• Archives of Pharmacal Research
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• v.19 no.3
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• pp.191-196
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• 1996

Bizelesin is a promising novel anticancer agent which is known to alkylate N3 of adenine to induce DNA interstrand cross-links (ISC) with in $5^I-TAATTA\; and\; 5^I-TAAAAAA$. We have investigated the base specificity for DNA ISC induced by bizelesin using oligomers containing the cross-linkable sequence $5^I-TAATTA\; and\; 5^I-TAAAAAA$. in which "N" was either A, C, G, or T. An analysis of denaturing polyacrylamide gel showed that bizelesin is able to induce DNA ISC in the duplex oligomer containing sequences $5^I-TAATTA\; and\; 5^I-TAAAAAA$. The formation of interstrand crosslinking did not occur in the sequences $5^I-TAATTA\; and\; 5^I-TAAAAAA$. DNA strand cleavage assay to determine the cross-linking site within $5^I-TAATTA$sequence showed that bizelesin alkylates guanine. These results demonstrate that bizelesin is able to induce DNA ISC at guanine but not at cytosine or thymine. In addition, guanine adducts have been found to be susceptible to DNA strand cleavage by exposure to hot piperidine. The extent of DNA strand cleavage, however, was not 100% efficient in either neutral pH buffer or hot piperidine.

• Analytical Science and Technology
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• v.17 no.1
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• pp.23-28
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• 2004

Trace amount of uranyl (II) has been determined spectrophotometrically by measuring the optical density of the light blue yellowish coloured solutions formed by reaction between the metal ion and nicotinohydroxamic acid (NHx) in presence of different secondary ligands in strong isoamyl alcohol alkaline medium. The absorption maxima for both aqueous and extracted systems measured at their respective optimum pH were found to be 360 and 559 nm (DETA), 375 and 358 nm (EDA), 369 and 362 nm (piperidine), 354 and 341 nm (pyridine) and 363 and 336 nm (3 piperidine), 354 and 341 nm (pyridine) and 363 and 336 nm (3 - picoline), respectively at which Beer's law was obeyed. Effect of pH, reagent concentration, order of addition of reagent, time, temperature and solvent media on the absorption spectra have also been studied. Among the different systems studied, the shortest concentration range of uranyl(II) adhering to Beer's Law was 2.4 - 10.5 ppm observed for $UO_2(II)$ - NHx - DETA system in aqueous medium and also for iso amyl alcohol(IAA) extracted $UO_2$ - NHx - pyridine system was 2.4 - 7.8.

• Journal of the Korean Chemical Society
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• v.36 no.4
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• pp.598-602
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• 1992

2-Piperidylglycine will be a model compound for the synthesis of antitumor agent 593A. 2-Piperidylglycine may be synthesized by alkylation of glycine equivalent to C-2 position of piperidine ring. ${\delta}$-Valerolactam was reacted with trimethyl oxonium tetrafluoroborate to give 2-methoxy-1-piperideine. The imino ether was not condensed with ethyl phthalimidoacetate, one of glycine equivalents, but with ethyl nitroacetate to afford ethyl nitro-2-piperidylene acetate. The subsequent hydrogenation over Pt/C gave ethyl 2-piperidyl glycinate. Because the Z-configuration of the condensed product was assigned by nmr, the stereochemistry of ethyl 2-piperidyl glycinate different from that of Agent 593A.

• Bulletin of the Korean Chemical Society
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• v.31 no.7
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• pp.1859-1862
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• 2010

A convenient one-pot condensation route has been developed for obtaining 5-[(2-(piperidin-1-yl) quinolin-3-yl) methylene]-2,4-thiazolidinediones using multicomponents, 2-chloro-3-formyl quinolines, piperidine, 2,4-thiazolidinedione and safer medium/mediator, polyethylene glycol-400.

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.248.3-249
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• 2003

A series of tetrahydroaminoacridine and their analogues were synthesized. Tetrahydroaminoacridine(tacrine) is an anticholinesterase agent used in the treatment of Alzheimer's disease. Introduction of piperidine group at the para position enhanced anti-inflamatory activity for Alzheimer's disease. We investigated their ability to inhibit cyclooxygenase-1 and 2 isoforms. (omitted)

• YAKHAK HOEJI
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• v.30 no.4
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• pp.163-168
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• 1986

Thirteen compounds were synthesized by condensing the N-heterocyclic amines (piperidine, pyrrolidine, morpholine) and secondary aliphatic amines (dimethylamine, diethylamine) with 3,4-methylenedioxyphenylalkenoic acid chlorides for developing CNS depressants. Among them, N, N-diethyl-3,4-methylenedioxycinnamamide (IX) and N, N-dimethyl-5-(3,4-methylenedioxyphenyl)-2, 4-pentadienoic acid amicle (XII) exhibited strong activity in antagonism against pentylenetetrazole-induced convulsion, strychnine-induced convulsion and maximal electroshock seizure. N, N-Dimethyl-3, 4-methylenedioxycinnamide (VIII) showed more potent activity in antagonism against strychnine-induced convulsion and maximal electroshock seizure and in the prolongation of hexobarbital sleeping time.

• Archives of Pharmacal Research
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• v.22 no.4
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• pp.398-400
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• 1999

Sufentanil, a potent anilidopiperidine analgesic, was synthesized from a simple thiophenylethylamine via six sequence. The key parts of this synthesis involved an efficient construction of thiophenylethylpiperidone by aminomethano desilylation-cyclization followed by Swern oxidation and a direct regioselective N-nucleophilic spiral epoxide cleavage with aniline promoted by Lewis acids.

• Bulletin of the Korean Chemical Society
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• v.7 no.6
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• pp.416-421
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• 1986

The solvent coordination effect on the excited state processes of Mg(II)- and Zn(II)-phthalocyanines has been described. The triplet state of these compounds decays with mixed first and second order kinetics or mainly second order kinetics depending on the solvents used. The first order component of the rate constants decrease along with the series, dimethylsulfoxide (5-coordinated), 1-chloronaphthalene (4-coordinated) and piperidine (6-coordinated), while the second order rate constant is dependent on the diffusion rate constant of the solvents. The excited state quenching by methylviologen or p-benzoquinone is discussed. And ion recombination rate constant is given.

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.181.1-181.1
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• 2003

2-Aminoindan derivatives has been shown the serotonergic activities. In order to find new serotonergic agent, we trid to enlarge the indan ring. 3, 4-Dimethoxybenzaldehyde, used as starting material was condensed with malonic acid, piperidine to form 3, 4-dimethoxycinnamic acid. It was catalytically hydrogenated and sudsequently cyclized by Friedel-Crafts acylation reaction to yield 5, 6-dimethoxyindanone. This compound was reacted with pyrrolidine and then acrylamide to be synthesized the 3-membered ring. (omitted)

• Journal of the Korean Chemical Society
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• v.39 no.8
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• pp.657-665
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• 1995

The oxidation of various benzyl ethers and benzyl alkyl ethers to benzoates has been studied in two-phase system of $CH_3CO_2Et$ and aqueous NaOCl (6.6 mol eq.). The oxidant N-oxo-4-methoxy-2,2,6,6-tetramethylpiperidium bromide (N-oxoammonium salt) was prepared in situ and recycled by addition of 4-methoxy-2,2,6,6-tetramethylpiperidine-1-oxyl (0.03 mol eq., 4-methoxy-TEMPO), co-catalyst KBr (0.03mol eq.) and second oxidant NaOCl. Thus the catalytic amount of 4-methoxy-TEMPO was used. An adjustment of the pH value of below 8.0 was also required for this reaction with 2.5 hr of reaction time at 0∼5$^{\circ}C$. Under these conditions benzyl ethers were oxidized to benzoates. The selectivity of oxidation of benzyl alkyl ethers is dependent on the acidity of hydrogen and steric effect of alkyl group.