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https://www.readbyqxmd.com/read/29792346/synthesis-of-novel-camphene-based-thiosemicarbazones-and-evaluation-of-anti-mycobacterium-tuberculosis-activity
#1
Mariana R P Souza, Narcimário P Coelho, Vanessa P Baldin, Regiane B L Scodro, Rosilene F Cardoso, Cleuza C da Silva, Fábio Vandresen
In this work the aim of study was the synthesis and evaluation of in vitro anti-Mycobacterium tuberculosis activity as well as the cytotoxicity in VERO cells of a series of 17 novel thiosemicarbazones derived from the natural monoterpene (-)-camphene by REMA and MTT methods. Overall, the majority of tested compounds exhibited considerable inhibitory effects on the growth of M. tuberculosis H37 Rv, especially the derivatives 3, 4a-c, 4f, 4i, 4k, 5 and 6a-b. MIC values of 20 tested compounds ranged from 3.9 to > 250 μg/mL...
May 24, 2018: Natural Product Research
https://www.readbyqxmd.com/read/29792329/residual-complexity-does-impact-organic-chemistry-and-drug-discovery-the-case-of-rufomyazine-and-rufomycin
#2
Mary P Choules, Larry L Klein, David C Lankin, James B McAlpine, Sang-Hyun Cho, Jinhua Cheng, Hanki Lee, Joo-Won Suh, Birgit U Jaki, Scott G Franzblau, Guido F Pauli
Residual complexity (RC) involves the impact of subtle but critical structural and biological features on drug lead validation, including unexplained effects related to unidentified impurities. RC commonly plagues drug discovery efforts due to the inherent imperfections of chromatographic separation methods. The new diketopiperazine, rufomyazine (6), and the previously known antibiotic, rufomycin (7), represent a prototypical case of RC that (almost) resulted in the misassignment of biological activity. The case exemplifies that impurities well below the natural abundance of 13 C (1...
May 24, 2018: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/29788329/pharmacokinetic-and-pharmacodynamic-properties-of-metronidazole-in-pediatric-patients-with-acute-appendicitis-a-prospective-study
#3
Jason Child, Xinhui Chen, Rakesh D Mistry, Stig Somme, Christine MacBrayne, Peter L Anderson, Ronald N Jones, Sarah K Parker
Background: Metronidazole is traditionally dosed every 6-8 hours even though in adults it has a long half-life, concentration-dependent killing, and 3-hour postantibiotic effect. Based on this logic, some pediatric hospitals adopted once-daily dosing for appendicitis, despite limited pharmacokinetics-pharmacodynamics (PK/PD) in children. We studied pediatric patients with appendicitis given metronidazole once daily to determine whether this dosing would meet target area under the curve (AUC)/minimum inhibitory concentration (MIC) ratio of ≥70 for Bacteroides fragilis...
May 16, 2018: Journal of the Pediatric Infectious Diseases Society
https://www.readbyqxmd.com/read/29788070/vt-1598-inhibits-the-in-vitro-growth-of-mucosal-candida-strains-and-protects-against-fluconazole-susceptible-and-resistant-oral-candidiasis-in-il-17-signalling-deficient-mice
#4
Timothy J Break, Jigar V Desai, Kelley R Healey, Mukil Natarajan, Elise M N Ferre, Christina Henderson, Adrian Zelazny, Ulrich Siebenlist, Christopher M Yates, Oren J Cohen, Robert J Schotzinger, David S Perlin, Edward P Garvey, Michail S Lionakis
Background: Chronic mucocutaneous candidiasis (CMC) treatment often induces drug resistance, posing long-term challenges. A novel broad-spectrum fungal CYP51 inhibitor, VT-1598, specifically targets fungal CYP51, but not human CYP enzymes. Objectives: To determine the efficacy of VT-1598 in the treatment of oral Candida infection caused by fluconazole-susceptible and -resistant clinical isolates. Methods: The MICs of VT-1598 and fluconazole for 28 Candida isolates recovered from patients with inherited CMC were determined using CLSI M27-A3 and M27-S4 guidelines...
May 16, 2018: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29785610/evaluation-of-strategies-for-the-assessment-of-drug-drug-interactions-involving-cytochrome-p450-enzymes
#5
Jelle Reinen, Martijn Smit, Mira Wenker
BACKGROUND AND OBJECTIVES: Drug-drug interactions (DDIs) can occur when one drug alters the metabolism of another drug. Drug metabolism mediated by cytochrome P450 enzymes (CYPs) is responsible for the majority of metabolism of known drugs and inhibition of CYP enzymes is a well-known cause of DDIs. In the current study, the use of various human liver microsomes (HLM)-based methods to determine occurrence of CYP-mediated metabolism-dependent inhibition (MDI) and possible follow-up studies were evaluated...
May 21, 2018: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29784273/halogenated-trimethoprim-derivatives-as-multidrug-resistant-staphylococcus-aureus-therapeutics
#6
Napon Nilchan, Wanida Phetsang, Taechin Nowwarat, Soraya Chaturongakul, Chutima Jiarpinitnun
Incorporation of halogen atoms to drug molecule has been shown to improve its properties such as enhanced in membrane permeability and increased hydrophobic interactions to its target. To investigate the effect of halogen substitutions on the antibacterial activity of trimethoprim (TMP), we synthesized a series of halogen substituted TMP and tested for their antibacterial activities against global predominant methicillin resistant Staphylococcus aureus (MRSA) strains. Structure-activity relationship analysis suggested a trend in potency that correlated with the ability of the halogen atom to facilitate in hydrophobic interaction to saDHFR...
May 19, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29779778/identification-of-tb-e12-as-a-novel-ftsz-inhibitor-with-anti-tuberculosis-activity
#7
Yuan Lin, Hongjuan Zhang, Ningyu Zhu, Xia Wang, Yanxing Han, Minghua Chen, Jiandong Jiang, Shuyi Si
The global pandemic of multidrug-resistant (MDR) Mycobacterium tuberculosis (TB) drives for more effective anti-TB drugs with new drug target. Filamentous temperature sensitive protein Z (FtsZ), a GTP dependent prokaryotic cell division protein, forms a dynamic Z-ring in the center of the cell. Differences between bacterial FtsZ and eukaryotic tubulin make FtsZ a highly attractive drug target. In this study, we used phenotype screening of M. smegmatis and model screening targeting M. tuberculosis FtsZ (Mtb-FtsZ) to identify a hit compound TB-E12...
May 2018: Tuberculosis
https://www.readbyqxmd.com/read/29778528/molecular-modeling-synthesis-antibacterial-and-cytotoxicity-evaluation-of-sulfonamide-derivatives-of-benzimidazole-indazole-benzothiazole-and-thiazole
#8
Farha Naaz, Ritika Srivastava, Anuradha Singh, Nidhi Singh, Rajesh Verma, Vishal K Singh, Ramendra K Singh
A new series of heterocyclic molecules bearing sulfonamide linkage has been synthesized and screened for antibacterial activity. During antibacterial screening using broath dilution method, molecules were found to be highly active (MIC value 50-3.1 µg/mL) against different human pathogens, namely B. cerus, S. aureus, E. coli and P. aeruginosa, and most effective against E. coli. A great synergistic effect was observed during determination of FIC where molecules were used in combination with reference drugs chloramphenicol and sulfamethoxazole...
May 11, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29778180/pharmacokinetic-pharmacodynamic-assessment-of-cefquinome-against-actinobacillus-pleuropneumoniae-in-a-piglet-tissue-cage-infection-model
#9
Longfei Zhang, Xun Wu, Zilong Huang, Nan Zhang, Yuzhi Wu, Qinren Cai, Xiangguang Shen, Huanzhong Ding
To evaluate the relationship between the pharmacokinetic/pharmacodynamic (PK/PD) parameters and the antibacterial effect of cefquinome against Actinobacillus pleuropneumoniae, a tissue cage infection model was established in piglets. In this model, an initial count of A. pleuropneumoniae of approximately 106 CFU/mL was exposed to different concentrations of cefquinome after multiple administration at dosages of 0.2, 0.4, 0.8, 1, 2, 4 mg/kg body weight once a day for 3 days. Concentration of cefquinome and bacterial numbers of A...
June 2018: Veterinary Microbiology
https://www.readbyqxmd.com/read/29777023/xanthates-metabolism-by-flavoprotein-containing-monooxygenases-fmo-and-antimycobacterial-activity
#10
Stanislav Yanev, Tsveta Stoyanova, Violeta Valcheva, Paul R Ortiz De Montellano
Ethionamide (ETH) plays a central role in the treatment of tuberculosis in patients resistant to the first-line drugs. The ETH, thioamide, and thiourea class of antituberculosis agents are pro-drugs that are oxidatively converted to their active S-oxides by the flavin monooxygenase EtaA of M. tuberculosis, thus initiating the chain of reactions that result in inhibition of mycolic acid biosynthesis and cell lysis. As part of a search for new lead candidates, we report here that several xanthates are oxidized by purified EtaA to S-oxide metabolites (perxanthates) that are implicated in the antimycobacterial activity of these compounds...
May 18, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29774093/distribution-of-virulence-associated-genes-and-antimicrobial-susceptibility-in-clinical-acinetobacter-baumannii-isolates
#11
Chao Liu, Yaowen Chang, Ying Xu, Yun Luo, Linrong Wu, Zhanjun Mei, Shigang Li, Rui Wang, Xu Jia
Acinetobacter baumannii is undoubtedly one of the most clinically significant pathogens. The multidrug resistance and virulence potential of A. baumannii are responsible for hospital-acquired nosocomial infections. Unlike numerous investigations on the drug-resistant epidemiology of A. baumanni , virulence molecular epidemiology is less studied. Here, we collected 88 A. baumannii clinical isolates, tested their antimicrobial susceptibility to 10 commonly used antibiotics and analyzed the distribution of 9 selected virulence-associated genes, aims to investigate the primary characteristics of the virulence-associated genes that exist in clinically multidrug resistant (MDR) and non-MDR isolates of A...
April 24, 2018: Oncotarget
https://www.readbyqxmd.com/read/29769064/antimicrobial-and-antioxidant-activities-of-triterpenoid-and-phenolic-derivatives-from-two-cameroonian-melastomataceae-plants-dissotis-senegambiensis-and-amphiblemma-monticola
#12
Raissa Tioyem Nzogong, Fabrice Sterling Tchantchou Ndjateu, Steve Endeguele Ekom, Jules-Arnaud Mboutchom Fosso, Maurice Ducret Awouafack, Mathieu Tene, Pierre Tane, Hiroyuki Morita, Muhammad Iqbal Choudhary, Jean-de-Dieu Tamokou
BACKGROUND: Antimicrobial resistance is a serious threat against humankind and the search for new therapeutics is needed. This study aims to investigate the antimicrobial and antioxidant activities of ethanol extracts and compounds isolated from Dissotis senegambiensis and Amphiblemma monticola, two Cameroonian Melastomataceae species traditionally used for the treatment of fever, malaria and infectious diseases. METHODS: The plant extracts were prepared by maceration in ethanol...
May 16, 2018: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/29765644/identification-of-potent-chromone-embedded-1-2-3-triazoles-as-novel-anti-tubercular-agents
#13
Viswanadh Nalla, Aslam Shaikh, Sanket Bapat, Renu Vyas, M Karthikeyan, P Yogeeswari, D Sriram, M Muthukrishnan
A series of 20 novel chromone embedded [1,2,3]-triazoles derivatives were synthesized via an easy and convenient synthetic procedure starting from 2-hydroxy acetophenone. The in vitro anti-mycobacterial evaluation studies carried out in this work reveal that seven compounds exhibit significant inhibition against Mycobacterium tuberculosis H37Rv strain with MIC in the range of 1.56-12.5 µg ml-1 . Noticeably, compound 6s was the most potent compound in vitro with a MIC value of 1.56 µg ml-1 . Molecular docking and chemoinformatics studies revealed that compound 6s displayed drug-like properties against the enoyl-acyl carrier protein reductase of M...
April 2018: Royal Society Open Science
https://www.readbyqxmd.com/read/29765372/is-iqg-607-a-potential-metallodrug-or-metallopro-drug-with-a-defined-molecular-target-in-mycobacterium-tuberculosis
#14
REVIEW
Bruno L Abbadi, Valnês da Silva Rodrigues-Junior, Adilio da Silva Dadda, Kenia Pissinate, Anne D Villela, Maria M Campos, Luiz G de França Lopes, Cristiano V Bizarro, Pablo Machado, Eduardo H S Sousa, Luiz A Basso
The emergence of strains of Mycobacterium tuberculosis resistant to isoniazid (INH) has underscored the need for the development of new anti-tuberculosis agents. INH is activated by the mycobacterial katG -encoded catalase-peroxidase, forming an acylpyridine fragment that is covalently attached to the C4 of NADH. This isonicotinyl-NAD adduct inhibits the activity of 2- trans -enoyl-ACP(CoA) reductase (InhA), which plays a role in mycolic acid biosynthesis. A metal-based INH analog, Na3 [FeII (CN)5 (INH)]·4H2 O, IQG-607, was designed to have an electronic redistribution on INH moiety that would lead to an intramolecular electron transfer to bypass KatG activation...
2018: Frontiers in Microbiology
https://www.readbyqxmd.com/read/29761517/pharmacokinetics-of-intravenous-gentamicin-in-healthy-young-adult-compared-to-aged-alpacas
#15
A Gestrich, D Bedenice, M Ceresia, I Zaghloul
The study objective was to evaluate the effects of age on aminoglycoside pharmacokinetics in eight young-adult (<4 years) and eight aged (≥14 years) healthy alpacas, receiving a single 6.6 mg/kg intravenous gentamicin injection. Heparinized plasma samples were obtained at designated time points following drug administration and frozen at -80°C until assayed by a validated immunoassay (QMS® ). Compartmental and noncompartmental analyses of gentamicin plasma concentrations versus time were performed using WinNonlin (v6...
May 14, 2018: Journal of Veterinary Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29760684/bioprospecting-deep-sea-actinobacteria-for-novel-anti-infective-natural-products
#16
Dongbo Xu, Linna Han, Chunhui Li, Qi Cao, Duolong Zhu, Nolan H Barrett, Dedra Harmody, Jing Chen, Haining Zhu, Peter J McCarthy, Xingmin Sun, Guojun Wang
The global prevalence of drug resistance has created an urgent need for the discovery of novel anti-infective drugs. The major source of antibiotics in current clinical practice is terrestrial actinobacteria; the less-exploited deep-sea actinobacteria may serve as an unprecedented source of novel natural products. In this study, we evaluated 50 actinobacteria strains derived from diverse deep water sponges and environmental niches for their anti-microbial activities against a panel of pathogens including Candida albicans , Clostridium difficile , Staphylococcus aureus , and methicillin-resistant S...
2018: Frontiers in Microbiology
https://www.readbyqxmd.com/read/29760140/evolution-of-antibiotic-resistance-in-biofilm-and-planktonic-p-aeruginosa-populations-exposed-to-sub-inhibitory-levels-of-ciprofloxacin
#17
Marwa N Ahmed, Andreas Porse, Morten Otto Alexander Sommer, Niels Høiby, Oana Ciofu
The opportunistic Gram-negative pathogen Pseudomonas aeruginosa , known for its intrinsic and acquired antibiotic resistance, has a notorious ability to form biofilms, which often facilitate chronic infections. The evolutionary paths to antibiotic resistance have mainly been investigated in planktonic cultures and are less studied in biofilms. We experimentally evolved P. aeruginosa PAO1 colony-biofilms and stationary-phase planktonic cultures for seven passages in the presence of sub-inhibitory levels (0.1 mg/L) of ciprofloxacin (CIP) and performed a genotypic (whole bacterial population sequencing) and phenotypic assessment of the populations...
May 14, 2018: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29758185/elucidating-the-bactericidal-mechanism-of-action-of-the-linear-antimicrobial-tetrapeptide-brbr-nh-2
#18
Qiu Ying Lau, Jianguo Li, Marc-Antoine Sani, Sheetal Sinha, Yan Li, Fui Mee Ng, CongBao Kang, Surajit Bhattacharjya, Frances Separovic, Chandra Verma, Cheng San Brian Chia
Linear antimicrobial peptides, with their rapid bactericidal mode of action, are well-suited for development as topical antibacterial drugs. We recently designed a synthetic linear 4-residue peptide, BRBR-NH2 , with potent bactericidal activity against Staphylococcus aureus (MIC 6.25 μM), the main causative pathogen of human skin infections with an unknown mechanism of action. Herein, we describe a series of experiments conducted to gain further insights into its mechanism of action involving electron microscopy, artificial membrane dye leakage, solution- and solid-state NMR spectroscopy followed by molecular dynamics simulations...
May 11, 2018: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/29753132/prevention-of-eskape-pathogen-biofilm-formation-by-antimicrobial-peptides-wlbu2-and-ll37
#19
Qiao Lin, Berthony Deslouches, Ronald C Montelaro, Y Peter Di
OBJECTIVES: Bacterial biofilm-dependent infections (e.g., cystic fibrosis, surgical sites, and medical implants) are associated with enhanced drug-resistance and thus difficult to eradicate. The goal of this study was to systematically compare three distinct classes of antimicrobial peptides (AMPs) that include the clinically used antibiotic colistin, the natural AMP LL37, the engineered cationic-AMP WLBU2, and four commonly used antibiotics with different bactericidal mechanisms (tobramycin, ciprofloxacin, ceftazidime and vancomycin) for biofilm prevention properties...
May 9, 2018: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/29746997/transcriptional-analysis-reveals-the-critical-role-of-rna-polymerase-binding-transcription-factor-dksa-in-regulating-multi-drug-resistance-of-escherichia-coli
#20
Jiawei Wang, Li Cao, Xiaowen Yang, Qingmin Wu, Lin Lu, Zhen Wang
The objective of this study was to comprehensively identify the target genes regulated by the RNA polymerase-binding transcription factor DksA in Escherichia coli, and to clarify the role of DksA in multi-drug resistance. A clinical E. coli strain, E8, was selected to construct the dksA gene deletion mutant by using the Red recombination system. The minimum inhibitory concentrations (MICs) of 12 antibiotics in the E8ΔdksA (mutant) were markedly lower than those in the wild-type strain, E8. Genes differentially expressed in the wild-type and dksA mutant were detected using RNA-Seq and were validated by performing quantitative real-time PCR (qRT-PCR)...
May 7, 2018: International Journal of Antimicrobial Agents
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