Optimization of pyrrolamides as mycobacterial GyrB ATPase inhibitors: structure-activity relationship and in vivo efficacy in a mouse model of tuberculosis.

abstract：:Despite dose-limiting nephrotoxicity concerns, polymyxin B has resurged as the treatment of last resort for multidrug-resistant Gram-negative bacterial infections. However, the pharmacokinetic, pharmacodynamic, and nephrotoxic properties of polymyxin B still are not thoroughly understood. The objective of this study w...

journal_title：Antimicrobial agents and chemotherapy

authors： Manchandani P,Zhou J,Ledesma KR,Truong LD,Chow DS,Eriksen JL,Tam VH

更新日期：2015-12-07 00:00:00

abstract：:The goal of the present study was to examine the ability of cytochrome P450-2C9 (CYP2C9) to activate cyclophosphamide (CPA) and elicit tumor cell death. A CYP2C9-deficient human lymphoblastoid cell line (AHH-1 cells) and a derivative cell line (H2C9 cells) stably transfected with a cDNA encoding CYP2C9 were used. The ...

journal_title：Antimicrobial agents and chemotherapy

authors： Zhou D,Lu Y,Steiner MS,Dalton JT

更新日期：2000-10-01 00:00:00

abstract：:The recent availability of CCR5 antagonists as anti-human immunodeficiency virus (anti-HIV) therapeutics has highlighted the need to accurately identify CXCR4-using variants in patient samples when use of this new drug class is considered. The Trofile assay (Monogram Biosciences) has become the method that is the most...

journal_title：Antimicrobial agents and chemotherapy

authors： Coakley E,Reeves JD,Huang W,Mangas-Ruiz M,Maurer I,Harskamp AM,Gupta S,Lie Y,Petropoulos CJ,Schuitemaker H,van 't Wout AB

更新日期：2009-11-01 00:00:00

abstract：:Mannopeptimycins alpha, beta, gamma, delta, and epsilon are new cyclic glycopeptide antibiotics produced by Streptomyces hygroscopicus LL-AC98. Mannopeptimycins gamma, delta, and epsilon, which have an isovaleryl substitution at various positions on the terminal mannose of the disaccharide moiety, demonstrated moderat...

journal_title：Antimicrobial agents and chemotherapy

authors： Singh MP,Petersen PJ,Weiss WJ,Janso JE,Luckman SW,Lenoy EB,Bradford PA,Testa RT,Greenstein M

更新日期：2003-01-01 00:00:00

abstract：:Early studies of immobilized peptides mainly focused upon the relationship between structural properties and the activity of soluble and surface-tethered sequences. The intention of this study was to analyze the influence of immobilization parameters upon the activity profile of peptides. Resin beads (TentaGel S NH(2)...

journal_title：Antimicrobial agents and chemotherapy

authors： Bagheri M,Beyermann M,Dathe M

更新日期：2009-03-01 00:00:00

abstract：:Antibiotic therapy with penicillin, doxycycline, and ceftriaxone has proven to be effective for the treatment of Lyme borreliosis. In some patients, however, it was noticed that borreliae can survival in the tissues in spite of seemingly adequate therapy. For a better understanding of this phenomenon, we investigated ...

journal_title：Antimicrobial agents and chemotherapy

authors： Kersten A,Poitschek C,Rauch S,Aberer E

更新日期：1995-05-01 00:00:00

abstract：:Two optically active (100% enantiomeric excess) isomers of ofloxacin [(+/-)-ofloxacin; DL-8280; (+/-)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7 H-pyrido[1,2,3-de] [1,4] benzoxazine-6-carboxylic acid] were prepared by use of their optically resolved synthetic intermediates. One of the isomers, (...

journal_title：Antimicrobial agents and chemotherapy

authors： Hayakawa I,Atarashi S,Yokohama S,Imamura M,Sakano K,Furukawa M

更新日期：1986-01-01 00:00:00

abstract：:Streptonigrin, a quinone antitumor antibiotic, has been reported to be effective in human trials. A sensitive and precise microbiological assay for the determination of distribution and concentrations of streptonigrin in the body fluids and tissues of treated mice has been developed in an attempt to supplement success...

journal_title：Antimicrobial agents and chemotherapy

authors： Pittillo RF,Woolley C

更新日期：1974-01-01 00:00:00

abstract：:Viridans group streptococci (VGS) are part of the normal flora that may cause bacteremia, often leading to endocarditis. We evaluated daptomycin against four clinical strains of VGS (MICs = 1 or 2 μg/ml) using an in vitro-simulated endocardial vegetation model, a simulated bacteremia model, and kill curves. Daptomycin...

journal_title：Antimicrobial agents and chemotherapy

authors： Akins RL,Katz BD,Monahan C,Alexander D

更新日期：2015-04-01 00:00:00

abstract：:The pharmacokinetics and protein binding of ceforanide were studied in 15 patients undergoing cholecystectomies. Each patient received ceforanide (20 mg/kg) intravenously on arrival in the operating room, after which serial blood samples were collected during the elimination phase for determination of total and free c...

journal_title：Antimicrobial agents and chemotherapy

authors： DiPiro JT,Bayoumi SM,Vallner JJ,Nesbit RR,Gokhale R,Rissing JP

更新日期：1985-04-01 00:00:00

abstract：:A total of 18 strains of Mycobacterium fortuitum, 15 strains of M. chelonei, and 31 strains of M. chelonei-like organisms were tested by both broth microdilution and agar dilution to determine their susceptibility to 34 antimicrobial agents. All strains grew well enough in cation-supplemented Mueller-Hinton broth for ...

journal_title：Antimicrobial agents and chemotherapy

authors： Swenson JM,Thornsberry C,Silcox VA

更新日期：1982-08-01 00:00:00

abstract：:Artermisinin and its derivatives are now the mainstays of antimalarial treatment; however, their mechanism of action is only poorly understood. We report on the synthesis of a novel series of epoxy-endoperoxides that can be prepared in high yields from simple starting materials. Endoperoxides that are disubstituted wi...

journal_title：Antimicrobial agents and chemotherapy

authors： del Pilar Crespo M,Avery TD,Hanssen E,Fox E,Robinson TV,Valente P,Taylor DK,Tilley L

更新日期：2008-01-01 00:00:00

abstract：:Current guidelines recommend vancomycin and linezolid as first-line agents against methicillin-resistant Staphylococcus aureus (MRSA) nosocomial pneumonia. Telavancin is a potential new therapeutic alternative, specifically in monomicrobial MRSA pneumonia. This study compared the efficacies of telavancin versus linezo...

journal_title：Antimicrobial agents and chemotherapy

authors： Battaglini D,Motos A,Li Bassi G,Yang H,Pagliara F,Yang M,Aguilera Xiol E,Meli A,Bobi J,Frigola G,Senussi T,Idone F,Travierso C,Chiurazzi C,Fernandez-Barat L,Rigol M,Ramirez J,Pelosi P,Chiumello D,Antonelli M,Nicol

更新日期：2020-12-16 00:00:00

abstract：:Intermittent preventive treatment in infants with sulfadoxine-pyrimethamine (IPTi-SP) reduces malaria episodes by 20 to 59% across Africa. This protective efficacy, however, may be affected by the high frequency of malnutrition in African infants. We analyzed the impact of malnutrition as defined by anthropometry on t...

journal_title：Antimicrobial agents and chemotherapy

authors： Danquah I,Dietz E,Zanger P,Reither K,Ziniel P,Bienzle U,Mockenhaupt FP

更新日期：2009-05-01 00:00:00

abstract：:Clostridioides difficile causes severe antibiotic-associated diarrhea and colitis. C. difficile is an anaerobic, Gram-positive sporeformer that is highly resistant to β-lactams, the most commonly prescribed antibiotics. The resistance of C. difficile to β-lactam antibiotics allows the pathogen to replicate and cause d...

journal_title：Antimicrobial agents and chemotherapy

authors： Sandhu BK,Edwards AN,Anderson SE,Woods EC,McBride SM

更新日期：2019-12-20 00:00:00

abstract：:An outbreak due to extended-spectrum beta-lactamase-producing Klebsiella pneumoniae (ESBL-KP) was detected from May 1993 to June 1995. A total of 145 patients, particularly patients in intensive care units (ICUs) (107 patients [72%]), were colonized or infected. Infection developed in 92 (63%) patients, and primary ba...

journal_title：Antimicrobial agents and chemotherapy

authors： Peña C,Pujol M,Ardanuy C,Ricart A,Pallares R,Liñares J,Ariza J,Gudiol F

更新日期：1998-01-01 00:00:00

abstract：:In vitro selection of mutants with decreased susceptibility to ertapenem was performed using Escherichia coli and Klebsiella pneumoniae clinical strains producing either the bla(CTX-M-2), bla(CTX-M-3), bla(CTX-M-9), or bla(CTX-M-15) gene. Frequencies of mutants with decreased susceptibilities to ertapenem were similar...

journal_title：Antimicrobial agents and chemotherapy

authors： Girlich D,Poirel L,Nordmann P

更新日期：2009-02-01 00:00:00

abstract：:Time-kill studies examined the activities of telithromycin (HMR 3647), erythromycin A, azithromycin, clarithromycin, roxithromycin, clindamycin, pristinamycin, amoxicillin-clavulanate, and metronidazole against 11 gram-positive and gram-negative anaerobic bacteria. Time-kill studies were carried out with the addition ...

journal_title：Antimicrobial agents and chemotherapy

authors： Credito KL,Ednie LM,Jacobs MR,Appelbaum PC

更新日期：1999-08-01 00:00:00

abstract：:The role of Ser-235 in the catalytic mechanism of the TEM-1 beta-lactamase has been explored by the study of a mutant enzyme in which Ser-235 has been substituted by alanine (Ala-235 mutant enzyme). A comparative kinetic analysis of both the wild-type and the Ala-235 TEM-1 enzymes revealed little effect of this substi...

journal_title：Antimicrobial agents and chemotherapy

authors： Imtiaz U,Manavathu EK,Lerner SA,Mobashery S

更新日期：1993-11-01 00:00:00

abstract：:Guanylhydrazones are cationic heteroaromatic drugs similar to the diamidines which are effective in the treatment of African trypanosomiasis and pneumocystosis. On the basis of their antitrypanosomal activity, different guanylhydrazones were selected for evaluation in a rat model of Pneumocystis carinii pneumonia. The...

journal_title：Antimicrobial agents and chemotherapy

authors： Walzer PD,Foy J,Runck J,Steele P,White M,Klein RS,Otter BA,Sundberg RJ

更新日期：1994-11-01 00:00:00

abstract：:The discovery of quorum-sensing (QS) systems regulating antibiotic resistance and virulence factors (VFs) has afforded a novel opportunity to prevent bacterial pathogenicity. Dietary molecules have been demonstrated to attenuate QS circuits of bacteria. But, to our knowledge, no study exploring the potential of colost...

journal_title：Antimicrobial agents and chemotherapy

authors： Srivastava A,Singh BN,Deepak D,Rawat AK,Singh BR

更新日期：2015-04-01 00:00:00

abstract：:Resistance-nodulation-division (RND) efflux pumps are important contributors to bacterial antibiotic resistance. In this study, we combined evolutionary sequence analyses, computational structural modeling, and ligand docking to develop a framework that can explain the known antibiotic substrate selectivity difference...

journal_title：Antimicrobial agents and chemotherapy

authors： Dey D,Kavanaugh LG,Conn GL

更新日期：2020-07-22 00:00:00

abstract：:Among respiratory tract isolates of Streptococcus pneumoniae from children, resistance to penicillins, cephalosporins, macrolides, and trimethoprim-sulfamethoxazole (SXT) increases on an annual basis. Pediatric patients who do not respond to conventional therapy for respiratory tract infections someday may be treated ...

journal_title：Antimicrobial agents and chemotherapy

authors： Karlowsky JA,Thornsberry C,Critchley IA,Jones ME,Evangelista AT,Noel GJ,Sahm DF

更新日期：2003-06-01 00:00:00

abstract：:3-O-(3',3'-Dimethylsuccinyl) betulinic acid (DSB), also known as PA-457, bevirimat (BVM), or MPC-4326, is a novel HIV-1 maturation inhibitor. Unlike protease inhibitors, BVM blocks the cleavage of the Gag capsid precursor (CA-SP1) to mature capsid (CA) protein, resulting in the release of immature, noninfectious viral...

journal_title：Antimicrobial agents and chemotherapy

authors： Lu W,Salzwedel K,Wang D,Chakravarty S,Freed EO,Wild CT,Li F

更新日期：2011-07-01 00:00:00

abstract：:The discovery of antibiotics in the last century is considered one of the most important achievements in the history of medicine. Antibiotic usage has significantly reduced morbidity and mortality associated with bacterial infections. However, inappropriate use of antibiotics has led to emergence of antibiotic resista...

journal_title：Antimicrobial agents and chemotherapy

authors： Ghosh D,Veeraraghavan B,Elangovan R,Vivekanandan P

更新日期：2020-01-27 00:00:00

abstract：:Clinical isolates of Klebsiella pneumoniae resistant to carbapenems are being isolated with increasing frequency. Loss of the expression of the major nonspecific porins OmpK35/36 is a frequent feature in these isolates. In this study, we looked for porins that could compensate for the loss of the major porins in carba...

journal_title：Antimicrobial agents and chemotherapy

authors： García-Sureda L,Doménech-Sánchez A,Barbier M,Juan C,Gascó J,Albertí S

更新日期：2011-10-01 00:00:00

abstract：:Rifampin was shown in vitro to decrease the amphotericin B minimal inhibitory concentrations of all of 10 strains of Coccidioides immitis tested. These decreases ranged from two- to fourfold and occurred with rifampin concentrations of 10 to 40 mug/ml. Rifampin alone was without effect. ...

journal_title：Antimicrobial agents and chemotherapy

authors： Rifkind D,Crowder ED,Hyland RN

更新日期：1974-12-01 00:00:00

abstract：:FCE 22891 is the oral prodrug of FCE 22101, a new broad-spectrum penem. The pharmacokinetics of FCE 22891 after single-dose administration, its absolute bioavailability, and the effect of food intake on its absorption were investigated in three different randomized crossover studies in healthy volunteers. Drug levels ...

journal_title：Antimicrobial agents and chemotherapy

authors： Saathoff A,Lode H,Hampel B,Deppermann KM,Borner K,Koeppe P

更新日期：1990-06-01 00:00:00

abstract：:When developing novel microbicide products for the prevention of HIV infection, the preclinical safety program must evaluate not only the active pharmaceutical ingredient but also the product itself. To that end, we applied several relatively standard toxicology study methodologies to female sheep, incorporating an as...

journal_title：Antimicrobial agents and chemotherapy

authors： Holt JD,Cameron D,Dias N,Holding J,Muntendam A,Oostebring F,Dreier P,Rohan L,Nuttall J

更新日期：2015-07-01 00:00:00

abstract：:Actinobacillus actinomycetemcomitans and Capnocytophaga spp. are gram-negative bacteria implicated in the etiology of periodontal disease (particularly in individuals with neutrophil defects) and life-threatening systemic infections. They are resistant to many antibiotics of microbial origin but are sensitive to the n...

journal_title：Antimicrobial agents and chemotherapy

authors： Miyasaki KT,Bodeau AL,Pohl J,Shafer WM

更新日期：1993-12-01 00:00:00