Search Results - "VARGA, S. L"
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Disposition and pharmacokinetics of the antimigraine drug, rizatriptan, in humans
Published in Drug metabolism and disposition (2000)“…The absorption and disposition of rizatriptan (MK-0462, Maxalt(TM)), a selective 5-HT(1B/1D) receptor agonist used in the treatment of migraine headaches, was…”
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Design and Synthesis of Potent, Selective, and Orally Bioavailable Tetrasubstituted Imidazole Inhibitors of p38 Mitogen-Activated Protein Kinase
Published in Journal of medicinal chemistry (17-06-1999)“…Novel potent and selective diarylimidazole inhibitors of p38 MAP (mitogen-activated protein) kinase are described which have activity in both cell-based assays…”
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Metabolism of 3-[2-(benzoxazol-2-yl)ethyl]-5-ethyl-6-methylpyridin-2 (1H)-one (L-696,229), an HIV-1 reverse transcriptase inhibitor, by rat liver slices and in humans
Published in Drug metabolism and disposition (01-03-1994)“…Healthy subjects were administered single oral doses of 800 mg or 400 mg 3-[2-(benzoxazol-2-yl)ethyl]-5-ethyl-6-methylpyridin-2(1H)-o ne (L-696,229), a…”
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Biotransformation of 5-chloro-3-phenylthioindole-2-carboxamide (L-734,005) in rhesus monkeys and rat liver microsomes to a potent HIV-1 reverse transcriptase inhibitor
Published in Drug metabolism and disposition (01-07-1993)“…Rhesus monkeys were dosed orally with 10 mg/kg 5-chloro-3-phenylthioindole-2-carboxamide (L-734,005), a nonnucleoside human immunodeficiency virus type 1…”
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Thienothiopyran-2-sulfonamides: a novel class of water-soluble carbonic anhydrase inhibitors
Published in Journal of medicinal chemistry (01-04-1987)“…An attempt to develop a water-soluble carbonic anhydrase inhibitor focused on exploring structure-activity relationships in the thienothiopyransulfonamide…”
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L-653,328: an ocular hypotensive agent with modest beta receptor blocking activity
Published in Investigative ophthalmology & visual science (01-05-1988)“…L-653,328 is the acetate ester of L-652,698 ((S)-3-tert-butylamino-1-[4-[2(hydroxy)ethyl]phenoxy]2-propanol). The penetration of L-652,698 into the albino…”
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On the use of the O-methylmandelate ester for establishment of absolute configuration of secondary alcohols
Published in Journal of organic chemistry (01-06-1986)Get full text
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Species differences in the metabolism of a potent HIV-1 reverse transcriptase inhibitor L-738,372. In vivo and in vitro studies in rats, dogs, monkeys, and human
Published in Drug metabolism and disposition (01-07-1995)“…In vivo and in vitro metabolism of 6-chloro-4(S)-cyclopropyl-3,4-dihydro-4-((2-pyridyl) ethynyl)quinazolin-2(1H)-one (L-738,372), a potent human…”
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An unusual dimer of 2-mercaptothiophene
Published in Journal of organic chemistry (01-06-1989)Get full text
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Acetamidomethyl. A Novel Thiol Protecting Group for Cysteine
Published in Journal of the American Chemical Society (01-07-1972)Get full text
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Beta 1-selective adrenoceptor antagonists: examples of the 2-[4-[3-(substituted amino)-2-hydroxypropoxy]phenyl]imidazole class. 2
Published in Journal of medicinal chemistry (01-06-1986)“…An attempt to develop a highly cardioselective beta-adrenoceptor antagonist devoid of intrinsic sympathomimetic activity (ISA) focused on exploring…”
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Convenient preparation of substituted 5-aminooxazoles via a microwave-assisted Cornforth rearrangement
Published in Tetrahedron (08-05-2006)“…The preparation of oxazole-4-carboxamides and their subsequent thermal rearrangement to 5-aminooxazole-4-carboxylates is optimized in a high-speed…”
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Studies on the total synthesis of an enzyme. V. The preparation of enzymatically active material
Published in Journal of the American Chemical Society (15-01-1969)Get full text
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Synthesis and pharmacological evaluation of a series of dibenzo[a,d]cycloalkenimines as N-methyl-D-aspartate antagonists
Published in Journal of medicinal chemistry (01-02-1990)“…A series of 73 dibenzo[a,d]cycloalkenimines were synthesized and evaluated for their ability to displace…”
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Identification and quantitation of extractables from cellulose acetate butyrate (CAB) and estimation of their in vivo exposure levels
Published in Journal of pharmaceutical and biomedical analysis (29-06-2004)“…The purpose of this study was to qualitatively and quantitatively determine potential cellulose acetate butyrate (CAB) extractables in a way to meaningfully…”
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Imino-bridged heterocycles. VII. N-aminobenzocycloheptapyridinimines
Published in Journal of heterocyclic chemistry (01-09-1986)“…Condensation of anhydrous hydrazine with a variety of benzocycloheptapyridinones led to N‐aminobenzocycloheptapyridinimines. Regiospecific ring closures…”
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Topically active carbonic anhydrase inhibitors. 2. Benzo[b]thiophenesulfonamide derivatives with ocular hypotensive activity
Published in Journal of medicinal chemistry (01-12-1989)“…Derivatives of benzo[b]thiophene-2-sulfonamide were prepared to investigate their potential utility as topically active inhibitors of ocular carbonic…”
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