Scintillation proximity assay for inhibitors of Escherichia coli MurG and, optionally, MraY.

abstract：:Ramoplanin is an actinomycetes-derived antibiotic with broad-spectrum activity against Gram-positive bacteria that has been evaluated in clinical trials for the treatment of gastrointestinal vancomycin-resistant enterococci (VRE) and Clostridium difficile infections. Recent studies have proposed that ramoplanin binds ...

journal_title：Antimicrobial agents and chemotherapy

authors： Cheng M,Huang JX,Ramu S,Butler MS,Cooper MA

更新日期：2014-11-01 00:00:00

abstract：:BILN 2061 is a novel, specific hepatitis C virus (HCV) NS3 serine protease inhibitor discovered by Boehringer Ingelheim that has shown potent activity against HCV replicons in tissue culture and is currently under clinical investigation for the treatment of HCV infection. The poor fidelity of the HCV RNA-dependent RNA...

journal_title：Antimicrobial agents and chemotherapy

authors： Lu L,Pilot-Matias TJ,Stewart KD,Randolph JT,Pithawalla R,He W,Huang PP,Klein LL,Mo H,Molla A

更新日期：2004-06-01 00:00:00

abstract：:RBx 11760, a bi-aryl oxazolidinone, was investigated for antibacterial activity against Gram-positive bacteria. The MIC90s of RBx 11760 and linezolid against Staphylococcus aureus were 2 and 4 mg/liter, against Staphylococcus epidermidis were 0.5 and 2 mg/liter, and against Enterococcus were 1 and 4 mg/liter, respecti...

journal_title：Antimicrobial agents and chemotherapy

authors： Barman TK,Kumar M,Mathur T,Chaira T,Ramkumar G,Kalia V,Rao M,Pandya M,Yadav AS,Das B,Upadhyay DJ,Hamidullah,Konwar R,Raj VS,Singh H

更新日期：2016-11-21 00:00:00

abstract：:Debio-025 is a synthetic cyclosporine with no immunosuppressive capacity but a high inhibitory potency against cyclophilin A (CypA)-associated cis-trans prolyl isomerase (PPIase) activity. A lack of immunosuppressive effects compared to that of cyclosporine was demonstrated both in vitro and in vivo. For three cyclosp...

journal_title：Antimicrobial agents and chemotherapy

authors： Ptak RG,Gallay PA,Jochmans D,Halestrap AP,Ruegg UT,Pallansch LA,Bobardt MD,de Béthune MP,Neyts J,De Clercq E,Dumont JM,Scalfaro P,Besseghir K,Wenger RM,Rosenwirth B

更新日期：2008-04-01 00:00:00

abstract：:An estimated 40 million women of reproductive age are infected with one of three species of the waterborne parasite Schistosoma spp. Treatment with praziquantel (PZQ) via mass drug administration (MDA) campaigns is the mainstay of schistosomiasis control for populations living in areas of endemicity. The World Health ...

journal_title：Antimicrobial agents and chemotherapy

authors： Bustinduy AL,Kolamunnage-Dona R,Mirochnick MH,Capparelli EV,Tallo V,Acosta LP,Olveda RM,Friedman JF,Hope WW

更新日期：2020-08-20 00:00:00

abstract：:Metronidazole is now being used with increasing frequency for various infectious conditions in patients with renal failure. It is commonly administered to septic patients who have developed acute renal failure requiring hemodialysis. The hemodialysis clearances of metronidazole and its metabolites were evaluated in ni...

journal_title：Antimicrobial agents and chemotherapy

authors： Lau AH,Chang CW,Sabatini S

更新日期：1986-02-01 00:00:00

abstract：:Replication of hepatitis C virus (HCV) RNA is catalyzed by the virally encoded RNA-dependent RNA polymerase NS5B. It is believed that the viral polymerase utilizes a de novo or primer-independent mechanism for initiation of RNA synthesis. Our previous work has shown that dinucleotides were efficient initiation molecul...

journal_title：Antimicrobial agents and chemotherapy

authors： Zhong W,An H,Barawkar D,Hong Z

更新日期：2003-08-01 00:00:00

abstract：:The in vitro potency and in vivo efficacy of Q-35, a new fluoroquinolone, against Mycoplasma pneumoniae were investigated by pharmacokinetic studies with M. pneumoniae-infected hamsters. By using fluoroquinolones, macrolides, and tetracyclines as references, Q-35 was found to possess the greatest mycoplasmacidal activ...

journal_title：Antimicrobial agents and chemotherapy

authors： Gohara Y,Arai S,Akashi A,Kuwano K,Tseng CC,Matsubara S,Matumoto M,Furudera T

更新日期：1993-09-01 00:00:00

abstract：:An antibody induced in rabbits against a gentamicin-bovine serum albumin conjugate cross-reacted with the chemically related aminoglycoside, sisomicin, facilitating the development of a sisomicin radioimmunoassay. Sisomicin was labeled with (125)I using an acylating agent [3-(4-hydroxyphenyl)propionic acid-N-hydroxy-s...

journal_title：Antimicrobial agents and chemotherapy

authors： Broughton A,Strong JE,Bodey GP

更新日期：1976-02-01 00:00:00

abstract：:We have used the endogenous reverse transcriptase reaction of viral core particles from duck liver to elucidate the mechanism of inhibition of duck hepatitis B virus (DHBV) replication by the nucleoside analog (-)-beta-L-2',3'-dideoxy-3'-thiacytidine (3TC). As is the case in human immunodeficiency virus replication, 3...

journal_title：Antimicrobial agents and chemotherapy

authors： Severini A,Liu XY,Wilson JS,Tyrrell DL

更新日期：1995-07-01 00:00:00

abstract：:Antibiotic treatment of lung infections may lead to the emergence of resistance in the gut flora. Appropriate dosing regimens could mitigate this adverse effect. In gnotobiotic rats harboring intestinal Escherichia coli and Enterococcus faecium populations, a lung infection by Klebsiella pneumoniae was instigated with...

journal_title：Antimicrobial agents and chemotherapy

authors： Kesteman AS,Perrin-Guyomard A,Laurentie M,Sanders P,Toutain PL,Bousquet-Mélou A

更新日期：2010-07-01 00:00:00

abstract：:DNA ligases are indispensable enzymes playing a critical role in DNA replication, recombination, and repair in all living organisms. Bacterial NAD+-dependent DNA ligase (LigA) was evaluated for its potential as a broad-spectrum antibacterial target. A novel class of substituted adenosine analogs was discovered by targ...

journal_title：Antimicrobial agents and chemotherapy

authors： Mills SD,Eakin AE,Buurman ET,Newman JV,Gao N,Huynh H,Johnson KD,Lahiri S,Shapiro AB,Walkup GK,Yang W,Stokes SS

更新日期：2011-03-01 00:00:00

abstract：:While it is well-known that adjunctive corticosteroid use improves the outcome of moderate-to-severe Pneumocystis jirovecii pneumonia (PcP) in patients with human immunodeficiency virus (HIV), there are limited data on its efficacy in non-HIV-infected patients with PcP. Patients undergoing fiber-optic bronchoscopy wit...

journal_title：Antimicrobial agents and chemotherapy

authors： Moon SM,Kim T,Sung H,Kim MN,Kim SH,Choi SH,Jeong JY,Woo JH,Kim YS,Lee SO

更新日期：2011-10-01 00:00:00

abstract：:Treating high-density bacterial infections is a challenging clinical problem. We have a paucity of new agents that can address this problem. Pseudomonas aeruginosa is a particularly difficult pathogen to treat effectively because of the plethora of resistance mechanisms it carries. Fosfomycin is an agent discovered ci...

journal_title：Antimicrobial agents and chemotherapy

authors： Drusano GL,Neely MN,Yamada WM,Duncanson B,Brown D,Maynard M,Vicchiarelli M,Louie A

更新日期：2018-11-26 00:00:00

abstract：:Cystathionine gamma-lyase (EC 4.4.1.1) was purified from Streptomyces cattleya, an actinomycete which produces the unusual beta-lactam antibiotic thienamycin. The enzyme displays broad substrate specificity and is similar to gamma-lyases purified from other microorganisms. That the gamma-lyase functions in vivo to pro...

journal_title：Antimicrobial agents and chemotherapy

authors： Williamson JM,Meyer R,Inamine E

更新日期：1985-10-01 00:00:00

abstract：:An oligonucleoside methylphosphonate (ONMP) complementary to the splice acceptor site of immediate-early (IE) pre-mRNAs 4 and 5 (IE4,5SA) inhibits herpes simplex virus type 1 (HSV-1) growth in vitro and in infected animals. The antiviral effect appears to be due to inhibition of IE pre-mRNA 4 and 5 splicing and/or IE4...

journal_title：Antimicrobial agents and chemotherapy

authors： Kulka M,Smith CC,Levis J,Fishelevich R,Hunter JC,Cushman CD,Miller PS,Ts'o PO,Aurelian L

更新日期：1994-04-01 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：:In this study, susceptibilities were determined for AZD0914, a spiropyrimidinetrione DNA gyrase inhibitor, azithromycin, doxycycline, and levofloxacin against Mycoplasma and Ureaplasma species. The activity of AZD0914 was comparable to that of levofloxacin and doxycycline against Mycoplasma genitalium and Mycoplasma p...

journal_title：Antimicrobial agents and chemotherapy

authors： Waites KB,Crabb DM,Duffy LB,Huband MD

更新日期：2015-01-01 00:00:00

abstract：:The racemic nucleoside analogue 2'-deoxy-3'-oxa-4'-thiocytidine (dOTC) is in clinical development for the treatment of human immunodeficiency virus (HIV) type 1 (HIV-1) infection. dOTC is structurally related to lamivudine (3TC), but the oxygen and sulfur in the furanosyl ring are transposed. Intracellular metabolism ...

journal_title：Antimicrobial agents and chemotherapy

authors： de Muys JM,Gourdeau H,Nguyen-Ba N,Taylor DL,Ahmed PS,Mansour T,Locas C,Richard N,Wainberg MA,Rando RF

更新日期：1999-08-01 00:00:00

abstract：:The in vitro antibacterial activity of AM-1155 against a wide variety of clinical isolates was compared with those of other fluoroquinolones. The MICs of AM-1155 for 90% of Staphylococcus aureus, Streptococcus pneumoniae, and Enterococcus faecalis isolates tested were 0.10, 0.39, and 0.78 microgram/ml, respectively. T...

journal_title：Antimicrobial agents and chemotherapy

authors： Wakabayashi E,Mitsuhashi S

更新日期：1994-03-01 00:00:00

abstract：:Preclinical animal models of infection are employed to develop new agents but also to screen among molecules to rank them. There are often major differences between human pharmacokinetic (PK) profiles and those developed by animal models of infection, and these may lead to substantial differences in efficacy relative ...

journal_title：Antimicrobial agents and chemotherapy

authors： Drusano GL,Duncanson B,Scanga CA,Kim S,Schmidt S,Neely MN,Yamada WM,Vicchiarelli M,Peloquin CA,Louie A

更新日期：2020-11-17 00:00:00

abstract：:The in vitro activity of tosufloxacin (A-61827; T-3262) against 15 clinical isolates of Chlamydia trachomatis and 31 recent clinical isolates of Neisseria gonorrhoeae, including 15 spectinomycin-resistant N. gonorrhoeae and 16 penicillinase-producing N. gonorrhoeae, was determined. Tosufloxacin was compared with doxyc...

journal_title：Antimicrobial agents and chemotherapy

authors： Segreti J,Hirsch DJ,Harris AA,Kapell KS,Orbach H,Kessler HA

更新日期：1990-06-01 00:00:00

abstract：:Subtherapeutic levels of oxytetracycline plus neomycin in animal feeds did not bring about increases in the quantity, prevalence, or shedding of Salmonella typhimurium in swine, calves, or chickens. In fact, the medication generally reduced the proportion of animals carrying S. typhimurium. The medicated groups were f...

journal_title：Antimicrobial agents and chemotherapy

authors： Girard AE,English AR,Evangelisti DG,Lynch JE,Solomons IA

更新日期：1976-07-01 00:00:00

abstract：:Hand-foot-and-mouth disease (HFMD), caused by enterovirus, is a threat to public health worldwide. To date, enterovirus 71 (EV71) has been one of the major causative agents of HFMD in the Pacific-Asia region, and outbreaks with EV71 cause millions of infections. However, no drug is currently available for clinical the...

journal_title：Antimicrobial agents and chemotherapy

authors： Wang Y,Cao L,Zhai Y,Yin Z,Sun Y,Shang L

更新日期：2017-06-27 00:00:00

abstract：:INX-08189 is an aryl-phosphoramidate of 6-O-methyl-2'-C-methyl guanosine. INX-08189 was highly potent in replicon assays, with a 50% effective concentration of 10±6 nM against hepatitis C genotype 1b at 72 h. The inhibitory effect on viral replication was rapid, with a 50% effective concentration (EC50) of 35±8 nM at ...

journal_title：Antimicrobial agents and chemotherapy

authors： Vernachio JH,Bleiman B,Bryant KD,Chamberlain S,Hunley D,Hutchins J,Ames B,Gorovits E,Ganguly B,Hall A,Kolykhalov A,Liu Y,Muhammad J,Raja N,Walters CR,Wang J,Williams K,Patti JM,Henson G,Madela K,Aljarah M,Gilles

更新日期：2011-05-01 00:00:00

abstract：:The intestinal elimination of ciprofloxacin in the large bowel was studied in a rabbit model. Segments from the cecum, colon, and sigmoid colon along with their intact blood vessels were isolated and perfused, and their contents were collected over a 90-min period following the administration of a single parenteral do...

journal_title：Antimicrobial agents and chemotherapy

authors： Ramon J,Dautrey S,Farinoti R,Carbon C,Rubinstein E

更新日期：1996-01-01 00:00:00

abstract：:Mutations in the kelch propeller domain (K13 propeller) of Plasmodium falciparum parasites from Southeast Asia are associated with reduced susceptibility to artemisinin. We exposed in vitro-cultured stage V gametocytes from Cambodian K13 propeller mutant parasites to dihydroartemisinin and evaluated the inhibition of ...

journal_title：Antimicrobial agents and chemotherapy

authors： Lozano S,Gamallo P,González-Cortés C,Presa Matilla JL,Fairhurst RM,Herreros E,Amaratunga C,Rodrigues J

更新日期：2018-11-26 00:00:00

abstract：:Bacterial susceptibility to a new organic acid related to nalidixic acid and oxolinic acid was tested. The in vitro susceptibility pattern of the new compound was found to be very similar to that of nalidixic acid. ...

journal_title：Antimicrobial agents and chemotherapy

authors： Gilis PM,Haemers A,Pattyn SR

更新日期：1978-03-01 00:00:00

abstract：:A vancomycin-resistant, anaerobic, gram-positive coccus containing the vanD and vanG-like genes (strain CCRI-16110) was isolated from a human fecal specimen during a hospital surveillance program to detect carriers of vancomycin-resistant enterococci. Comparison of the 16S rRNA gene sequence of strain CCRI-16110 with ...

journal_title：Antimicrobial agents and chemotherapy

authors： Domingo MC,Huletsky A,Giroux R,Picard FJ,Bergeron MG

更新日期：2007-11-01 00:00:00

abstract：:The yeast Candida albicans is an opportunistic human fungal pathogen and the cause of superficial and systemic infections in immunocompromised patients. The classes of antifungal agents most commonly used to treat Candida infections are the azoles, polyenes, and echinocandins. In the present study, we identified chang...

journal_title：Antimicrobial agents and chemotherapy

authors： Hoehamer CF,Cummings ED,Hilliard GM,Rogers PD

更新日期：2010-05-01 00:00:00