• Archives of Pharmacal Research
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• v.23 no.6
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• pp.564-567
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• 2000

The use of amino acid derivatives as building blocks in peptide synthesis is increasingly being recognized as a potential route for the development of pharmaceutical agents. Side chain protection of polyfunctional amino acids such as Ser, Thr, Tyr is viewed as being particularly important. Although these derivatives are commercially listed, they are expensive and not widely available. We describe here a practical large-scale synthesis of t-butyl introduced D-serine, one of the building blocks of zoladex, a peptide drug.

• Archives of Pharmacal Research
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• v.7 no.1
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• pp.65-68
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• 1984

Mechanism of the monoamine oxidase inhibition by tranylcypromine was studied in relation to its metabolism to reactive apecies. A metabolic study performed to collect general biotransformation pathway in rats provided GC/MS evidence for the detection of two new metabolites, N-acetyl and hydroxylated N-acetyltranylacypromine.

• Archives of Pharmacal Research
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• v.7 no.2
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• pp.121-126
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• 1984

From the roots of Patrinia scabiosaefolia Valerianaceae), scopoletin (1), esculetin (2), oleanonic acid (3), 3-O-.alpha.-L-rhamnopyranosyl (1.rarw.2)-.alpha.-l-arabinopyranosyl oleanolic acid (4) and 3-O-.alpha.-L- rhamnopyranosyl (1 .rarw. 2)-.alpha.-L-arabinopyranosyl header agenin (5) were isolated and characterized by spectral data.

• Archives of Pharmacal Research
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• v.7 no.2
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• pp.141-143
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• 1984

A metabolic study was performed in order to characterize the in vivo MAO-inhibitory activity of benzyl trans-2-phenylcylopropanecarbamate which was reported to be twice as potent as the tranylcypromine. In the rat urine which was obtained after the administration of the benzyl trans-2-pheny-lcyclopropanecarbamate (40mg/kg) through oral route, a metabolic product, tranylcypromine as well as the intact drug was detected by GC/MS.

• Archives of Pharmacal Research
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• v.7 no.2
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• pp.101-107
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• 1984

The concentrations of metabolites of low molecular weights (90 to 310 amu) present in rat urine were determined by field ionization mass spectrometry. Three groups of rats were examined; intact controls, sham-operated rats and rats with selective lesions in their hypothalamus. The latter lesions are shown to induce characteristic aberrations in the metabolic profile, demonstrable five weeks after treatment, which are distinct from those induced by a sham operation.

• Archives of Pharmacal Research
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• v.13 no.1
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• pp.64-68
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• 1990

The stabilization effect of .alpha.-tocopherol incorporated into liposomal phospholipid membrane was investigated by fluorospectrophotometry and UV-visible spectretarded by the presence of .alpha.-tocopherol in the bilayer of liposomal phospholipid membrane relative to cholesterol-containing liposomes and pure phospholipid liposomes. .alpha.-tocopherol-containing liposomes prolonged the oxidation of liposomes-embedded heme as those of cholesterol-containing liposomes and pure phospholipid liposomes. Thus .alpha.-tocopherol-containing liposomes may be useful for the carrier systems of nutrients and drugs to phospholipid bilayer and stabilized liposomes.

• Archives of Pharmacal Research
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• v.5 no.1
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• pp.1-5
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• 1982

From the seeds of Phytolacca americana, acentonylidene americanin. A was isolated and its structure elucidated mainly by spectroscopic methods. This compound is not a genuine constituent but formed in the tissue on heating with acetone.

• Archives of Pharmacal Research
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• v.28 no.6
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• pp.730-735
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• 2005

Nine polymorphic modifications of doxazosin mesylate have been obtained by recrystallization in organic solvents under variable conditions. Different polymorphs of doxazosin mesylate were characterized by powder X-ray crystallography diffractometry (PXRD), differential scanning calorimetry (DSC), and thermogravimetric analysis (TG). Transformation of Form 1 and Form 2 was not occurred in three relative humidities ($0\%$, $51\%$, and $99\%$) at 20$\pm$0.5 for 30 days.

• Archives of Pharmacal Research
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• v.27 no.8
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• pp.811-815
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• 2004

Coumarin and its derivatives occur widely in nature. Many attempts were made for synthesis of various coumarin derivatives because of their interesting biological activities. In this study, solid phase synthetic approach of 3-(4-hydroxyphenyl)coumarin was achieved for combinatorial synthesis of substituted 3-phenylcoumarin analogues. Starting from 4-hydroxyphenylacetic acid methyl ester, release of 3-(4-hydroxypnehyl)coumarin from polymer support was accom-plished.

• Archives of Pharmacal Research
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• v.27 no.11
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• pp.1099-1105
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• 2004

The peroxisome proliferator-activated receptors (PPARs) are a primary regulator of lipid metabolism. Potency for activation of PPAR$\gamma$, one of a subfamily of PPARs, particularly mirrors glucose lowering activity. We prepared thiazolidinediones featuring benzoxazole moiety for subtype selective PPAR$\gamma$ activators. 5-[4-[2-(Benzoxazol-2-yl-alkylamino)ethoxy]benzyl]thiazolidine-2,4-diones have been prepared by Mitsunobu reaction of benzoxazolylalkylaminoethanol 8 and hydroxybenzylthiazolidinedione 6 and their activities were evaluated. Most compounds tested were identified as potent PPAR$\gamma$ agonists.