NDLI: Comparisons of anti-human immunodeficiency virus activities, cellular transport, and plasma and intracellular pharmacokinetics of 3'-fluoro-3'-deoxythymidine and 3'-azido-3'-deoxythymidine.

Please wait, while we are loading the content...

Year: 2016, Volume: 60

Year: 2015, Volume: 60

Year: 2015, Volume: 59

Year: 2014, Volume: 59

Year: 2014, Volume: 58

Year: 2013, Volume: 57

Year: 2012, Volume: 56

Year: 2011, Volume: 55

Year: 2010, Volume: 54

Year: 2009, Volume: 53

Year: 2008, Volume: 52

Year: 2007, Volume: 51

Year: 2006, Volume: 50

Year: 2005, Volume: 49

Year: 2004, Volume: 48

Year: 2003, Volume: 47

Year: 2002, Volume: 46

Year: 2001, Volume: 45

Year: 2000, Volume: 44

Year: 1999, Volume: 43

Year: 1998, Volume: 42

Year: 1997, Volume: 41

Year: 1996, Volume: 40

Year: 1995, Volume: 39

Year: 1994, Volume: 38

Year: 1993, Volume: 37

Year: 1992, Volume: 36

Year: 1992, Volume: 36, Issue: 12

Year: 1992, Volume: 36, Issue: 11

Year: 1992, Volume: 36, Issue: 10

Year: 1992, Volume: 36, Issue: 9

Year: 1992, Volume: 36, Issue: 8

Year: 1992, Volume: 36, Issue: 7

Year: 1992, Volume: 36, Issue: 6

Year: 1992, Volume: 36, Issue: 5

Year: 1992, Volume: 36, Issue: 4

Active efflux mechanisms for antimicrobial resistance.

Molecular targets of 5-fluoroorotate in the human malaria parasite, Plasmodium falciparum.

Characterization of two plasmids from Campylobacter jejuni isolates that carry the aphA-7 kanamycin resistance determinant.

In vitro susceptibilities of aerotolerant Campylobacter isolates to 22 antimicrobial agents.

4-week treatment of streptococcal native valve endocarditis with high-dose teicoplanin.

Safety and efficacy of intranasal pirodavir (R77975) in experimental rhinovirus infection.

(-)-2'-deoxy-3'-thiacytidine is a potent, highly selective inhibitor of human immunodeficiency virus type 1 and type 2 replication in vitro.

Identification of a streptomycin resistance gene and a partial Tn3 transposon coding for a beta-lactamase in a periodontal strain of Eikenella corrodens.

Identification of factors affecting in vivo aminoglycoside activity in an experimental model of gram-negative endocarditis.

Effects of novel fluoroquinolones on the catalytic activities of eukaryotic topoisomerase II: Influence of the C-8 fluorine group.

Metabolism of S-1108, a new oral cephem antibiotic, and metabolic profiles of its metabolites in humans.

Phase I clinical studies of S-1108: safety and pharmacokinetics in a multiple-administration study with special emphasis on the influence on carnitine body stores.

Characterization of the tet(M) determinant of Tn916: evidence for regulation by transcription attenuation.

Antimicrotubule benzimidazoles inhibit in vitro growth of Pneumocystis carinii.

Overproduction of a penicillin-binding protein is not the only mechanism of penicillin resistance in Enterococcus faecium.

Interaction of Vibrio cholerae cells with beta-lactam antibiotics: emergence of resistant cells at a high frequency.

Pharmacokinetics of cefpodoxime proxetil and interactions with an antacid and an H2 receptor antagonist.

Imipenem versus gentamicin combined with either cefuroxime or cephalothin as initial therapy for febrile neutropenic patients.

Comparisons of anti-human immunodeficiency virus activities, cellular transport, and plasma and intracellular pharmacokinetics of 3'-fluoro-3'-deoxythymidine and 3'-azido-3'-deoxythymidine.

Bactericidal activities of five quinolones for Escherichia coli strains with mutations in genes encoding the SOS response or cell division.

The lipid A biosynthesis mutation lpxA2 of Escherichia coli results in drastic antibiotic supersusceptibility.

Effects of aluminum hydroxide and calcium carbonate antacids on the bioavailability of ciprofloxacin.

Efficacy and safety of temafloxacin versus those of amoxicillin in hospitalized adults with community-acquired pneumonia.

Iron transport-mediated antibacterial activity of and development of resistance to hydroxamate and catechol siderophore-carbacephalosporin conjugates.

In vitro antistaphylococcal activities of two investigative fluoroquinolones, CI-960 and WIN 57273, compared with those of ciprofloxacin, mupirocin (pseudomonic acid), and peptide-class antimicrobial agents.

In vitro antistaphylococcal activity and testing of RP 59500, a new streptogramin, by two methods.

Susceptibilities of penicillin-susceptible and -resistant strains of Streptococcus pneumoniae to RP 59500, vancomycin, erythromycin, PD 131628, sparfloxacin, temafloxacin, win 57273, ofloxacin, and ciprofloxacin.

In vitro and in vivo antibacterial activities of levofloxacin (l-ofloxacin), an optically active ofloxacin.

Evidence for in vivo incorporation of D-lactate into peptidoglycan precursors of vancomycin-resistant enterococci.

In vitro susceptibilities of Mycoplasma genitalium to antibiotics.

In vitro activity of decaplanin (M86-1410), a new glycopeptide antibiotic.

Tet determinants provide poor protection against some tetracyclines: further evidence for division of tetracyclines into two classes.

In vitro activity of Ro 23-9424, a dual-action antibacterial agent, against bacterial isolates from cancer patients compared with those of other agents.

Lack of effect of carbonyl cyanide m-chlorophenylhydrazone on KB-5246 accumulation by Staphylococcus aureus.

A pneumococcal clinical isolate with high-level resistance to cefotaxime and ceftriaxone.

Kinetic interaction of biofilm cells of Staphylococcus aureus with cephalexin and tobramycin in a chemostat system.

Relative beta-lactamase- and transpeptidase-inhibitory activities of the new quinolone WIN-57273 in Staphylococcus aureus.

In vitro studies of activities of some antifungal agents against Candida albicans ATCC 10231 by the turbidimetric method.

Effects of amino acids on expression of enterococcal vancomycin resistance.

Immune Response to a Major Epitope of p24 during Infection with Human Immunodeficiency Virus Type 1 and Implications for Diagnosis and Prognosis

Year: 1992, Volume: 36, Issue: 3

Year: 1992, Volume: 36, Issue: 2

Year: 1992, Volume: 36, Issue: 1

Year: 1991, Volume: 35

Year: 1990, Volume: 34

Year: 1989, Volume: 33

Year: 1988, Volume: 32

Year: 1987, Volume: 31

Year: 1986, Volume: 30

Year: 1986, Volume: 29

Year: 1985, Volume: 28

Year: 1985, Volume: 27

Year: 1984, Volume: 26

Year: 1984, Volume: 25

Year: 1983, Volume: 24

Year: 1983, Volume: 23

Year: 1982, Volume: 22

Year: 1982, Volume: 21

Year: 1981, Volume: 20

Year: 1981, Volume: 19

Year: 1980, Volume: 18

Year: 1980, Volume: 17

Year: 1979, Volume: 16

Year: 1979, Volume: 15

Year: 1978, Volume: 14

Year: 1978, Volume: 13

Year: 1977, Volume: 12

Year: 1977, Volume: 11

Year: 1976, Volume: 10

Year: 1976, Volume: 9

Year: 1975, Volume: 8

Year: 1975, Volume: 7

Year: 1974, Volume: 6

Year: 1974, Volume: 5

Year: 1973, Volume: 4

Year: 1973, Volume: 3

Year: 1972, Volume: 2

Year: 1972, Volume: 1

Comparisons of anti-human immunodeficiency virus activities, cellular transport, and plasma and intracellular pharmacokinetics of 3'-fluoro-3'-deoxythymidine and 3'-azido-3'-deoxythymidine.

Content Provider	PubMed Central
Author	Zhu, Q. Y. Vidal, P. M. Watanabe, K. A. Polsky, B. Armstrong, D. Ostrander, M. Lang, S. A. Muchmore, E. Chou, T. C. Kong, X. B.
Abstract	3'-Fluoro-3'-deoxythymidine (FLT), a candidate anti-AIDS compound in clinical trials, showed anti-human immunodeficiency virus type 1 (HIV-1) potency (50% effective concentration, 0.0052 microM) slightly better than or equal to that of 3'-azido-3'-deoxythymidine (AZT) in MT4 cells and was threefold more potent in H9 cells. There was no FLT resistance demonstrable in the AZT-resistant HIV-1 strains. Both FLT and AZT showed low cytotoxicity for MT4 cells, with selectivity indices (efficacy/toxicity ratio) of greater than 47,000 and greater than 33,000, respectively. Cellular permeation of FLT and thymidine (dThd) was greater than that of AZT, and FLT and dThd permeated the cell membranes by a carrier-mediated mechanism as well as by simple diffusion, as indicated by the existence of nitrobenzylthioinosine-5'-monophosphate-sensitive and -insensitive components. By contrast, transport of AZT into cells was by simple diffusion. The intracellular level of the triphosphate of FLT (FLTTP) in MT4 cells was two- to threefold higher than that of AZT (AZTTP) after exposure to 1.8 microM each compound for 12 h. The elimination kinetics of FLTTP and AZTTP in HIV-1-infected MT4 cells in fresh medium showed biphasic patterns, with initial half-lives of 1.03 and 1.09 h, respectively. In phytohemagglutinin-stimulated human peripheral blood lymphocytes, the FLTTP level was increased 59-fold compared with that in unstimulated cells at 12 h, was four- to sixfold higher than the level of AZTTP in stimulated cells at 12 h, and remained four- to fivefold higher during a 4-h elimination period in fresh medium and twofold higher at the end of a 12-h elimination period. Two- to eightfold more [3H]AZT than [3H]FLT was incorporated into the host cell DNA, and both [3H]AZT and [3H]FLT remained persistently incorporated for over 24 h. The incorporated [3H]AZT and [3H]FLT were alkali labile, whereas incorporated [3H]dThd was alkali stable. Pharmacokinetics of FLT in plasma of monkeys after intravenous (i.v.) administration showed that the FLT concentration in plasma declined, with a half-life of 1.19 +/- 0.1 h; the steady-state volume of distribution was 0.93 +/- 0.2 liter/kg of body weight, and total clearance was 0.56 +/- 0.15 liter/kg. Oral bioavailability of FLT was excellent and comparable to i.v. bioavailability in terms of areas under the concentration-time curves for three monkeys. Of the total dose, 41 to 61% was excreted in urine as unchanged FLT, and only 3.2 to 7.4% of the total dose was identified as glucuronide-conjugated FLT in urine 48 h after i.v. administration to monkeys. We conclude that FLT exhibits an anti-HIV-1 potency similar to that of AZT but with slightly better selectivity of effects and with higher intracellular active metabolite levels.
Starting Page	808
File Format	PDF
ISSN	10986596
e-ISSN	10986596
Journal	Antimicrobial Agents and Chemotherapy
Issue Number	4
Volume Number	36
Language	English
Publisher Date	1992-04-01
Access Restriction	Open
Subject Keyword	Research in Higher Education
Content Type	Text
Resource Type	Article
Subject	Infectious Diseases Pharmacology Pharmacology (medical)

Central Library (ISO-9001:2015 Certified)
Indian Institute of Technology Kharagpur
Kharagpur, West Bengal, India | PIN - 721302

See location in the Map
03222 282435
Mail: support@ndl.gov.in

Sl.	Authority	Responsibilities	Communication Details
1	Ministry of Education (GoI), Department of Higher Education	Sanctioning Authority	https://www.education.gov.in/ict-initiatives
2	Indian Institute of Technology Kharagpur	Host Institute of the Project: The host institute of the project is responsible for providing infrastructure support and hosting the project	https://www.iitkgp.ac.in
3	National Digital Library of India Office, Indian Institute of Technology Kharagpur	The administrative and infrastructural headquarters of the project	Dr. B. Sutradhar bsutra@ndl.gov.in
4	Project PI / Joint PI	Principal Investigator and Joint Principal Investigators of the project	Dr. B. Sutradhar bsutra@ndl.gov.in Prof. Saswat Chakrabarti will be added soon
5	Website/Portal (Helpdesk)	Queries regarding NDLI and its services	support@ndl.gov.in
6	Contents and Copyright Issues	Queries related to content curation and copyright issues	content@ndl.gov.in
7	National Digital Library of India Club (NDLI Club)	Queries related to NDLI Club formation, support, user awareness program, seminar/symposium, collaboration, social media, promotion, and outreach	clubsupport@ndl.gov.in
8	Digital Preservation Centre (DPC)	Assistance with digitizing and archiving copyright-free printed books	dpc@ndl.gov.in
9	IDR Setup or Support	Queries related to establishment and support of Institutional Digital Repository (IDR) and IDR workshops	idr@ndl.gov.in