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drug MIC

Diego G Ghiano, Agustina de la Iglesia, Nina Liu, Peter J Tonge, Héctor R Morbidoni, Guillermo R Labadie
A collection of 1,2,3-triazoles unsaturated fatty acid mimics were efficiently synthesized by click chemistry. The 1,4-disubstituted analogs prepared covered different alkyl chain lengths and triazole positions. The compounds were subsequently tested against Mycobacterium tuberculosis, being most of them active with some of the analogs displaying activity at micromolar concentration. The most potent member of the series has the triazole moiety on the C-2 position with a carbon chain of eight or ten carbon atoms...
September 28, 2016: European Journal of Medicinal Chemistry
Kunal Zaveri, Kiranmayi Patnala
BACKGROUND: The prevalence of multi-drug resistance S. aureus is one most challenging task for treatment of nosocomial infections. Proteins and enzymes of peptidoglycan biosynthesis pathway are one among the well-studied targets, but many of the enzymes are unexplored as targets. MurE is one such enzyme featured to be a promising target. As MurE plays an important role in ligating the L-lys to stem peptide at third position that is crucial for peptidoglycan synthesis. OBJECTIVE: To screen the potential MurE inhibitor...
October 10, 2016: Current Computer-aided Drug Design
Andrés Felipe Cartagena, Luís Antonio Esmerino, Rogerio Polak-Junior, Sibelli Olivieri Parreiras, Milton Domingos Michél, Paulo Vitor Farago, Nara Hellen Campanha
OBJECTIVE: The purpose of this study was to develop a new oral drug delivery system by incorporating polymeric miconazole nitrate (MN) microparticles on an experimental antifungal denture adhesive (DA). METHODS: Spray drying Eudragit L-100 (E) and Gantrez MS-955 (G) MN-microparticles were incorporated in DA. DAE1, DAG1, DAEG1, DAE2, DAG2, DAEG2 groups were obtained from the combination of polymers used in MN-microparticles (E, G and EG) and concentration of MN into DA (1, for 1% and 2, for 2%)...
October 10, 2016: Dental Materials: Official Publication of the Academy of Dental Materials
Susanne Paukner, Rosemarie Riedl
Pleuromutilins are antibiotics that selectively inhibit bacterial translation and are semisynthetic derivatives of the naturally occurring tricyclic diterpenoid pleuromutilin, which received its name from the pleuromutilin-producing fungus Pleurotus mutilus Tiamulin and valnemulin are two established derivatives in veterinary medicine for oral and intramuscular administration. As these early pleuromutilin drugs were developed at a time when companies focused on major antibacterial classes, such as the β-lactams, and resistance was not regarded as an issue, interest in antibiotic research including pleuromutilins was limited...
October 14, 2016: Cold Spring Harbor Perspectives in Medicine
Shashikant Srivastava, Devyani Deshpande, Jotam Pasipanodya, Eric Nuermberger, Soumya Swaminathan, Tawanda Gumbo
BACKGROUND:  When treated with the same antibiotic dose, children achieve different 0- to 24-hour area under the concentration-time curves (AUC0-24) because of maturation and between-child physiological variability on drug clearance. Children are also infected by Mycobacterium tuberculosis isolates with different antibiotic minimum inhibitory concentrations (MICs). Thus, each child will achieve different AUC0-24/MIC ratios when treated with the same dose. METHODS:  We used 10 000-subject Monte Carlo experiments to identify the oral doses of linezolid, moxifloxacin, and faropenem that would achieve optimal target exposures associated with optimal efficacy in children with disseminated tuberculosis...
November 1, 2016: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
Abrar K Thabit, Jared L Crandon, David P Nicolau
Increasing antimicrobial resistance in community-acquired pneumonia (CAP) pathogens has contributed to infection-related morbidity and mortality. Delafloxacin is a novel fluoroquinolone with broad-spectrum activity against Gram-positive and -negative organisms, including Streptococcus pneumoniae and methicillin-resistant Staphylococcus aureus (MRSA). This study aimed to define the pharmacodynamic profile of delafloxacin against CAP pathogens using a neutropenic murine lung infection model. Five S. pneumoniae, 2 methicillin-susceptible S...
September 29, 2016: International Journal of Antimicrobial Agents
Juliana Hotta, Wilson Gustavo Cral, Vinicius Tatsuyuji Sakima, Vanessa Soares Lara, Vanessa Migliorini Urban, Karin Hermana Neppelenbroek
BACKGROUND: Antifungal agents incorporated into temporary denture resilient liners as drug carries and delivery have been suggested as an alternative treatment for denture stomatitis. However, to test the in vivo biocompatibility of this protocol, standardization of an intraoral device for optimal drug delivery is required. OBJECTIVE: Standardized criteria were produced to adjust an acrylic intraoral device (IOD) for rats feasible for denture stomatitis treatment by sustained drug-delivery based on minimal inhibitory drug concentrations (MICs) of antifungals for Candida albicans biofilm...
October 13, 2016: Current Drug Delivery
Emilio Fernández-Varón, Carlos Cárceles-García, Juan Manuel Serrano-Rodríguez, Carlos M Cárceles-Rodríguez
BACKGROUND: Bacterial pneumonia in goats is usually caused by Mannheimia haemolytica and Pasteurella multocida. Another important infection disease in lactating goats is intramammary infection producing mastitis, usually associated with coagulase-negative Staphylococcus spp. However, treatment of bacterial pneumonia in goats not affected by mastitis problems should be restricted to antimicrobials with scant penetration to milk in order to avoid long withdrawal times. Ceftiofur is a third-generation cephalosporin antimicrobial with activity against various gram-positive and gram-negative, aerobic and anaerobic bacteria encountered by domestic animals...
October 13, 2016: BMC Veterinary Research
Neha Sharma, Savita Jandaik, Sanjeev Kumar
Combination therapy of antibiotics and nanoparticles can be used against multi drug resistant microorganisms. Nanoparticles (NPs) have been reported to show antimicrobial activity. The antimicrobial activities of doped ZnO nanoparticles (ZnO NPs) were studied against fungi, gram-positive and gram-negative bacteria using the standard microdilution method. The interaction between the nanoparticle and the antibiotic was estimated by calculating the fractional inhibitory concentration (FIC index) of the combination through checkerboard assay...
October 10, 2016: Anais da Academia Brasileira de Ciências
Suporn Pholwat, Suzanne Stroup, Scott Heysell, Oleg Ogarkov, Svetlana Zhdanova, Girija Ramakrishnan, Eric Houpt
We studied the significance of particular eis mutations on M. tuberculosis drug resistance by using a specialized transduction strategy. Recombinant strains harboring eis mutations C-14T C-12T, and G-10A exhibited kanamycin resistance with MICs of 40, 10, and 20 μg/ml respectively, while recombinant strains harboring C-14G and C-15G were kanamycin susceptible (MIC 2.5-5 μg/ml). All of the tested eis mutants remained amikacin susceptible (MIC 0.5-4 μg/ml). The identification of specific eis mutations is needed for accurate genotypic susceptibility testing for kanamycin...
October 10, 2016: Antimicrobial Agents and Chemotherapy
Yaseen A M M Elshaier, Assem Barakat, Bander M Al-Qahtany, Abdullah Mohammed Al-Majid, Mohamed H Al-Agamy
A one-pot reaction was described that results in various pyrazole-thiobarbituric acid derivatives as new pharmacophore agents. These new heterocycles were synthesized in high yields with a broad substrate scope under mild reaction conditions in water mediated by NHEt₂. The molecular structures of the synthesized compounds were assigned based on different spectroscopic techniques. The new compounds were evaluated for their antibacterial and antifungal activity. Compounds 4h and 4l were the most active compounds against C...
October 9, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Michael Osthoff, Martin Siegemund, Gianmarco Balestra, Mohd Hafiz Abdul-Aziz, Jason A Roberts
Prolonged infusion of β-lactam antibiotics as either extended (over at least 2 hours) or continuous infusion is increasingly applied in intensive care units around the world in an attempt to optimise treatment with this most commonly used class of antibiotics, whose effectiveness is challenged by increasing resistance rates. The pharmacokinetics of β-lactam antibiotics in critically ill patients is profoundly altered secondary to an increased volume of distribution and the presence of altered renal function, including augmented renal clearance...
2016: Swiss Medical Weekly
Igor K Voukeng, Veronique P Beng, Victor Kuete
BACKGROUND: Infectious diseases due to multidrug-resistant bacteria are one of the causes of treatment failures contributing to an increase in mortality and/or morbidity. In this study, we evaluated the antibacterial potential of different parts of six medicinal plants namely Alstonia boonei, Ageratum conyzoides, Croton macrostachys, Cassia obtusifolia, Catharanthus roseus and Paullinia pinnata against a panel of 36 multi-drug resistant (MDR) Gram-negative and Gram-positive bacteria. METHODS: Minimum Inhibitory Concentration (MIC) and Minimal Bactericidal Concentration (MBC) of the methanol extracts from different parts of the plants were determined using broth microdilution method; standard phytochemical methods were used for phytochemical screening...
October 10, 2016: BMC Complementary and Alternative Medicine
Jing Shao, GaoXiang Shi, TianMing Wang, DaQiang Wu, ChangZhong Wang
Candida tropicalis has emerged as an important pathogenic fungus in nosocomial infections due to its recalcitrant resistance to conventional antifungal agents, especially to fluconazole (FLC). Berberine (BBR) is a bioactive herbal-originated alkaloids and has been reported to possess antifungal functions against C. albicans. In this paper, we tried to figure out the antifungal mechanisms of BBR and/or FLC in a clinical C. tropicalis isolate 2006. In the microdilution test, the minimum inhibitory concentration (MIC) of BBR was found 16 μg/mL with fractional inhibitory concentration index (FICI) 0...
2016: Frontiers in Microbiology
Vaishali Gaikwad, Tejash Gohel, Shrijeet Panickar, Vijay Chincholkar, Santosh Mangalkar
INTRODUCTION: Staphylococcus is one of the most common causes of nosocomial infection, especially pneumonia, surgical site infections, blood stream infections, and continues to be a major cause of community-acquired infections. The emergence of penicillin resistance followed by the development and spread of strains resistant to the semisynthetic penicillins such as methicillin, oxacillin and nafcillin, macrolides, tetracycline, and aminoglycosides has made the treatment of staphylococcal infection a global challenge...
October 2016: Indian Journal of Pathology & Microbiology
Ekaterina A Burakova, Irina V Saranina, Nina V Tikunova, Zhanna K Nazarkina, Pavel P Laktionov, Lubov' A Karpinskaya, Vadim B Anikin, Vladimir V Zarubaev, Vladimir N Silnikov
A series of 1,4-diazabicyclo[2.2.2]octane derivatives differing by linker moiety was evaluated for activity against several strains of both Gram-positive and Gram-negative bacteria including drug-resistant strains, one strain of fungus and influenza virus A/Puerto Rico/8/34 (H1N1). All compounds exhibited high antibacterial activity against all bacteria except Proteus vulgaris. The minimum inhibitory concentrations (MICs) of compound 1c with an o-phenylenebismethyl linker and compound 1e with a propylene aliphatic linker were found to be low and were comparable or better to the reference drug ciprofloxacin for Pseudomonas aeruginosa and Staphylococcus aureus...
September 28, 2016: Bioorganic & Medicinal Chemistry
Jingdong Shi, Ying Jiang, Yanfang Zhao
The objective of this study was to investigate the prevalence of drug-resistant Helicobacter pylori in Beijing Tian Tan Hospital (Beijing, China) and to determine the susceptibility of H. pylori to linezolid and novel oxazolidinone analogues. Minimum inhibitory concentrations (MICs) of amoxicillin, clarithromycin, metronidazole, ciprofloxacin, tetracycline and levofloxacin against H. pylori were determined by Etest. The in vitro antibacterial activities of linezolid and novel oxazolidinone analogues were assessed by the disk diffusion method...
September 15, 2016: Journal of Global Antimicrobial Resistance
Heber Silva-Díaz, Lorena Flores-Esqueche, Dunalia Llatas-Cancino, Génesis Guevara Vásquez, Teresa Silva-García
OBJECTIVE: To describe the frequency and antiparasitic in vitro susceptibility of Blastocystis hominis in patients admitted to theHospital Regional Lambayeque, Peru. MATERIAL AND METHODS: A cross-sectional study was conducted from January to August 2015 at 313 patients of all ages. B. hominis detection was performed on serial fecal samples by direct microscopic examination and microculture in modified Locke solution. The in vitro susceptibility testing against the drug metronidazole, nitazoxanide, trimethoprim-sulfamethoxazole and erythromycin was performed in 24 strains of B...
July 2016: Revista de Gastroenterología del Perú: órgano Oficial de la Sociedad de Gastroenterología del Perú
Andrée F Maheux, Adnane Sellam, Yves Piché, Maurice Boissinot, René Pelletier, Dominique K Boudreau, François J Picard, Hélène Trépanier, Marie-Josée Boily, Marc Ouellette, Paul H Roy, Michel G Bergeron
Successful treatment of a Candida infection relies on 1) an accurate identification of the pathogenic fungus and 2) on its susceptibility to antifungal drugs. In the present study we investigated the level of correlation between phylogenetical evolution and susceptibility of pathogenic Candida spp. to antifungal drugs. For this, we compared a phylogenetic tree, assembled with the concatenated sequences (2475-bp) of the ATP2, TEF1, and TUF1 genes from 20 representative Candida species, with published minimal inhibitory concentrations (MIC) of the four principal antifungal drug classes commonly used in the treatment of candidiasis: polyenes, triazoles, nucleoside analogues, and echinocandins...
October 3, 2016: Journal of Microbiological Methods
Ahmed AbdelKhalek, Charles R Ashby, Bhargav A Patel, Tanaji T Talele, Mohamed N Seleem
Bacterial infections present a serious challenge to healthcare practitioners due to the emergence of resistance to numerous conventional antibacterial drugs. Therefore, new bacterial targets and new antimicrobials are unmet medical needs. Rhodanine derivatives have been shown to possess potent antimicrobial activity via a novel mechanism. However, their potential use as antibacterials has not been fully examined. In this study, we determined the spectrum of activity of seven rhodanine derivatives (compounds Rh 1-7) against clinical isolates of Gram-positive and Gram-negative bacterial strains and Candida albicans...
2016: PloS One
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