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https://www.readbyqxmd.com/read/28436655/investigating-the-antibacterial-activity-of-biphenylthiazoles-against-methicillin-and-vancomycin-resistant-staphylococcus-aureus-mrsa-and-vrsa
#1
Mohamed Hagras, Haroon Mohammad, Mohamed S Mandour, Youssef A Hegazy, Adel Ghiaty, Mohamed N Seleem, Abdelrahman S Mayhoub
Phenylthiazoles were reported previously as a new scaffold with antibacterial activity against an array of multidrug-resistant staphylococci. However, their promising antibacterial activity was hampered in large part by their short half-life due to excessive hepatic clearance. Close inspection of the structure-activity-relationships (SAR) of the phenylthiazoles revealed two important structural features necessary for antibacterial activity (a nitrogenous and a lipophilic component). Incorporating the nitrogenous part within a pyrimidine ring resulted in analogues with a prolonged half-life, while the biphenyl moiety revealed the most potent analogue 1b...
April 24, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28435351/in-vitro-antifungal-activity-of-1-n-2-methoxybenzyl-1-10-phenanthrolinium-bromide-against-candida-albicans-and-its-effects-on-membrane-integrity
#2
Setiawati Setiawati, Titik Nuryastuti, Ngatidjan Ngatidjan, Mustofa Mustofa, Jumina Jumina, Dhina Fitriastuti
Metal-based drugs, such as 1,10-phenanthroline, have demonstrated anticancer, antifungal and antiplasmodium activities. One of the 1,10-phenanthroline derivatives compounds (1)-N-2-methoxybenzyl-1,10-phenanthrolinium bromide (FEN), which has been demonstrated an inhibitory effect on the growth of Candida spp. This study aimed to explore the in vitro antifungal activity of FEN and its effect on the membrane integrity of Candida albicans. The minimum inhibitory concentration (MIC) and the minimum fungicidal concentration (MFC) of FEN against planktonic C...
March 2017: Mycobiology
https://www.readbyqxmd.com/read/28435070/siderophores-in-clinical-isolates-of-klebsiella-pneumoniae-promote-ciprofloxacin-resistance-by-inhibiting-the-oxidative-stress
#3
Wenli Zhang, Ying Zhang, Xinxin Wang, Fengshu Ding, Yingmei Fu, Jizi Zhao, Wuqi Song, Ogutu James Opiyo, Fengmin Zhang, Xiaobei Chen
To explore the relevance of and understand the potential mechanisms behind the production of siderophores by clinical isolates of K. pneumoniae and ciprofloxacin (CIP) resistance, we divided the K. pneumoniae isolates into two groups based on bacterial siderophores productin: high siderophore-yielding group (39 strains) and low siderophore-yielding group (38 strains). The rate of CIP resistance in K. pneumoniae (27/39 = 69.23%) from the high siderophore-yielding group was significantly higher than that (16/38 = 42...
April 20, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28429168/bedaquiline-susceptibility-test-for-totally-drug-resistant-tuberculosis-mycobacterium-tuberculosis
#4
Ji-Chan Jang, Yong-Gyun Jung, Jungil Choi, Hyunju Jung, Sungweon Ryoo
This study aimed to provide information that bedaquilline is significantly effective for treatment of totally drug resistant (TDR) Mycobacterium tuberculosis that shows resistant to all first- and second-line drugs-using an innovative disc agarose channel (DAC) system. Time-lapse images of single bacterial cells under culture conditions with different concentrations of bedaquiline were analysed by image processing software to determine minimum inhibitory concentrations (MICs). Bedaquiline inhibited the growth of TDR M...
April 20, 2017: Journal of Microbiology / the Microbiological Society of Korea
https://www.readbyqxmd.com/read/28428773/mutation-at-g103-of-mtbftsz-altered-their-sensitivity-to-coumarins
#5
Duggirala Sridevi, Karpagam U Sudhakar, Ragamanvitha Ananthathatmula, Rakesh P Nankar, Mukesh Doble
Coumarins are natural polyphenol lactones comprising of fused rings of benzene and α-pyrone. The current study demonstrates the inhibitory effect of coumarins with various substitutions on Mycobacterium smegmatis mc(2) 155. We also demonstrate the effect of pomegranate (Punica granatum) extract containing ellagic acid, on M. smegmatis as well as their affect on MtbFtsZ (FtsZ from Mycobacterium tuberculosis). The ellagic acid extracts from pomegranate peels inhibit mycobacteria with a MIC of 25 μM and 0.3 to 3...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28427794/occurrence-of-a-novel-class-1-integron-harboring-qnrvc4-in-salmonella-rissen
#6
Sirirat Luk-In, Chaiwat Pulsrikarn, Aroon Bangtrakulnonth, Tanittha Chatsuwan, Wanla Kulwichit
We described qnrVC4 in S. Rissen 166ANSS50, a swine isolate, which was detected in the study on quinolone resistance mechanisms of nontyphoidal Salmonella in Thailand. The isolate was found to harbor a ̴17-kb non-conjugative plasmid carrying qnrVC4 within 8.91kb of a novel In4-like class 1 integron (In805). It contained the multi-drug resistance gene cassettes of qnrVC4-qacH4-aacA4-cmlA7-blaOXA-10-aadA1-dfrA14 and unusual 3'-CS of mobC-IS6100. This 1014-bp qnrVC4 cassette included with promoter (PqnrVC4: -35 TTGAGA and -10 TAGTCT) showed high homology with qnrVC4 in superintegron of V...
March 31, 2017: Diagnostic Microbiology and Infectious Disease
https://www.readbyqxmd.com/read/28427461/inhibitory-activities-of-selected-sudanese-medicinal-plants-on-porphyromonas-gingivalis-and-matrix-metalloproteinase-9-and-isolation-of-bioactive-compounds-from-combretum-hartmannianum-schweinf-bark
#7
Ebtihal Abdalla M Mohieldin, Ali Mahmoud Muddathir, Tohru Mitsunaga
BACKGROUND: Periodontal diseases are one of the major health problems and among the most important preventable global infectious diseases. Porphyromonas gingivalis is an anaerobic Gram-negative bacterium which has been strongly implicated in the etiology of periodontitis. Additionally, matrix metalloproteinases-9 (MMP-9) is an important factor contributing to periodontal tissue destruction by a variety of mechanisms. The purpose of this study was to evaluate the selected Sudanese medicinal plants against P...
April 20, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28423019/design-synthesis-and-structure-activity-relationship-study-of-wollamide-b-a-new-potential-anti-tb-agent
#8
Henok Asfaw, Katja Laqua, Anna Maria Walkowska, Fraser Cunningham, Maria Santos Martinez-Martinez, Juan Carlos Cuevas-Zurita, Lluís Ballell-Pages, Peter Imming
Wollamide B is a cationic antimycobacterial cyclohexapeptide that exhibits activity against Mycobacterium bovis (M. bovis) (IC50 of 3.1 μM). Aiming to define its structural activity relationship (SAR), optimizing potency and pharmacokinetic properties, libraries of analogues were synthesized following a standard Fmoc-based solid phase peptide synthesis approach. The antimycobacterial activities of wollamide B and all the synthesized analogues were tested against Mycobacterium tuberculosis (Mtb) H37Rv. Parallely, in vitro drug metabolism and pharmacokinetic (ADME) profiling was done for the synthesized compounds to evaluate their drug likeness...
2017: PloS One
https://www.readbyqxmd.com/read/28420136/discovery-of-an-octahedral-silicon-complex-as-a-potent-antifungal-agent
#9
Chen Fu, Bin Fu, Xixi Peng, Guojian Liao
Octahedral transition metal complexes have been shown to have tremendous applications in chemical biology and medicinal chemistry. Meanwhile, structural transition metals can be replaced by inert octahedral silicon in a proof-of-principle study. We here introduce the first example of octahedral silicon complexes, which can very well serve as an efficient antimicrobial agent. The typical silicon arenediolate complex 1 {[(phen)₂Si(OO)](PF₆)₂, with phen = 1,10-phenanthroline, OO = 9,10-phenanthrenediolate} exhibited significant inhibition towards the growth of Cryptococcus neoformans with MIC and MFC values of 4...
April 15, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28417524/biofilms-of-candida-spp-from-the-ocular-conjunctiva-of-horses-with-reduced-azole-susceptibility-a-complicating-factor-for-the-treatment-of-keratomycosis
#10
Raimunda Sâmia Nogueira Brilhante, Paula Vago Bittencourt, Débora de Souza Collares Castelo-Branco, Glaucia Morgana de Melo Guedes, Jonathas Sales de Oliveira, Lucas Pereira Alencar, Rossana de Aguiar Cordeiro, Mariana Pinheiro, Evilázio Fernandes Nogueira-Filho, Waldemiro de Aquino Pereira-Neto, José Júlio Costa Sidrim, Marcos Fábio Gadelha Rocha
OBJECTIVES: This study aimed to assess the biofilm-forming ability of Candida spp. from the ocular conjunctiva of horses and to investigate the antifungal susceptibility of these biofilms. PROCEDURES: Initially, the biofilm-forming ability of 15 strains was assessed by crystal violet staining, which reveals the fungal biomass adhered to the polystyrene plates, and scanning electron microscopy. Then, the minimum inhibitory concentrations (MICs) of amphotericin B, fluconazole, itraconazole, and caspofungin were initially determined against strains in planktonic form...
April 18, 2017: Veterinary Ophthalmology
https://www.readbyqxmd.com/read/28416553/pharmacokinetics-and-dialytic-clearance-of-ceftazidime-avibactam-in-a-critically-ill-patient-on-continuous-venovenous-hemofiltration
#11
Eric Wenzler, Kristen L Bunnell, Susan C Bleasdale, Scott Benken, Larry H Danziger, Keith A Rodvold
Ceftazidime-avibactam 1.25 g every 8 hours was used to treat multi-drug resistant Pseudomonas aeruginosa bacteremia in a critically ill patient on continuous venovenous hemofiltration (CVVH). Pre-filter plasma drug concentrations of ceftazidime and avibactam were measured at 0, 1, 2, 4, 6, and 8 hours along with post-filter and ultrafiltrate concentrations at hours 2 and 6. Plasma pharmacokinetic parameters of ceftazidime and avibactam, respectively, were Cmax 61.10 and 14.54 mg/L, Cmin 31.96 and 8.45 mg/L, t1/2 6...
April 17, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28416552/in-vivo-pharmacodynamic-target-assessment-of-eravacycline-against-escherichia-coli-in-a-murine-thigh-infection-model
#12
Miao Zhao, Alexander J Lepak, Karen Marchillo, Jamie VanHecker, David R Andes
Eravacycline is a novel fluorocycline antibiotic with potent activity against a broad range of pathogens, including strains with tetracycline and other drug-resistance phenotypes. The goal of the studies was to determine which pharmacokinetic/pharmacodynamic (PK/PD) parameter and magnitude best correlated with efficacy in the murine thigh infection model. Six E. coli were utilized for the studies. MICs were determined using CLSI methods and ranged from 0.125 to 0.25 mg/L. A neutropenic murine thigh infection model was utilized for all treatment studies...
April 17, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28416551/comparative-pharmacodynamics-of-telavancin-and-vancomycin-in-the-neutropenic-murine-thigh-and-lung-infection-models-against-staphylococcus-aureus
#13
Alexander J Lepak, Miao Zhao, David R Andes
The pharmacodynamics of telavancin and vancomycin were compared using neutropenic murine thigh and lung infection models. Four S. aureus strains were included. The telavancin MIC ranged from 0.06 - 0.25 mg/L and vancomycin MIC from 1 - 4 mg/L. Plasma pharmacokinetics of escalating doses (1.25, 5, 20 and 80 mg/kg) of telavancin and vancomycin were linear over the dose range. Epithelial lining fluid (ELF) pharmacokinetics for each drug revealed penetration into the ELF mirrored the percent free fraction (not protein bound) in plasma for each drug...
April 17, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28415444/formulation-of-thermoreversible-gel-of-cranberry-juice-concentrate-evaluation-biocompatibility-studies-and-its-antimicrobial-activity-against-periodontal-pathogens
#14
Rajeshwari H R, Dinesh Dhamecha, Satveer Jagwani, Dhanashree Patil, Satisha Hegde, Raksha Potdar, Renuka Metgud, Sunil Jalalpure, Subarna Roy, Kiran Jadhav, Neeraj Kumar Tiwari, Sravani Koduru, Shweta Hugar, Suneel Dodamani
The present work aims to investigate the efficacy of thermoreversible gel of cranberry juice concentrate (CJC) as local drug delivery for the treatment of periodontitis. CJC was initially tested for its antimicrobial activities like MIC, MBC, antiadhesion, antibiofilm and time kill assay against the panel of organisms (S. mutans (SM), E. faecalis (EF), A. actinomycetemcomitans (AA), P. gingivalis (PG), T. forsythia (TF)) responsible for periapical and periodontal infections. Antimicrobial activity of CJC showed MIC value of 50mg/ml and MBC value of 100mg/ml with desirable antiadhesion (83-90%) and antibiofilm activity (70-85%)...
June 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28413506/active-efflux-pump-adeb-is-involved-in-multidrug-resistance-of-acinetobacter-baumannii-induced-by-antibacterial-agents
#15
Tingting Zhang, Min Wang, Yixin Xie, Xianping Li, Zhihui Dong, Yanhua Liu, Ling Wang, Min Yang, Huan Song, Hong Cao, Wei Cao
The aim of the present study was to investigate the resistance of Acinetobacter baumannii, which was induced by cefepime (FEP), cefoperazone-sulbactam (SCF), tazobactam (TZP), levofloxacin (LEV), amikacin (AK), imipenem (IPM), and ciprofloxacin (CIP), in vitro. Multi-step drug resistance selection of 16 A. baumannii strains was performed using seven antibacterial agents (FEP, TZP, CIP, AK, IPM, SCF, and LEV). The minimum inhibitory concentration (MIC) was determined using the agar dilution method. Random amplified polymorphic DNA polymerase chain reaction was performed to analyze the genotypes and the carrying rates of aac(3)-I, aac(6')-I, ant(3)-I, aph(3)-Via, OXA-23, OXA-24, AmpC, TEM-1, metallo-β-lactamase gene (IMP), armA, rmtA, rmtB, parC, gyrA and adeB...
April 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28413476/the-mechanism-of-human-%C3%AE-defensin-3-in-mrsa-induced-infection-of-implant-drug-resistant-bacteria-biofilm-in-the-mouse-tibial-bone-marrow
#16
Chen Zhu, Ni-Rong Bao, Shuo Chen, Jian-Ning Zhao
The mechanism of human β-defensin 3 (HBD-3) in methicillin-resistant Staphylococcus aureus (MRSA-induced infection of implant drug-resistant bacteria biofilm in the mouse tibial bone marrow was studied. Healthy adult male Sprague-Dawley rats with average weight of 230 g were selected to construct the infection model of MRSA-induced implant drug-resistant bacteria biofilm in the mouse left tibial bone marrow. The drugs were intraperitoneally injected after 24 h medullary cavity infection, and the experimental groups included the model group, HBD-3 group, and vancomycin group (20 rats in each group)...
April 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28411559/synthesis-and-antimycobacterial-screening-of-new-thiazolyl-oxazole-derivatives
#17
Yogita K Abhale, Amit V Sasane, Abhijit P Chavan, Saddam Husen Shekh, Keshav K Deshmukh, Sujit Bhansali, Laxman Nawale, Dhiman Sarkar, Pravin C Mhaske
In the present study a series of 4-methyl-2-aryl-5-(2-aryl/benzyl thiazol-4-yl) oxazole (4a-v) have been synthesized and evaluated for their preliminary antitubercular, antimicrobial and cytotoxicity activity. Among all the synthesized compounds, 4v reported comparable activity against dormant M. tuberculosis H37Ra and M. bovis BCG strains with respect to standard drug rifampicin. The active compounds from the antitubercular study were further tested for anti-proliferative activity against HeLa, A549 and PANC-1 cell lines using MTT assay and showed no significant cytotoxic activity at the maximum concentration evaluated...
March 28, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28403782/synthesis-cytotoxicity-and-antimicrobial-activity-of-new-enmein-type-kauranoid-diterpenoid-derivatives
#18
Dahong Li, Tong Han, Xu Hu, Kangtao Tian, Shengtao Xu, Tingting Zhou, Keguang Cheng, Zhanlin Li, Huiming Hua, Jinyi Xu
Eleven new enmein-type diterpenoid derivatives with different substituents and drug-like properties were designed and synthesized. The antimicrobial activities against E. coli, S. aureus, B. subtilis and M. albicans were disclosed. The results revealed that enmein-type diterpenoids showed more promising activities against tested gram-positive bacteria than gram-negative bacterium and fungus. Compound 9 with R of 2-quinolyl group exhibited the strongest antimicrobial activities with MIC values of 7.81 μg/ml and 0...
April 12, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28398220/antibiotic-loaded-mos-sub-2-sub-nanosheets-to-combat-bacterial-resistance-via-biofilms-inhibition
#19
Xu Zhang, Wentao Zhang, Lizhi Liu, Mei Yang, Lunjie Huang, Kai Chen, Rong Wang, Baowei Yang, Daohong Zhang, Jianlong Wang
The emergence of antibiotic resistance has resulted in an increasing difficulty treating clinical infections associated with biofilms formation, one of the key processes contributed to enhance antibiotic resistance in return. With the rapid development of nanotechnology, a new way to overcome antibiotic resistance was opened up. Based on multiple properties especially antibacterial potential of MoS<sub>2</sub> nanosheets that have aroused wide attention, herein, a novel antimicrobial agent to combat resistant gram-positive <i>Staphylococcus aureus (S...
April 11, 2017: Nanotechnology
https://www.readbyqxmd.com/read/28396549/in-vivo-pharmacokinetics-and-pharmacodynamics-of-zti-01-fosfomycin-for-injection-in-the-neutropenic-murine-thigh-infection-model-against-e-coli-k-pneumoniae-and-p-aeruginosa
#20
Alexander J Lepak, Miao Zhao, Brian VanScoy, Daniel S Taylor, Evelyn Ellis-Grosse, Paul G Ambrose, David R Andes
Fosfomycin is a broad-spectrum agent with activity against gram-positive and gram-negative bacteria, including drug-resistant strains, such as extended spectrum beta-lactamase (ESBL)-producing and carbapenem-resistant (CR) gram-negative rods. In the present study, the pharmacokinetic/pharmacodynamic (PK/PD) activity of ZTI-01 (fosfomycin for injection) was evaluated in the neutropenic murine thigh infection model against 5 E. coli (EC), 3 K. pneumoniae (KPN), and 2 P. aeruginosa (PSA) strains, including a subset with ESBL and CR phenotype...
April 10, 2017: Antimicrobial Agents and Chemotherapy
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