clinical characteristics and outcomes of CPJI treated with various surgical and antifungal strategies. METHODS: We conducted a multicenter retrospective study of all CPJI diagnosed between 2003 and 2015 in 16 Spanish hospitals. RESULTS: Forty-three patients included: median age, 75 years, and median Charlson Comorbidity Index score, 4...
May 7, 2018: Journal of Infection
https://www.readbyqxmd.com/read/29746162/antifungal-activity-of-essential-oils-against-azole-resistant-and-azole-susceptible-i-i-candida-glabrata-i-i-strains-vaginal-isolates
#16
Nadia Massa, Simone Cantamessa, Giorgia Novello, Elia Ranzato, Simona Martinotti, Matteo Pavan, Andrea Rocchetti, Graziella Berta, Elisa Gamalero, Elisa Bona
<i></i>Candida glabrata<i></i> is an opportunistic pathogen, associated with endocarditis, meningitis and disseminated disease and also with complicated vaginitis. Essential oils derived from aromatic plants are known in traditional medicine as antimicrobial agents and have antifungal properties. The aim of this work was to evaluate whether the twelve tested essential oils (tea tree, laurel, anise, basil, bergamot, lavender, mint, oregano, grapefruit, rosemary, winter savory and ginger) could have a transverse effect on <i></i>C...
May 10, 2018: Canadian Journal of Microbiology
https://www.readbyqxmd.com/read/29743305/five-year-national-surveillance-of-invasive-candidiasis-species-distribution-and-azole-susceptibility-from-the-china-hospital-invasive-fungal-surveillance-net-chif-net-study
#17
Meng Xiao, Zi-Yong Sun, Mei Kang, Da-Wen Guo, Kang Liao, Sharon C-A Chen, Fanrong Kong, Xin Fan, Jing-Wei Cheng, Xin Hou, Meng-Lan Zhou, Ying Li, Shu-Ying Yu, Jing-Jing Huang, He Wang, Ying-Chun Xu
Data on the epidemiology of invasive candidiasis (IC) and antifungal susceptibility of Candida isolates in China are still limited. Here we report surveillance for IC from the China Hospital Invasive Fungal Surveillance Net (CHIF-NET) Study. Sixty-five tertiary hospitals collected 8,829 Candida isolates from August 1, 2009 to July 31, 2014. Matrix-assisted laser desorption/ionization -time of flight mass spectrometry supplemented by rDNA sequencing was used to define species, and fluconazole and voriconazole susceptibilities determined by the Clinical and Laboratory Standards Institute disk diffusion method...
May 9, 2018: Journal of Clinical Microbiology
https://www.readbyqxmd.com/read/29740403/overview-of-commercially-available-pcr-assays-for-the-detection-of-aspergillus-spp-dna-in-patient-samples
#18
REVIEW
Peter-Michael Rath, Joerg Steinmann
Invasive aspergillosis (IA) is a life-threatening infection in immunocompromised patients. Early diagnosis is essential to improve survival. Since the 1990s, attempts for PCR-based diagnosis of IA were made. Progress in the standardization of methods enabled the development of commercially available Aspergillus PCR assays in the last few years. Up to now, the clinical value of only a few commercial assays was investigated more extensively in large cohort studies. Most often, respiratory secretions such as bronchoalveolar lavage (BAL) were investigated, but some studies also included serum samples from high-risk patients...
2018: Frontiers in Microbiology
https://www.readbyqxmd.com/read/29738315/diagnosis-and-treatment-of-histoplasmosis-in-solid-organ-transplant-patients
#19
Kiran Gajurel, Reshika Dhakal, Stan Deresinski
PURPOSE OF REVIEW: Unlike immunocompetent hosts, solid organ transplant (SOT) recipients with posttransplant histoplasmosis (PTH) often present with disseminated disease and have an attributable mortality of approximately 10%. In this review, we discuss currently available diagnostic tests and treatment strategies in PTH. RECENT FINDINGS: None of the available tests have a 100% diagnostic accuracy. Histoplasma antigen assays are the most sensitive commercially available tests...
May 5, 2018: Current Opinion in Infectious Diseases
https://www.readbyqxmd.com/read/29730129/anticandidal-synergistic-activity-of-ocimum-sanctum-and-fluconazole-of-azole-resistance-strains-of-clinical-isolates
#20
K U Zaidi, F Shah, R Parmar, V Thawani
Candida albicans is the most prevalent fungal pathogen in humans. It is the causative agent and most associated with serious fungal infection, accounting for more than 90% of cases. It is a most common cause of deep mycoses and vulvovaginal candidiasis. In the present study we found that methanolic extract of O. sanctum in combination of fluconazole shows higher zone of inhibition and lesser MIC values as compared to methanolic extract of leaves of O. sanctum or fluconazole when used alone. Synergistic antimicrobial activity was found when methanolic extract of leaves of O...
May 2, 2018: Journal de Mycologie Médicale
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