• Applied Biological Chemistry
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• 제37권6호
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• pp.516-521
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• 1994

새로운 17종의 imazapyr 유도체인 3-(N-methyl-N(X)-치환-phenylaminooxoacetyl)-2-(4-isopropyl-5-oxo-2-imidazoline-2-yl)pyridine, 6을 합성하고 3-(N-methyl-N(X)-치환-phenylaminooxoacetyl group중의 X-치환기 변화에 따른 구조와 옥수수(Zea mays L.)와 참비듬(Amaranthus viridis L.)에 대한 발아 전의 제초활성에 미치는 관계(SAR)를 검토 한 바, 옥수수의 경우에는 MR상수의 적정값(optimal value)이 $5.56\;cm^3/mol$이었으므로 이 값보다 크거나 작을수록 제초활성이 작았다. 참비듬의 경우에는 $L_1$상수의 적정값이 3.34 A이므로 이 값에 가까울수록 제초활성이 클 것임을 알 수 있었다. 특히, 2,5-difluoro group 치환체, 6i는 참비듬에 가장 큰 제초활성을 나타내었으나 옥수수에는 가장 작은 제초활성을 미치므로써 현저하게 두 초종간에 선택성을 나타내는 화합물이었다.

• Bulletin of the Korean Chemical Society
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• 제18권4호
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• pp.409-415
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• 1997

Several calixarene derivatives of 5,11,17,23-tetra-tert-butyl-25-(3,5-dinitrobenzoyloxy)-26,27,28-trihydroxycalix[4]arene 2 were synthesized by the reaction of 2 with several acyl and alkylating agents in the presence of base such as pyridine and K2CO3 in THF. Acylation of monobenzoylated p-tert-butylcalix[4]arene 2 yielded their corresponding 1,3-diacylated calix[4]arenes 3a-3g. On the other hand, alkylation of 2 produced a variety calix[4]arene derivatives such as 1,2- and 1,3-disubstituted calix[4]arenes 4a-4c, 4e-4f, or 1,2,4-trisubstituted calix[4]arene 4d. 1,2-Disubstituted calix[4]arenes are chiral. All derivatives exist as a cone conformation based on NMR studies.

• 약학회지
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• 제41권2호
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• pp.187-194
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• 1997

For the development of antifungal agents, modification of naftifine which exhibits significant antimycotic activity was performed by replacing the naphthalene ring of it to hete ro cyclic rings such as morpholine. benzothiazole, piperidine and pyridine derivatives. The synthesized compounds were tested in vitro antifungal activity against five different fungi with naftifine as a comparative antimycotic molecule. From the biological evaluation two compounds, (E)-N-(3-phenyl-2-propenyl)-N-(4-piperidinylmethyl)amine(3d) and (E)-N-(3-phenyl-2-propenyl)-N-(3-pyridylmethyl)amine(3f) showed relatively noticeable activity(MIC=50${\mu}g$/ml). On the other hand, the other compounds had no activity.

• 대한화학회지
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• 제20권5호
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• pp.406-416
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• 1976

Pyridine관여 탈수소 효소는 $N^1$-alkylnicotinamide chloride 유도체에 의하여 저해 작용을 받고 있는 바 저해제이 농도 변화에 따른 효소 저해작용이 가역 또는 비가역 불활성화 반응에 기인하는지의 여부를 밝혀 보기 위하여 토끼 근육으로 부터 유리한 L-${\alpha}$-glycerophosphate dehydrogenase를 사용하여 연구하였다. 이 효소의 저해작용은 상용한 저해제 유도체의 농도가 희박했을 경우 가역적인 효소저해 반응을 보여주고 있으나 저해제의 농도가 증가함에 따라 점차 비가역적인 효소 불활성화로서 나타남을 알았으며 이러한 비가역 불활성화 반응은 저해제의 농도가 증가함에 따라 형성될 수 있는 micelle 구조의 미세분자와의 결합에 의한 효소의 변성에 기인할 것이라고 결론을 얻었다.

• Archives of Pharmacal Research
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• 제25권3호
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• pp.258-269
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• 2002

2-Thiouracil-5-sulfonylchloride 1 reacted with a series of aromatic and heterocyclic amines to give 2a-j. The same compound 1 was reacted with a series of sulphonamides giving different sulphonamides of type 3a-e. On the other hand compound 1 was allowed to react with p-aminoacetophenone givining compound 4 which in turn was allowed to react with derivatives of alkyl thiosemicarbazides to give thiosemicarbazones of type 5a-e, also compound 4 was monobrominated to give compound 6 which in turn was reacted thiosemicarbazones of some aldehydes to give the corresponding thiazole derivatives 7a-f. In the same time compound 4 was reacted with a series of aromatic and heterocyclic aldehydes givining chalcones 8a-g (Claisen-Schemidt reaction). Also compound 4 was allowed to react with a series of aromatic and heterocyclic aldehydes, ethyl cyano acetate and/or malononitrile, and ammonium acetate giving pyridine derivatives 9a-d and 10a-e respectively. The biological effects of some of the new synthesized compounds was also investigated.

• Archives of Pharmacal Research
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• 제13권4호
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• pp.351-354
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• 1990

2, 3-diphenyl-4-cyano-pyrrole-5-thione (4) was either by the reaction of benzoin (1) and cyanothioacetamide (3) followed by cyclization using AcOH/sodium acetate or by refluxing a mixture of benzoin (1) and cyanothioacethamide in pyridine to afford directly 4. Several new pyrrole and pyrazole derivatives were synthesised using 4 as synthon. The structure of the newly synthesised derivatives were based on celemental and spectral data studies. Methylation of the SH group in 4 afforded 5. Reaction of 4 with ethyl bromo acetate afforded (6). Treatment of (5) and (6) with hydrazine hydrate afforded the same pyrazole derivative (10) through the intermediate (9). Treatment of 6 with aniline and phenylhydrazine afforded the pyrrole derivatives 8a, b respectively. Treatment of 6 while dill HCI gave 2, 3-diphenyl-4-cyano-pyrrole-5-one (7). Treatment of 6 with $NH_3$/EtOH afforded the amidic derivatives (11) with treatment of 6 $NH_3$/ heat then acidification it gave the carboxylic derivatives (12).

• Corrosion Science and Technology
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• 제12권2호
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• pp.65-78
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• 2013

The present investigation deals with the corrosion inhibition of mild steel in 1M $H_2SO_4$ with 1, 4-dihydro pyridine and its derivatives prepared using microwave activation method. The synthesis of inhibitor was confirmed by IR spectra. The effect of 1, 4-dihydropyridine derivatives on the corrosion inhibition of mild steel in 1M $H_2SO_4$ was studied using weight loss and electrochemical polarization techniques. Influence of temperature (303-333K) and synergistic effect of halide ions ($I^-$, $Br^-$ and $Cl^-$) on the inhibition behaviour was also studied. Corrosion products on the metal surface were analyzed by scanning electron microscopy (SEM) and a possible mechanism of inhibition by the compounds is suggested. Thermodynamic parameters were calculated using weight loss data in order to elaborate the mechanism of corrosion inhibition. Polarization measurements revealed that the studied compounds acted as mixed type inhibitor but slightly anodic in nature. Electrochemical impedance measurements revealed that the compounds were adsorbed onto the carbon steel surface and the adsorption obeyed the Langmuir adsorption isotherm. The synergistic effect of halide ions on the IE increases with increase in concentration. The IE obtained from atomic absorption spectrophotometric studies was found to be in good agreement with that obtained from the conventional weight loss method. SEM revealed the information of a smooth, dense protective layer in presence of the inhibitors.

• 통합자연과학논문집
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• 제10권2호
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• pp.85-94
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• 2017

Fibroblast growth factor receptor (FGFR) belongs to the family of receptor tyrosine kinase. They play important roles in cell proliferation, differentiation, development, migration, survival, wound healing, haematopoiesis and tumorigenesis. FGFRs are reported to cause several types of cancers in humans which make it an important drug target. In the current study, HQSAR analysis was performed on a series of recently reported 1H-Pyrazolo [3,4-b]pyridine derivatives as FGFR antagonists. The model was developed with Atom (A) and bond (B) connection (C), chirality (Ch), hydrogen (H) and donor/acceptor (DA) parameters and with different set of atom counts to improve the model. A reasonable HQSAR model ($q^2=0.701$, SDEP=0.654, NOC=5, $r^2=0.926$, SEE=0.325, BHL=71) was generated which showed good predictive ability. The contribution map depicted the atom contribution in inhibitory effect. A contribution map for the most active compound (compound 24) indicated that hydrogen and nitrogen atoms in the side chains of ring B as well as hydrogen atoms in the side chain of ring C and the nitrogen atom in the ring D contributed positively to the activity in inhibitory effect whereas, the lowest active compound (compound 04) showed negative contribution to inhibitory effect. Thus results of our study can provide insights in the designing potent and selective FGFR kinase inhibitors.

• Bulletin of the Korean Chemical Society
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• 제23권9호
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• pp.1309-1338
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• 2002

The fluorescence and photoisomerization quantum yields of trans-1-(9-anthryl)-2-(4-pyridyl)ethene (t-4-APyE), 1-(10-methyl-9-anthryl)-2-(4-pyridyl)ethene (t-4-MeAPyE), and 1-(10-chloro-9-anthryl)-2-(4- pyridyl)ethene (t-4-ClAPyE) were measured in cyclohexane, acetonitrile, and methanol at room temperature.Polar solvents result in the drastic reduction of fluorescence quantum yield and increase of photoisomerization quantum yield for all three compounds. These results are probably due to the stabilization of intramolecular charge transfer (ICT) excited state in polar solvent. The higher contribution of ICT in the presence of more electron-donating methyl substituent, manifested by largest positive fluorescence solvatochromism, indicates that the pyridine ring acts as an electron acceptor. Protonation or methylation makes pyridine ring stronger electron acceptor and causes long-wavelength ground state charge transfer absorption band and complete quenching of fluorescence. The fluorescence from t-4-APyE derivatives can be switched off responding external stimuli viz. medium polarity, protonation, or methylation.

• 대한화학회지
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• 제56권4호
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• pp.464-467
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• 2012

A novel chitosan derivative with double quaternary ammonium salt-2-pyridine-acetyl-N-trimethyl chitosan chloride (PATMCS) was synthesized and the antioxidant activity of PATMCS against hydroxyl radicals was assessed. The results indicated that PATMCS had potent hydroxyl scavenging activity. The $IC_{50}$ of PATMCS was 0.13 mg/mL. PATMCS showed 100% scavenging effect at a dose of 0.8 mg/mL which markedly better than that of N-trimethyl chitosan chloride (TMCS). It was confirmed that quaternary chitosan derivatives showed potent antioxidant activity. PATMCS has double quaternary ammonium salt structure in the molecules. Therefore, the antioxidant activity of PATMCS was better than TMCS. The above results are theoretically fundamental for further development and making use of chitosan resources to prepare new antioxidants.