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https://www.readbyqxmd.com/read/28106743/design-synthesis-and-antifungal-activity-evaluation-of-new-thiazolin-4-ones-as-potential-lanosterol-14%C3%AE-demethylase-inhibitors
#1
Anca Stana, Dan C Vodnar, Radu Tamaian, Adrian Pîrnău, Laurian Vlase, Ioana Ionuț, Ovidiu Oniga, Brînduşa Tiperciuc
Twenty-three thiazolin-4-ones were synthesized starting from phenylthioamide or thiourea derivatives by condensation with α-monochloroacetic acid or ethyl α-bromoacetate, followed by substitution in position 5 with various arylidene moieties. All the synthesized compounds were physico-chemically characterized and the IR (infrared spectra), ¹H NMR (proton nuclear magnetic resonance), (13)C NMR (carbon nuclear magnetic resonance) and MS (mass spectrometry) data were consistent with the assigned structures...
January 17, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28104135/renal-allograft-aspergillus-infection-presenting-with-obstructive-uropathy-a-case-report
#2
L Sadagah, M Alharbi, M Alshomrani, A Almalki
BACKGROUND: Isolated renal allograft aspergillosis is rare and usually presents with fever and decreased glomerular filtration rate. Presentation with obstructive uropathy caused by aspergillus fungal balls is much less common. We report a young male patient who presented with obstructive uropathy secondary to isolated renal allograft aspergillus infection 6 weeks after transplant. He was treated with nephrectomy and antifungal medications. CASE PRESENTATION: A 29-year-old Saudi male patient had a recent living non-related kidney transplantation in Pakistan...
January 2017: Transplantation Proceedings
https://www.readbyqxmd.com/read/28103779/flavone-analogues-as-antimicrobial-agents
#3
Kamlesh Kumar Naik, Sivakumar Thangavel, Afroze Alam
BACKGROUND: Most of the available antimicrobial drugs have developed resistance, some of them suffer from severe toxicity, side effects. So, there is a need to discover novel compound(s) which should not only be potent, but also less toxic and cost effective. OBJECTIVES: The aim of the study is to develop new synthetic antimicrobial agents (Anti-bacterial and anti-fungal) such as 3-substituted flavone/flavanone derivatives, which should be significantly potent with low toxicity...
January 18, 2017: Recent Patents on Inflammation & Allergy Drug Discovery
https://www.readbyqxmd.com/read/28040409/antifungal-effects-of-phytocompounds-on-candida-species-alone-and-in-combination-with-fluconazole
#4
REVIEW
Mengjiao Lu, Tao Li, Jianjian Wan, Xiuyun Li, Lei Yuan, Shujuan Sun
Invasive fungal infections caused by Candida spp. remain the most predominant nosocomial fungal infections. Owing to the increased use of antifungal agents, resistance of Candida spp. to antimycotics has emerged frequently, especially to fluconazole (FLC). To cope with this issue, new efforts have been dedicated to discovering novel antimycotics or new agents that can enhance the susceptibility of Candida spp. to existing antimycotics. The secondary metabolites of plants represent a large library of compounds that are important sources for new drugs or compounds suitable for further modification...
December 15, 2016: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28026947/biodegradable-kojic-acid-based-polymers-controlled-delivery-of-bioactives-for-melanogenesis-inhibition
#5
Jonathan J Faig, Alysha Moretti, Laurie B Joseph, Yingyue Zhang, Mary Joy Nova, Kervin Smith, Kathryn E Uhrich
Kojic acid (KA) is a naturally occurring fungal metabolite that is utilized as a skin-lightener and anti-browning agent owing to its potent tyrosinase inhibition activity. While efficacious, KA's inclination to undergo pH-mediated, thermal-, and photo-degradation reduces its efficacy, necessitating stabilizing vehicles. To minimize degradation, poly(carbonate-esters) and polyesters comprised of KA and natural diacids were prepared via solution polymerization methods. In vitro hydrolytic degradation analyses revealed KA release was drastically influenced by polymer backbone composition (e...
December 27, 2016: Biomacromolecules
https://www.readbyqxmd.com/read/28003000/double-edge-sword-behavior-of-carbendazim-a-potent-fungicide-with-anti-cancer-therapeutic-properties
#6
Karan Goyal, Ajay Sharma, Ridhima Arya, Rohit Sharma, Girish K Gupta, Anil K Sharma
A number of benzimidazole derivatives such as benomyl and carbendazim have been known for their potential role as agricultural fungicides. Simultaneously carbendazim has also been found to inhibit proliferation of mammalian tumor cells specifically drug and multidrug resistant cell lines. Studies carried out with fungal and mammalian cells have highlighted the potential role of carbendazim in inhibiting proliferation of cells, thereby exhibiting therapeutic implications against cancer. Because of its promising preclinical antitumor activity, Carbendazim had undergone phase I clinical trials and is under further clinical investigations for treatment of cancer...
December 21, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27994583/beyond-traditional-antimicrobials-a-caenorhabditis-elegans-model-for-discovery-of-novel-anti-infectives
#7
REVIEW
Cin Kong, Su-Anne Eng, Mei-Perng Lim, Sheila Nathan
The spread of antibiotic resistance amongst bacterial pathogens has led to an urgent need for new antimicrobial compounds with novel modes of action that minimize the potential for drug resistance. To date, the development of new antimicrobial drugs is still lagging far behind the rising demand, partly owing to the absence of an effective screening platform. Over the last decade, the nematode Caenorhabditis elegans has been incorporated as a whole animal screening platform for antimicrobials. This development is taking advantage of the vast knowledge on worm physiology and how it interacts with bacterial and fungal pathogens...
2016: Frontiers in Microbiology
https://www.readbyqxmd.com/read/27976895/angiogenesis-inhibitors-and-anti-inflammatory-agents-from-phoma-sp-ntou4195
#8
Ming-Shian Lee, Shih-Wei Wang, Guei-Jane Wang, Ka-Lai Pang, Ching-Kuo Lee, Yueh-Hsiung Kuo, Hyo-Jung Cha, Ruo-Kai Lin, Tzong-Huei Lee
Seven new polyketides, phomaketides A-E (1-5) and pseurotins A3 (6) and G (7), along with the known compounds FR-111142, pseurotins A, A1, A2, D, and F2, 14-norpseurotin A, α-carbonylcarbene, tyrosol, cyclo(-l-Pro-l-Leu), and cyclo(-l-Pro-l-Phe), were purified from the fermentation broth and mycelium of the endophytic fungal strain Phoma sp. NTOU4195 isolated from the marine red alga Pterocladiella capillacea. The structures were established through interpretation of spectroscopic data. The antiangiogenic and anti-inflammatory effects of 1-7 and related analogues were evaluated using human endothelial progenitor cells (EPCs) and lipopolysaccharide (LPS)-activated murine macrophage RAW264...
December 23, 2016: Journal of Natural Products
https://www.readbyqxmd.com/read/27914593/systemic-and-localized-infection-by-candida-species-in-patients-with-rheumatic-diseases-receiving-anti-tnf-therapy
#9
Nadia E Aikawa, Daniela T A Rosa, Gilda M B Del Negro, Julio C B Moraes, Ana C M Ribeiro, Carla Gonçalves Saad, Clovis A Silva, Eloisa Bonfá
OBJECTIVE: To evaluate the prevalence of systemic and localized infection by Candida species and its possible association with demographic, clinical and laboratory manifestations and therapy in patients with rheumatic diseases taking TNF blockers. METHODS: Consecutive patients with rheumatic diseases receiving anti-TNF agents were included. The following risk factors up to four weeks prior to the study were analyzed: use of antibiotics, immunosuppressant drugs, hospitalization and invasive procedures...
November 2016: Revista Brasileira de Reumatologia
https://www.readbyqxmd.com/read/27907875/s-substituted-3-5-dinitrophenyl-1-3-4-oxadiazole-2-thiols-and-tetrazole-5-thiols-as-highly-efficient-antitubercular-agents
#10
Galina Karabanovich, Jan Němeček, Lenka Valášková, Alejandro Carazo, Klára Konečná, Jiřina Stolaříková, Alexandr Hrabálek, Oto Pavliš, Petr Pávek, Kateřina Vávrová, Jaroslav Roh, Věra Klimešová
Two new classes of antitubercular agents, namely 5-alkylsulfanyl-1-(3,5-dinitrophenyl)-1H-tetrazoles and 2-alkylsulfanyl-5-(3,5-dinitrophenyl)-1,3,4-oxadiazoles, and their structure-activity relationships are described. These compounds possessed excellent activity against Mycobacterium tuberculosis, including the clinically isolated multidrug (MDR) and extensively drug-resistant (XDR) strains, with no cross resistance with first or second-line anti-TB drugs. The minimum inhibitory concentration (MIC) values of the most promising compounds reached 0...
November 21, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27876749/anti-fungal-activity-of-ctn-15-34-the-c-terminal-peptide-fragment-of-crotalicidin-a-rattlesnake-venom-gland-cathelicidin
#11
Carolina Sidrim P Cavalcante, Cláudio B Falcão, Raquel Os Fontenelle, David Andreu, Gandhi Rádis-Baptista
Crotalicidin (Ctn), a 34-residue cathelicidin from a South American rattlesnake, and its fragment (Ctn[15-34]) have shown anti-infective and cytotoxic activities against Gram-negative bacteria and certain tumor lines, respectively. The extent of such effects has been related to physicochemical characteristics such as helicity and hydrophobicity. We now report the anti-fungal activity of Ctn and its fragments (Ctn[1-14]) and (Ctn[15-34]). MIC determination and luminescent cell viability assays were used to evaluate the anti-infective activity of Ctn and its fragments (Ctn[1-14]) and (Ctn[15-34]) as anti-fungal agents against opportunistic yeast and dermatophytes...
November 23, 2016: Journal of Antibiotics
https://www.readbyqxmd.com/read/27874849/systematic-chemical-genetic-and-chemical-chemical-interaction-datasets-for-prediction-of-compound-synergism
#12
Jan Wildenhain, Michaela Spitzer, Sonam Dolma, Nick Jarvik, Rachel White, Marcia Roy, Emma Griffiths, David S Bellows, Gerard D Wright, Mike Tyers
The network structure of biological systems suggests that effective therapeutic intervention may require combinations of agents that act synergistically. However, a dearth of systematic chemical combination datasets have limited the development of predictive algorithms for chemical synergism. Here, we report two large datasets of linked chemical-genetic and chemical-chemical interactions in the budding yeast Saccharomyces cerevisiae. We screened 5,518 unique compounds against 242 diverse yeast gene deletion strains to generate an extended chemical-genetic matrix (CGM) of 492,126 chemical-gene interaction measurements...
November 22, 2016: Scientific Data
https://www.readbyqxmd.com/read/27855875/mechanisms-of-antifungal-and-anti-aflatoxigenic-properties-of-essential-oil-derived-from-turmeric-curcuma-longa-l-on-aspergillus-flavus
#13
Yichen Hu, Jinming Zhang, Weijun Kong, Gang Zhao, Meihua Yang
The antifungal activity and potential mechanisms in vitro as well as anti-aflatoxigenic efficiency in vivo of natural essential oil (EO) derived from turmeric (Curcuma longa L.) against Aspergillus flavus was intensively investigated. Based on the previous chemical characterization of turmeric EO by gas chromatography-mass spectrometry, the substantially antifungal activities of turmeric EO on the mycelial growth, spore germination and aflatoxin production were observed in a dose-dependent manner. Furthermore, these antifungal effects were related to the disruption of fungal cell endomembrane system including the plasma membrane and mitochondria, specifically i...
April 1, 2017: Food Chemistry
https://www.readbyqxmd.com/read/27842800/anti-candida-albicans-natural-products-sources-of-new-antifungal-drugs-a-review
#14
REVIEW
A Zida, S Bamba, A Yacouba, R Ouedraogo-Traore, R T Guiguemdé
INTRODUCTION: Candida albicans is the most prevalent fungal pathogen in humans. Due to the development of drug resistance, there is today a need for new antifungal agents for the efficient management of C. albicans infections. Therefore, we reviewed antifungal activity, mechanisms of action, possible synergism with antifungal drugs of all natural substances experimented to be efficient against C. albicans for future. METHODS: An extensive and systematic review of the literature was undertaken and all relevant abstracts and full-text articles analyzed and included in the review...
November 11, 2016: Journal de Mycologie Médicale
https://www.readbyqxmd.com/read/27829814/quinoline-based-furanones-and-their-nitrogen-analogues-docking-synthesis-and-biological-evaluation
#15
Sukhbir Lal Khokra, Jyoti, Chetan, Pawan Kaushik, M M Alam, M S Zaman, Aftab Ahmad, Shah Alam Khan, Asif Husain
A small library of twenty-four quinoline based butenolides also known as furanones and their nitrogen analogues was prepared by using two different aroylpropionic acids, viz. 3-(2-naphthoyl)propionic acid (3) and 3-(biphenyl-4-yl)propionic acid (4), as starting materials. The 3-aroylpropionic acids were reacted with different 6-substituted-2-chloroquinolin-3-carbaldehydes (2a-d) to obtain the corresponding furan-2(3H)-ones (5a-h). The purified and characterized furanones were then converted into their corresponding 2(3H)-pyrrolones (6a-h) and N-benzyl-pyrrol-2(3H)-ones (7a-h)...
November 2016: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/27816628/amphotericin-b-copper-ii-complex-shows-improved-therapeutic-index-in-vitro
#16
Barbara Chudzik, Grzegorz Czernel, Arkadiusz Miaskowski, Mariusz Gagoś
The AmB-Cu(II) complex has recently been reported as an antifungal agent with reduced aggregation of AmB in aqueous solutions, increased anti C. albicans activity and lower toxicity against human cells in vitro. In the present work, investigations of the activity of the AmB-Cu (II) complex against fungal pathogens with varying susceptibility, including C. albicans and C. parapsilosis strains and intrinsically resistant A. niger, and cytotoxicity in normal human dermal fibroblasts (NHDF) in vitro were performed...
January 15, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27806050/protein-translation-enzyme-lysyl-trna-synthetase-presents-a-new-target-for-drug-development-against-causative-agents-of-loiasis-and-schistosomiasis
#17
Arvind Sharma, Manmohan Sharma, Manickam Yogavel, Amit Sharma
Helminth parasites are an assemblage of two major phyla of nematodes (also known as roundworms) and platyhelminths (also called flatworms). These parasites are a major human health burden, and infections caused by helminths are considered under neglected tropical diseases (NTDs). These infections are typified by limited clinical treatment options and threat of drug resistance. Aminoacyl-tRNA synthetases (aaRSs) are vital enzymes that decode genetic information and enable protein translation. The specific inhibition of pathogen aaRSs bores well for development of next generation anti-parasitics...
November 2016: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/27801509/anti-rhodotorula-activity-of-mycophenolic-acid-enhanced-in-the-presence-of-polyene-antibiotic-nystatin
#18
H Kinoshita, S Wongsuntornpoj, F Ihara, T Nihira
: Rhodotorula species are opportunistic pathogens, which cause not only systemic fungaemia but also other localized infections. Despite serious side effects such as nephrotoxicity and hypokalemia, amphotericin B (a polyene antifungal) has been commonly prescribed for Rhodotorula infection because Rhodotorula species are resistant against a candin family of antifungal agents. In this study, novel active compounds against Rhodotorula species were screened from the extracts of entomopathogenic fungi based on the synergistic effect of polyene nystatin (NYS), which causes efficient targeting of compounds due to increased permeability through the fungal cell membrane...
November 1, 2016: Letters in Applied Microbiology
https://www.readbyqxmd.com/read/27789337/aspergillus-flavus-induced-alterations-in-tear-protein-profile-reveal-pathogen-induced-host-response-to-fungal-infection
#19
Jeyalakshmi Kandhavelu, Naveen Luke Demonte, Venkatesh Prajna Namperumalsamy, Lalitha Prajna, Chitra Thangavel, Jeya Maheshwari Jayapal, Dharmalingam Kuppamuthu
: Aspergillus flavus and Fusarium sp. are primary causative agents of keratitis that results in corneal tissue damage leading to vision loss particularly in individuals from the tropical parts of the world. Proteins in the tear film collected from control and keratitis patients was profiled and compared. A total of 1873 proteins from control and 1400 proteins from patient tear were identified by mass spectrometry. While 847 proteins were found to be glycosylated in the patient tear, only 726 were glycosylated in control tear...
January 30, 2017: Journal of Proteomics
https://www.readbyqxmd.com/read/27789295/effect-of-stress-on-heat-shock-protein-levels-immune-response-and-survival-to-fungal-infection-of-mamestra-brassicae-larvae
#20
E H Richards, M P Dani, Y Lu, T Butt, R J Weaver
Although the utilisation of fungal biological control agents to kill insect pests is desirable, it is known that the outcome of infection may be influenced by a number of criteria, including whether or not the target insect is stressed. In the current work, topical treatment of larvae of the lepidopteran pest, Mamestra brassicae, with conidia of Beauveria bassiana, followed by a heat stress (HS; 37°C for 1h) 48h later, resulted in a similar level of larval survival to that occurring for no heat stress (No-HS), fungus-treated larvae...
January 2017: Journal of Insect Physiology
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