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Preclinical evaluation of MKC-442, a highly potent and specific inhibitor of human immunodeficiency virus type 1 in vitro.
MKC-442 (6-benzyl-1-ethoxymethyl-5-isopropyluracil or I-EBU) has recently been identified as a highly potent and specific inhibitor of human immunodeficiency virus type 1 (HIV-1) reverseExpand
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Antiviral Activities of MCC-478, a Novel and Specific Inhibitor of Hepatitis B Virus
ABSTRACT MCC-478 is a newly synthesized 2-amino-6-arylthio-9-phosphonomethoxyethylpurine bis(2,2,2-trifluoroethyl) ester derivative. MCC-478 showed a substantially higher (ca. 80-fold) anti-hepatitisExpand
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Effect of human serum on the in vitro anti-HIV-1 activity of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) derivatives as related to their lipophilicity and serum protein binding.
Several derivatives of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) were examined for their inhibitory effects on the replication of human immunodeficiency virus type 1 (HIV-1) in MT-4Expand
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Potassium activity and plasma membrane potentials in epithelial cells of toad bladder.
Intracellular potassium activity (aki), mucosal and serosal membrane potential (mEm, sEm), short-circuit current (Isc), and transepithelial potential difference in the epithelium of the toad bladderExpand
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Selective and synergistic inhibition of human immunodeficiency virus type 1 reverse transcriptase by a non-nucleoside inhibitor, MKC-442.
In the search for 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives, we have found 6-benzyl-1-(ethoxymethyl)-5-isopropyl-uracil (MKC-442) to be a highly potent and selective inhibitor ofExpand
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Effect of different prostaglandins on the permeability of the toad urinary bladder.
Abstract 1. PGE 1 alone induced no significant change in osmotic water flow, but stimulated the short-circuit current and inhibited vasopressin- and theophylline-induced osmotic flow across theExpand
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2-Amino-6-arylthio-9-[2-(phosphonomethoxy)ethyl]purine bis(2,2,2-trifluoroethyl) esters as novel HBV-specific antiviral reagents.
Novel 2-amino-6-arylthio-9-[2-(phosphonomethoxy)ethyl]purine bis(2,2,2-trifluoroethyl) esters were synthesized and evaluated for antihepatitis B virus (HBV) activity in vitro using HB611, HuH-6 cellExpand
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Comparative study of the effects of different diuretics on the permeability properties of the toad bladder.
Abstract 1. The effects of nine representative diuretics on the short-circuit current and the hydroosmotic response to vasopressin were studied under the same conditions using the toad bladder. 2. OnExpand
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[Suppressive effect of tritoqualine (TRQ) on the acceleration of fibrosis in the liver].
Liver cirrhosis was induced by consecutive CCl4-treatment of rats (0.5 ml/kg, s.c., 2 times/week) to investigate the effect of TRQ on the acceleration of fibrosis in the liver. An increase ofExpand
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Inhibitory mechanism of tritoqualine on histamine release from mast cells.
Tritoqualine (TRQ, (+)-(R*)-7-amino-4,5,6-triethoxy-3-[(R*)-5,6,7, 8-tetrahydro-4-methoxy-6-methyl-1,3-dioxolo[4,5-g]isoquinolin++ +-5-yl] phthalide) strongly inhibited the increased metabolism ofExpand
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