keyword
MENU ▼
Read by QxMD icon Read
search

Azole

keyword
https://www.readbyqxmd.com/read/29168743/synthesis-and-anticandidal-activity-evaluation-of-new-benzimidazole-thiazole-derivatives
#1
Zafer Asım Kaplancıklı, Serkan Levent, Derya Osmaniye, Begüm Nurpelin Sağlık, Ulviye Acar Çevik, Betül Kaya Çavuşoğlu, Yusuf Özkay, Sinem Ilgın
Azole-based antifungal agents constitute one of the important classes of antifungal drugs. Hence, in the present work, 12 new benzimidazole-thiazole derivatives 3a-3l were synthesized to evaluate their anticandidal activity against C.albicans, C.glabrata, C.krusei, and C.parapsilopsis. The structures of the newly synthesized compounds 3a-3l were confirmed by IR, ¹H-NMR, (13)C-NMR, and ESI-MS spectroscopic methods. ADME parameters of synthesized compounds 3a-3l were predicted by an in-slico study and it was determined that all synthesized compounds may have a good pharmacokinetic profile...
November 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29168537/pd-catalyzed-regioselective-intramolecular-dehydrogenative-c-5-cross-coupling-in-an-n-substituted-pyrrole-azole-system
#2
Krishna N Tripathi, Devalina Ray, Ravi P Singh
Functionalized polycyclic pyrrole-azole structures possessing fused six membered and seven membered rings were directly synthesized via ligand-enabled, Pd-catalyzed, site selective, intramolecular cross couplings of N-substituted pyrrole-azoles. C5-H activation in the presence of a reactive C2-H remains a challenge that needs to be addressed and this was targeted to be resolved through the present approach by specifically generating the cyclized products with 83-100% selectivity. The featured methodology provides a novel disconnection for the synthesis of pyrrole containing alkaloids and medicinal compounds...
November 23, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/29168144/a-review-of-chronic-granulomatous-disease
#3
REVIEW
Danielle E Arnold, Jennifer R Heimall
Chronic granulomatous disease (CGD) is a primary immunodeficiency caused by defects in any of the five subunits of the NADPH oxidase complex responsible for the respiratory burst in phagocytic leukocytes. Patients with CGD are at increased risk of life-threatening infections with catalase-positive bacteria and fungi and inflammatory complications such as CGD colitis. The implementation of routine antimicrobial prophylaxis and the advent of azole antifungals has considerably improved overall survival. Nevertheless, life expectancy remains decreased compared to the general population...
November 22, 2017: Advances in Therapy
https://www.readbyqxmd.com/read/29164433/distal-lateral-subungual-onychomycosis-owing-to-tritirachium-oryzae-a-bystander-or-invader
#4
Hari Pankaj Vanam, P Narsimha Rao, Kalyani Mohanram, Prakash Peralam Yegneswaran, Shiva Prakash Mandya Rudramurthy
The genus Tritirachium is a mitosporic fungus which inhabits in soil and decaying plant material and also a notable insect pathogen. Human infections with Tritirachium species though rare were previously reported to cause corneal ulcers, otomycosis, onychomycosis, and dermatomycosis of the scalp and hence may be considered as a potential pathogen. Here we report a case of distal lateral subungual onychomycosis involving right great toenail in a 22-year-old female, wherein direct potassium hydroxide preparations, fungal cultures, and molecular sequencing of the isolate established Tritirachium oryzae as the etiological agent...
November 21, 2017: Mycopathologia
https://www.readbyqxmd.com/read/29163916/a-new-face-of-phenalenyl-based-radicals-in-the-transition-metal-free-c-h-arylation-of-heteroarenes-at-room-temperature-trapping-the-radical-initiator-via-c-c-%C3%AF-bond-formation
#5
Jasimuddin Ahmed, Sreejyothi P, Gonela Vijaykumar, Anex Jose, Manthan Raj, Swadhin K Mandal
The radical-mediated transition metal-free approach for the direct C-H bond functionalization of arenes is considered as a cost effective alternative to transition metal-based catalysis. An organic ligand-based radical plays a key role by generating an aryl radical which undergoes a subsequent functionalization process. The design principle of the present study takes advantage of a relatively stable odd alternant hydrocarbon-based phenalenyl (PLY) radical. In this study, the first transition metal-free catalyzed direct C-H arylation of a variety of heteroarenes such as azoles, furan, thiophene and pyridine at room temperature has been reported using a phenalenyl-based radical without employing any photoactivation step...
November 1, 2017: Chemical Science
https://www.readbyqxmd.com/read/29162893/intrinsic-short-tailed-azole-resistance-in-mucormycetes-is-due-to-an-evolutionary-conserved-aminoacid-substitution-of-the-lanosterol-14%C3%AE-demethylase
#6
Rita Caramalho, Joel D A Tyndall, Brian C Monk, Thomas Larentis, Cornelia Lass-Flörl, Michaela Lackner
Mucormycoses are emerging and potentially lethal infections. An increase of breakthrough infections has been found in cohorts receiving short-tailed azoles prophylaxis (e.g. voriconazole (VCZ)). Although VCZ is ineffective in vitro and in vivo, long-tailed triazoles such as posaconazole remain active against mucormycetes. Our goal was to validate the molecular mechanism of resistance to short-tailed triazoles in Mucorales. The paralogous cytochrome P450 genes (CYP51 F1 and CYP51 F5) of Rhizopus arrhizus, Rhizopus microsporus, and Mucor circinelloides were amplified and sequenced...
November 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29158527/azole-sensitivity-in-leptosphaeria-pathogens-of-oilseed-rape-the-role-of-lanosterol-14%C3%AE-demethylase
#7
Thomas R Sewell, Nichola J Hawkins, Henrik U Stotz, YongJu Huang, Steven L Kelly, Diane E Kelly, Bart Fraaije, Bruce D L Fitt
Lanosterol 14-α demethylase is a key enzyme intermediating the biosynthesis of ergosterol in fungi, and the target of azole fungicides. Studies have suggested that Leptosphaeria maculans and L. biglobosa, the causal agents of phoma stem canker on oilseed rape, differ in their sensitivity to some azoles, which could be driving pathogen frequency change in crops. Here we used CYP51 protein modelling and heterologous expression to determine whether there are interspecific differences at the target-site level...
November 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29158264/azole-resistance-in-a-candida-albicans-mutant-lacking-the-abc-transporter-cdr6-roa1-depends-on-tor-signaling
#8
Nitesh Kumar Khandelwal, Neeraj Chauhan, Parijat Sarkar, Brooke D Esquivel, Paola Coccetti, Ashutosh Singh, Alix T Coste, Meghna Gupta, Dominique Sanglard, Theodore C White, Murielle Chauvel, Christophe dEnfert, Amitabha Chattopadhyay, Naseem A Gaur, Alok Kumar Mondal, Rajendra Prasad
ATP-binding cassette (ABC) transporters help export various substrates across the cell membrane and significantly contribute to drug resistance. However, a recent study reported an unusual case in which the loss of an ABC transporter in Candida albicans, orf19.4531 (previously named ROA1), increases resistance against antifungal azoles, which was attributed to an altered membrane potential in the mutant strain. To get further mechanistic insights into this phenomenon, here we confirmed that the plasma membrane localized transporter (renamed CDR6/ROA1 for consistency with C...
November 20, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29155163/antifungal-azoles-itraconazole-and-posaconazole-exhibit-potent-in-vitro-antiviral-activity-against-clinical-isolates-of-parechovirus-a3-picornaviridae
#9
Eric Rhoden, W Allan Nix, William C Weldon, Rangaraj Selvarangan
Parechovirus A3 (Par-A3, formerly human parechovirus 3) is an emerging viral infection of the central nervous system in children. We used an automated, homogeneous, cell based assay to identify itraconazole and posaconazole as inhibitors of Par-A3, with antiviral activity below concentrations clinically attainable in pediatric patients. Currently, there is no approved antiviral treatment for Par-A3 infection, despite numerous reports of serious Par-A3 disease in neonates and infants.
November 15, 2017: Antiviral Research
https://www.readbyqxmd.com/read/29153588/azole-hydrazone-derivatives-design-synthesis-in-vitro-biological-evaluation-dual-egfr-her2-inhibitory-activity-cell-cycle-analysis-and-molecular-docking-study-as-anticancer-agents
#10
Madlen B Labib, John N Philoppes, Phoebe F Lamie, Esam R Ahmed
In this research, three series of azole-hydrazone derivatives namely, benzimidazole, benzoxazole and benzothiazole were designed and synthesized. Their structures were confirmed by elemental analysis and spectroscopic techniques. Stereochemical configuration of the synthesized compounds (Z/E) was determined. The new derivatives were tested in vitro against both human breast adenocarcinoma (MCF-7) and human hepatic adenocarcinoma (HepG2) cell lines. The most active compounds 3h (IC50 = 0.067 μM against MCF-7) and 3l (IC50 = 0...
November 15, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29150592/the-influence-of-genetic-stability-on-aspergillus-fumigatus-virulence-and-azole-resistance
#11
Thaila Fernanda Dos Reis, Lilian Pereira Silva, Patrícia Alves de Castro, Pollyne Borborema Almeida de Lima, Rafaela Andrade do Carmo, Marjorie Mendes Marini, José Franco da Silveira, Beatriz Henriques Ferreira, Fernando Rodrigues, Iran Malavazi, Gustavo H Goldman
Genetic stability is extremely important for the survival of every living organism and a very complex set of genes have evolved to cope with DNA repair upon DNA damage. Here, we investigated the Aspergillus fumigatus AtmA (Ataxia-telangiectasia mutated) and AtrA kinases and how they impact virulence and the evolution of azole resistance. We demonstrated that A. fumigatus atmA and atrA null mutants are haploid and have a discrete chromosomal polymorphism. The ΔatmA and ΔatrA strains are sensitive to several DNA damaging agents but surprisingly both strains were more resistant than the wild-type strain to paraquat, menadione, and hydrogen peroxide...
November 17, 2017: G3: Genes—Genomes—Genetics
https://www.readbyqxmd.com/read/29141039/identification-of-isolates-of-the-plant-pathogen-leptosphaeria-maculans-with-resistance-to-the-triazole-fungicide-fluquinconazole-using-a-novel-in-planta-assay
#12
Angela P Van de Wouw, Vicki L Elliott, Steven Chang, Francisco J López-Ruiz, Steven J Marcroft, Alexander Idnurm
Leptosphaeria maculans is the major pathogen of canola (oilseed rape, Brassica napus) worldwide. In Australia, the use of azole fungicides has contributed to the 50-fold increase in canola production in the last 25 years. However, extensive application of fungicides sets the stage for the selection of fungal populations with resistance. A high-throughput in planta assay was developed to allow screening of thousands of isolates from multiple populations. Using this screen, isolates were identified with decreased sensitivity to the fungicide fluquinconazole when applied at field rates as a protective seed dressing: these isolates cause significantly larger lesions on cotyledons and true leaves and increased disease severity at plant maturity...
2017: PloS One
https://www.readbyqxmd.com/read/29138059/pityrosporum-folliculitis-a-retrospective-review-of-110-cases
#13
Brea Prindaville, Leah Belazarian, Nikki A Levin, Karen Wiss
BACKGROUND: Pityrosporum folliculitis is an under-recognized eruption of the face and upper trunk that may be confused with, or occur simultaneously with, acne vulgaris. OBJECTIVE: We sought to characterize risk factors for Pityrosporum folliculitis, its clinical presentation, and response to treatment. METHODS: A retrospective chart review was performed on all patients aged 0 to 21 years seen from 2010-2015 with Pityrosporum folliculitis confirmed by potassium hydroxide (KOH) preparation...
November 11, 2017: Journal of the American Academy of Dermatology
https://www.readbyqxmd.com/read/29136186/clonal-spread-and-azole-resistant-mechanisms-of-non-susceptible-candida-albicans-isolates-from-vulvovaginal-candidiasis-patients-in-three-shanghai-maternity-hospitals
#14
YongQin Wu, Cui Li, ZhiHeng Wang, Jing Gao, ZhenHua Tang, HuiFen Chen, ChunMei Ying
In our multicenter study, 43 fluconazole non-susceptible and 45 fluconazole-susceptible isolates were collected from vulvovaginal candidiasis (VVC) patients from three Shanghai maternity hospitals to analyze their molecular epidemiological features and fluconazole resistant mechanisms. Cross-resistance to fluconazole, itraconazole and voriconazole was observed in 53.5% of the nonsusceptible isolates. Though we acquired 12 clonal complexes (CCs) of diploid sequence types (DSTs) in clinical isolates by a multilocus sequence typing method, fluconazole nonsusceptible isolates all belonged to CC69 with a predominant genotype of DST 79...
November 9, 2017: Medical Mycology: Official Publication of the International Society for Human and Animal Mycology
https://www.readbyqxmd.com/read/29133157/microbiological-and-clinical-characteristics-of-biofilm-forming-candida-parapsilosis-isolates-associated-with-fungaemia-and-their-impact-on-mortality
#15
Silvia Soldini, Brunella Posteraro, Antonietta Vella, Elena De Carolis, Elisa Borghi, Monica Falleni, Angela Raffaella Losito, Giuseppe Maiuro, Enrico Maria Trecarichi, Maurizio Sanguinetti, Mario Tumbarello
OBJECTIVES: Biofilm formation (BF) by fungal isolates may dramatically complicate infection. We determined the ability of C. parapsilosis isolates from single fungaemia episodes to form biofilms and we analysed biofilm subgroups for antifungal susceptibility and pathogenic potential. We then correlated BF with clinical characteristics and outcomes of the episodes. METHODS: BF was measured using the crystal-violet biomass assay, antifungal susceptibility of preformed biofilms was assessed, and virulence was studied using the Galleria mellonella model...
November 10, 2017: Clinical Microbiology and Infection
https://www.readbyqxmd.com/read/29127020/does-the-use-of-antifungal-agents-in-agriculture-and-in-food-foster-polyene-resistance-development-a-reason-for-concern
#16
REVIEW
Axel Dalhoff
Environmental fungicides are used in agriculture to reduce fungal spoilage of crop to a minimum and the polyene macrolide natamycin is used as a food preservative. The use of natamycin in yoghurt has recently been authorized in the USA and some other countries. However, resistance development is a serious risk associated with the use of antimicrobials as food additives and environmental fungicides. Cross-resistance between agricultural and medical azoles and amphothericin B, respectively, not being used in agriculture has been demonstrated in clinical and environmental isolates...
November 7, 2017: Journal of Global Antimicrobial Resistance
https://www.readbyqxmd.com/read/29124846/prevalence-mechanisms-and-genetic-relatedness-of-the-human-pathogenic-fungus-aspergillus-fumigatus-exhibiting-resistance-to-medical-azoles-in-the-environment-of-taiwan
#17
Hsuan-Chen Wang, Jui-Chang Huang, Yong-Hong Lin, Yu-Hsin Chen, Ming-I Hsieh, Pui-Ching Choi, Hsiu-Jung Lo, Wei-Lun Liu, Ching-Shan Hsu, Hsin-I Shih, Chi-Jung Wu, Yee-Chun Chen
Emerging azole resistance in Aspergillus fumigatus poses a serious threat to human health. This nationwide surveillance study investigated the prevalence and molecular characteristics of azole-resistant A. fumigatus environmental isolates in Taiwan, an island country with increasing use of azole fungicides. Of the 2,760 air and soil samples screened from 2014-2016, 451 A. fumigatus isolates were recovered from 266 samples, and 34 isolates from 29 samples displayed resistance to medical azoles (itraconazole, voriconazole, or posaconazole)...
November 10, 2017: Environmental Microbiology
https://www.readbyqxmd.com/read/29112282/antifungals-discovery-an-insight-into-new-strategies-to-combat-antifungal-resistance
#18
REVIEW
Alexandre M Fuentefria, Bruna Pippi, Daiane F Dalla Lana, Katarzyna K Donato, Saulo F de Andrade
Undeniably, new antifungal treatments are necessary against pathogenic fungi. Fungal infections have significantly increased in recent decades, being highlighted as important causes of morbidity and mortality, particularly in immunocompromised patients. Five main antifungal classes are used: (i) azoles, (ii) echinocandins, (iii) polyenes, (iv) allylamines and (v) pyrimidine analogs. Moreover, the treatment of mycoses has several limitations, such as; undesirable side effects, narrow activity spectrum, a small number of targets and fungal resistance; which are still of major concern in clinical practice...
November 7, 2017: Letters in Applied Microbiology
https://www.readbyqxmd.com/read/29109169/environmental-triazole-induces-cross-resistance-to-clinical-drugs-and-affects-morphophysiology-and-virulence-of-cryptococcus-gattii-and-c-neoformans
#19
Rafael Wesley Bastos, Hellem Cristina Silva Carneiro, Lorena Vívien Neves de Oliveira, Karen Maia Rocha, Gustavo José Cota Freitas, Marliete Carvalho Costa, Thaís Furtado Ferreira Magalhães, Vanessa Silva Dutra de Carvalho, Cláudia Emanuela Rocha, Gabriella Freitas Ferreira, Tatiane Alves de Paixão, Frédérique Moyrand, Guilhem Janbon, Daniel Assis Santos
Cryptococcus gattii and Cryptococcus neoformans are environmental fungi that cause cryptococcosis, which is usually treated with amphotericin B and fluconazole. However, therapeutic failure is increasing because of the emergence of resistant strains. Because these species are constantly isolated from vegetal materials and the usage of agrochemicals is growing, we postulate pesticides could be responsible for the altered susceptibility of these fungi to clinical drugs. Therefore, we evaluated the influence of the pesticide tebuconazole on the susceptibility to clinical drugs, morphophysiology, and virulence of C...
November 6, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29102310/-vertebral-osteomyelitis-due-to-candida-tropicalis-secondary-to-candidemia-a-case-report
#20
S Zayet, I Chaabane, B Kilani, M Bouaziz, F Ladeb, H B Tiouiri
Candida spp. vertebral osteomyelitis is rare. Clinical presentation is unspecific. Diagnosis requires mycological culture of a biopsy specimen. Therapeutic management is based on prolonged course of azole or liposomal amphotericin B. We report the case of Candida tropicalis vertebral osteomyelitis with epidural involvement in a 27 years-old male patient, followed for S-β-thalassemia and with a history of candidemia. The fungus was isolated from a needle biopsy of the vertebral disk. The outcome was favorable under antifungal treatment by amphotericin B and voriconazole...
October 25, 2017: Journal de Mycologie Médicale
keyword
keyword
69463
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"