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https://www.readbyqxmd.com/read/27914363/new-insights-into-the-sar-and-drug-combination-synergy-of-2-quinolin-4-yloxy-acetamides-against-mycobacterium-tuberculosis
#1
Bruno Couto Giacobbo, Kenia Pissinate, Valnês Rodrigues-Junior, Anne Drumond Villela, Estêvão Silveira Grams, Bruno Lopes Abbadi, Fernanda Teixeira Subtil, Nathalia Sperotto, Rogério Valim Trindade, Davi Fernando Back, Maria Martha Campos, Luiz Augusto Basso, Pablo Machado, Diógenes Santiago Santos
2-(Quinolin-4-yloxy)acetamides have been described as potent and selective in vitro inhibitors of Mycobacterium tuberculosis (Mtb) growth. Herein, a new series of optimized compounds were found to demonstrate highly potent antitubercular activity, with minimum inhibitory concentration (MIC) values against drug-susceptible and drug-resistant Mycobacterium tuberculosis strains in the submicromolar range. Furthermore, the most active compounds had no apparent toxicity to mammalian cells, and they showed intracellular activities similar to those of isoniazid and rifampin in a macrophage model of Mtb infection...
November 23, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27914001/subtilosin-prevents-biofilm-formation-by-inhibiting-bacterial-quorum-sensing
#2
Ammar Algburi, Saskia Zehm, Victoria Netrebov, Anzhelica B Bren, Vladimir Chistyakov, Michael L Chikindas
Subtilosin, the cyclic lantibiotic protein produced by Bacillus subtilis KATMIRA1933, targets the surface receptor and electrostatically binds to the bacterial cell membrane. In this study, subtilosin was purified using ammonium sulfate ((NH4)2SO4) precipitation and purified via column chromatography. Subtilosin's antibacterial minimum and sub-minimum inhibitory concentrations (MIC and sub-MIC) and anti-biofilm activity (biofilm prevention) were established. Subtilosin was evaluated as a quorum sensing (QS) inhibitor in Gram-positive bacteria using Fe(III) reduction assay...
December 2, 2016: Probiotics and Antimicrobial Proteins
https://www.readbyqxmd.com/read/27912884/synergism-of-coumarins-from-the-chinese-drug-zanthoxylum-nitidum-with-antibacterial-agents-against-methicillin-resistant-staphylococcus-aureus-mrsa
#3
Guo-Ying Zuo, Chun-Juan Wang, Jun Han, Yu-Qing Li, Gen-Chun Wang
BACKGROUND: Methicillin-resistant Staphylococcus aureus (MRSA) poses a serious therapeutic challenge in current clinic and new drug development. Natural coumarins have diverse bioactivities and the potential of resistance modifying effects. PURPOSE: This study is to present in-depth evaluations of in vitro antimicrobial activities of four natural coumarins 5-geranyloxy-7-methoxycoumarin (Gm, 1), (5,7-dimethoxy-8-prenyloxycoumarin (artanin, Ar, 2)), isopimpinellin (Is, 3) and phellopterin (Ph, 4) from Zanthoxylum nitidum (Roxb...
December 15, 2016: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/27912176/novel-designed-vmct1-analogs-with-increased-antimicrobial-activity
#4
Cibele Nicolaski Pedron, Marcelo Der Torossian Torres, Julia Aparecida da Silva Lima, Pedro Ismael Silva, Fernanda Dias Silva, Vani Xavier Oliveira
Antimicrobial peptides are biologically active molecules produced by a wide range of organisms as an essential component of the innate immune response. They have recently attracted great interest, since they have antimicrobial activity against a broad spectrum of microorganisms. VmCT1 is a cationic peptide from the venom of Vaejovis mexicanus smithi scorpions, which presents antibacterial activity and tends to helical structures. Its analogs were synthesized, characterized and the conformational studies were performed by circular dichroism...
November 24, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27910791/effects-of-ethyl-acetate-extracts-from-the-polycephalomyces-nipponicus-isolate-cod-mk1201-ascomycetes-against-human-pathogenic-bacteria-and-a-breast-cancer-cell-line
#5
Kusavadee Sangdee, Prapairat Seephonkai, Benjaporn Buranrat, Nilawan Surapong, Aphidech Sangdee
This study aimed to identify a suitable organic solvent for extracting bioactive compounds from Polycephalomyces nipponicus and to evaluate the antibacterial and anticancer activities of the extracts obtained. Only extracts obtained with ethyl acetate exhibited antibacterial activity, so ethyl acetate was chosen for large-scale extraction. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) against Gram-positive and Gram-negative human pathogenic bacteria of the 3 ethyl acetate-derived extracts-ethyl acetate extract from P...
2016: International Journal of Medicinal Mushrooms
https://www.readbyqxmd.com/read/27910702/a-new-isoquinolone-alkaloid-from-an-endophytic-fungus-r22-of-nerium-indicum
#6
Yang-Min Ma, Ke Qiao, Yang Kong, Meng-Yun Li, Lin-Xin Guo, Zhi Miao, Chao Fan
A new isoquinolone alkaloid named 5-hydroxy-8-methoxy-4-phenylisoquinolin-1(2H)-one (3), together with two known quinolinone alkaloids 3-O-methylviridicatin (1) and viridicatol (2) were isolated from the fermentation of an endophytic fungus Penicillium sp. R22 in Nerium indicum. Their structures were elucidated by NMR, IR and MS data, and were also confirmed by comparing with the reported data in the literature. Meanwhile, the antibacterial and antifungal activities of all compounds were tested, and the results showed that three compounds had strong antifungal activity...
December 2, 2016: Natural Product Research
https://www.readbyqxmd.com/read/27910191/tintelnotia-a-new-genus-in-phaeosphaeriaceae-harbouring-agents-of-cornea-and-nail-infections-in-humans
#7
S A Ahmed, W Hofmüller, M Seibold, G S de Hoog, H Harak, I Tammer, A D van Diepeningen, W Behrens-Baumann
Phaeosphaeriaceae is a family in the order Pleosporales containing numerous plant pathogens, endophytes, lichenised fungi, and environmental saprobes. A novel genus, Tintelnotia is introduced containing two species, one of which caused an eye infection and several nail infections in humans. All species of Tintelnotia produce conidia in soft pycnidia with a wide ostiole. The generic type species is T. opuntiae causing necrotic spots on cactus plants. The isolates of the human opportunist T. destructans showed variable susceptibility pattern to a panel of common antifungal agents...
December 1, 2016: Mycoses
https://www.readbyqxmd.com/read/27909995/solithromycin-a-novel-fluoroketolide-for-the-treatment-of-community-acquired-bacterial-pneumonia
#8
REVIEW
George G Zhanel, Erika Hartel, Heather Adam, Sheryl Zelenitsky, Michael A Zhanel, Alyssa Golden, Frank Schweizer, Bala Gorityala, Philippe R S Lagacé-Wiens, Andrew J Walkty, Alfred S Gin, Daryl J Hoban, Joseph P Lynch, James A Karlowsky
Solithromycin is a novel fluoroketolide developed in both oral and intravenous formulations to address increasing macrolide resistance in pathogens causing community-acquired bacterial pneumonia (CABP). When compared with its macrolide and ketolide predecessors, solithromycin has several structural modifications which increase its ribosomal binding and reduce its propensity to known macrolide resistance mechanisms. Solithromycin, like telithromycin, affects 50S ribosomal subunit formation and function, as well as causing frame-shift errors during translation...
December 1, 2016: Drugs
https://www.readbyqxmd.com/read/27909820/genomic-analysis-reveals-the-presence-of-a-class-d-beta-lactamase-with-broad-substrate-specificity-in-animal-bite-associated-capnocytophaga-species
#9
S Zangenah, A F Andersson, V Özenci, P Bergman
Capnocytophga canimorsus and Capnocytophga cynodegmi can be transmitted from cats and dogs to humans, and can cause a wide range of infections including wound infections, sepsis, or endocarditis. We and others recently discovered two new Capnocytophaga species, C. canis and C. stomatis, mainly associated with wound infections. The first-line treatment of animal bite related infections is penicillin, and in case of allergy, doxycycline and trimethoprim/sulfamethoxazole. However, there is a lack of antibiotic susceptibility patterns for animal bite associated Capnocytophaga species...
December 1, 2016: European Journal of Clinical Microbiology & Infectious Diseases
https://www.readbyqxmd.com/read/27909273/-minimally-invasive-coronary-artery-bypass-grafting-using-bilateral-in-situ-internal-thoracic-arteries
#10
Akihiko Yamauchi, Masaki Tabuchi, Shinya Terada, Keita Kikuchi
A 73-year-old male with diabetes mellitius was referred to our hospital for coronary artery bypass grafting (CABG). Preoperative coronary angiography revealed three-vessel coronary disease. Minimally invasive coronary artery grafting (MICS CABG) via left thoracotomy was selected to decrease surgical site infection due to severe diabetes. In situ bilateral internal thoracic arteries (BITA) were harvested using a long type Harmonic scalpel. In situ right internal thorac artery( RITA)-left anterior descending artery (LAD), in situ left internal thorac artery( LITA)-high lateral branch (HL), and aorta-saphenous vein graft (SVG)-#4 posterior descending artery were performed...
December 2016: Kyobu Geka. the Japanese Journal of Thoracic Surgery
https://www.readbyqxmd.com/read/27908580/antimicrobial-activity-of-novel-4h-4-oxoquinolizine-compounds-against-extensively-drug-resistant-acinetobacter-baumannii-strains
#11
Seok Hyeon Na, Hyejin Jeon, Yoo Jeong Kim, Hyo Il Kwon, Gati Noble Selasi, Asiimwe Nicholas, Chang-Soo Yun, Sang Ho Lee, Je Chul Lee
The aim of this study was to screen lead compounds exhibiting potent in vitro antimicrobial activity against multidrug-resistant (MDR) Acinetobacter baumannii strains from a library of chemical compounds. In a high-throughput screening analysis of 7520 compounds representative of 340,000 small molecules, two 4H-4-oxoquinolizine compounds were the most active against A. baumannii ATCC 17978. Subsequent selection and analysis of 70 4H-4-oxoquinolizine compounds revealed that the top 7 compounds were extremely active against extensively drug-resistant (XDR) A...
November 21, 2016: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/27908268/synthesis-of-new-fluoro-benzimidazole-derivatives-as-an-approach-towards-the-discovery-of-novel-intestinal-antiseptic-drug-candidates
#12
Ulviye Acar, Begüm Nurpelin Sağlık, Yusuf Özkay, Zerrin Cantürk, Juan Bueno, Fatih Demirci
In the present study, nineteen new fluoro-benzimidazole derivatives, including nifuroxazide analogues, were synthesized by microwave-supported reactions and tested against a panel of pathogenic microorganisms consisting of resistant strains. The synthesized compounds were characterised and identified by FT-IR, 1H- and 13C-NMR, mass spectroscopy, and elemental analyses, respectively. In vitro antimicrobial and cytotoxic effects of the synthesized compounds were determined by microdilution and by [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] (MTT) assay...
December 1, 2016: Current Pharmaceutical Design
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
#13
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/27907048/chemical-defence-in-a-millipede-evaluation-and-characterization-of-antimicrobial-activity-of-the-defensive-secretion-from-pachyiulus-hungaricus-karsch-1881-diplopoda-julida-julidae
#14
Slaviša Stanković, Ivica Dimkić, Ljubodrag Vujisić, Sofija Pavković-Lučić, Zvezdana Jovanović, Tatjana Stević, Ivana Sofrenić, Bojan Mitić, Vladimir Tomić
The chemical defence of the millipede Pachyiulus hungaricus is reported in the present paper, in which a chemical characterization is given and antimicrobial activity is determined. In total, independently of sex, 44 compounds were identified. All compounds belong to two groups: quinones and pentyl and hexyl esters of long-chain fatty acids. The relative abundances of quinones and non-quinones were 94.7% vs. 5.3% (males) and 87.3% vs. 12.7% (females), respectively. The two dominant quinones in both sexes were 2-methyl-1,4,-benzoquinone and 2-methoxy-3-methyl-1,4-benzoquinone...
2016: PloS One
https://www.readbyqxmd.com/read/27907002/chemical-composition-an-antioxidant-cytotoxic-and-microbiological-activity-of-the-essential-oil-from-the-leaves-of-aeollanthus-suaveolens-mart-ex-spreng
#15
Rosany Lopes Martins, Ranggel Carvalho Simões, Érica de Menezes Rabelo, Ana Luzia Ferreira Farias, Alex Bruno Lobato Rodrigues, Ryan da Silva Ramos, João Batista Fernandes, Lourivaldo da Silva Santos, Sheylla Susan Moreira da Silva de Almeida
Aeollanthus suaveolens species popularly known as catinga de mulata belongs to the Lamiaceae family. In the Amazon region, it is used in folk medicine for the treatment of gastritis, convulsions of epileptic origin, stomach pain and diarrhea in the form of tea and juice. Essential oils have analgesic, anti-inflammatory, and antimicrobial activity. This study evaluated the chemical composition of the A. suaveolens essential oil, and its cytotoxic, antimicrobial and antioxidant activity on Artemia salina Leach...
2016: PloS One
https://www.readbyqxmd.com/read/27906990/surveillance-of-helicobacter-pylori-antibiotic-susceptibility-in-indonesia-different-resistance-types-among-regions-and-with-novel-genetic-mutations
#16
Muhammad Miftahussurur, Ari Fahrial Syam, Iswan Abbas Nusi, Dadang Makmun, Langgeng Agung Waskito, Lukman Hakim Zein, Fardah Akil, Willy Brodus Uwan, David Simanjuntak, I Dewa Nyoman Wibawa, Jimmy Bradley Waleleng, Alexander Michael Joseph Saudale, Fauzi Yusuf, Syifa Mustika, Pangestu Adi, Ummi Maimunah, Hasan Maulahela, Yudith Annisa Ayu Rezkitha, Phawinee Subsomwong, Nasronudin, Dadik Rahardjo, Rumiko Suzuki, Junko Akada, Yoshio Yamaoka
Information regarding Helicobacter pylori antibiotic resistance in Indonesia was previously inadequate. We assessed antibiotic susceptibility for H. pylori in Indonesia, and determined the association between virulence genes or genetic mutations and antibiotic resistance. We recruited 849 dyspeptic patients who underwent endoscopy in 11 cities in Indonesia. E-test was used to determine the minimum inhibitory concentration of five antibiotics. PCR-based sequencing assessed mutations in 23S rRNA, rdxA, gyrA, gyrB, and virulence genes...
2016: PloS One
https://www.readbyqxmd.com/read/27905408/limitations-of-mic-as-sole-metric-of-pharmacodynamic-response-across-the-range-of-antimicrobial-susceptibilities-within-a-single-bacterial-species
#17
Xuesong Wen, Ronette Gehring, Andrea Stallbaumer, Jim E Riviere, Victoriya V Volkova
The minimum inhibitory concentration (MIC) of an antimicrobial drug for a bacterial pathogen is used as a measure of the bacterial susceptibility to the drug. However, relationships between the antimicrobial concentration, bacterial susceptibility, and the pharmacodynamic (PD) inhibitory effect on the bacterial population are more complex. The relationships can be captured by multi-parameter models such as the Emax model. In this study, time-kill experiments were conducted with a zoonotic pathogen Pasteurella multocida and the fluoroquinolone enrofloxacin...
December 1, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27904808/effect-of-common-and-experimental-anti-tuberculosis-treatments-on-mycobacterium-tuberculosis-growing-as-biofilms
#18
James P Dalton, Benedict Uy, Narisa Phummarin, Brent R Copp, William A Denny, Simon Swift, Siouxsie Wiles
Much is known regarding the antibiotic susceptibility of planktonic cultures of Mycobacterium tuberculosis, the bacterium responsible for the lung disease tuberculosis (TB). As planktonically-grown M. tuberculosis are unlikely to be entirely representative of the bacterium during infection, we set out to determine how effective a range of anti-mycobacterial treatments were against M. tuberculosis growing as a biofilm, a bacterial phenotype known to be more resistant to antibiotic treatment. Light levels from bioluminescently-labelled M...
2016: PeerJ
https://www.readbyqxmd.com/read/27904747/comparing-the-disk-diffusion-and-agar-dilution-tests-for-neisseria-gonorrhoeae-antimicrobial-susceptibility-testing
#19
Hsi Liu, Thomas H Taylor, Kevin Pettus, Steve Johnson, John R Papp, David Trees
BACKGROUND: We assessed the validity of testing for antimicrobial susceptibility of clinical and mutant Neisseria gonorrhoeae (GC) isolates by disk diffusion in comparison to agar dilution, and Etest® (bioMerieux, France), respectively, for three third generation extended spectrum cephalosporins (ESC): ceftriaxone (CRO), cefixime (CFX), and cefpodoxime (CPD). METHODS: One hundred and five clinical isolates and ten laboratory-mutants were tested following Clinical Laboratory Standard Institute (CLSI) and manufacturer's standards for each of the three methods...
2016: Antimicrobial Resistance and Infection Control
https://www.readbyqxmd.com/read/27904273/efficacy-and-safety-of-cream-containing-climbazole-piroctone-olamine-for-facial-seborrheic-dermatitis-a-single-center-open-label-split-face-clinical-study
#20
Hae Jeong Youn, Soo Young Kim, Minji Park, Won Hee Jung, Yang Won Lee, Yong Beom Choe, Kyu Joong Ahn
BACKGROUND: Seborrheic dermatitis (SD) is a multifactorial disease; Malassezia species play an important role in its pathogenesis. OBJECTIVE: We aimed to determine whether a cream containing climbazole/piroctone olamine (C/P cream), antifungal agents with expected efficacy against Malassezia species, could improve SD symptoms. METHODS: We instructed 24 patients with mild-to-moderate SD to apply the C/P cream and emollient cream on the right and left sides of the face, respectively, every morning and evening for 4 weeks...
December 2016: Annals of Dermatology
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