• Archives of Pharmacal Research
• /
• 제26권2호
• /
• pp.107-113
• /
• 2003

Several fused triazolo and ditriazoloquinoxaline derivatives such as 1-aryl-4-chloro-[1,2,4]triazolo[4,3-a]quinoxalines (3a-d), 4-alkoxy[1,2,4]triazolo[4,3-a]quinoxalines (4a,b), 4-substituted-amino-[1,2,4] triazolo[4,3-a]quinoxalines (5a-h), 1-(aryl)-[1,2,4]triazolo[4,3-a]quinoxalin-4(5H)-thione (6), 4-(arylidenehydrazino )-1-phenyl-[1,2,4]triazolo[4,3-a]quinoxalines (10a-e) and [1,2,4]ditriazolo[4,3-a:3',4'-c]quinoxaline derivatives (11-13) have been synthesized and some of these derivatives were evaluated for antimicrobial and antifungal activity in vitro. It was found that compounds 3a and 9b possess potent antibacterial activity compared to the standard tetracycline.

• 한국정보디스플레이학회:학술대회논문집
• /
• 한국정보디스플레이학회 2003년도 International Meeting on Information Display
• /
• pp.504-508
• /
• 2003

New banana-shaped achiral compounds, 4-chloro-1,3-phenylene bis [4-4(3-fluoro-9-alkenyloxy) phenyl-iminomethylbenzoate]s and 4-chloro-1,3-phenylene bis [4-4-(3-fluoro-10-alkanyloxy) phenyliminomethyl benzoate]s were synthesized by varying the substituent (X=H, F, or Cl); their electrooptical properties are described. The smectic phases, including a switchable chiral smectic C ($SmC^{\ast}$) phase, were characterized by differential scanning calorimetry, polarizing optical microscopy, and triangular method. The presence of vinyl end group at the terminals of linear side wings in the banana-shaped molecules induced a decrease in melting temperature. The smectic phase having the undecenyloxy group such $as-(CH_2)_9CH=CH_2$ showed ferroelectric switching, and its value of spontaneous polarization on reversal of an applied electric field was 2250 $nC/cm^2$, while the value of spontaneous polarization of the smectic phase having the decanyloxy group such as $-(CH2)_9CH_3$ was 3700 $nC/cm^2$. We could obtain the ferroelectric phase with low isotropic temperature by varying the end group at the terminals of linear side wings in the banana-shaped achiral molecules.

• Applied Biological Chemistry
• /
• 제23권2호
• /
• pp.131-139
• /
• 1980

물리화학적(物理化學的) 특성을 달리하는 청주토와 충주토에 제초제(除草劑) TOK를 일정(一定) 농도로 처리하여 담수상태로 일정기간(一定期間) 배양한 후 생성(生成)된 분해산물(分解産物)과 분해(分解)에 관여한 토양미생들에 관하며 연구(硏究)를 행(行)한바 다음과 같은 결과(結果)를 얻었다. 1. TOK를 500ppm으로 청주토와 충주토에 처리하고 2, 4, 6개월간(個月間) $30^{\circ}C$에서 배양시 주(主)된 분해산물(分解産物)로 4-Chloro-4'-amino diphenyl ether, 2, 4-dichloro -4'amino diphenyl ether(amino-TOK), N-[4'-(4-chlorophenoxy)] phenyl acetamide, 및 N-[4'-(4-Chlorophenoxy)] phenyl formamide의 순(順)으 생성(生成)되었다. 2. 상기(上記) 토양중에 상기와 같은 농도로 TOK를 처리하면 nitro기(基)의 amino기(基)로의 환원, 탈염소화, acetylation 및 formylation이 주(主)로 일어나고 ether결합(結合)의 붕괴는 일어나지 않았다. 3. pH가 보다 높고 토성이 Clay loam이고 C.E.C가 높은 충주토에서 TOK의분해(分解)는 더 용이 하게일어 났다. 4. 상기(上記)와 같은 변화가 생기면 TOK의 독성(毒性)은 현저히 감소되어 환경의 오염원으로서의 기능은 약화된다. 5. TOK를 처리한 토양으로부터 12균주의 세균(細菌)을 분리(分離)하였다. 6. 분리한 토양미생물의 순수배양액중에서 TOK를 배양시킨 결과 청주토에서 분리한 T-1-1균주는 거의 분해력(分解力)이 없고 T-2-3 균주가 가장분해력(分解力)이 우수한 것으로 보인다. 7. 분리한 균주에 의한 TOK의 분해(分解)는 주로(主) nitro기(基)의 amino기(基)로의 환원이었다. 8. 충주토의 citrate buffer추출액은 청주토의 citrate buffer추출액보다 TOK를 amino-TOK으로 환원시키는 능력이 컸다.

• Applied Biological Chemistry
• /
• 제47권4호
• /
• pp.414-421
• /
• 2004

새로운 5-methyl-3-phenylisoxazolin-5-yl)methoxy-2-chloro-4-fluorobenzenes 유도체들의 구조 변화에 의한 벼(Orysa sativa L.)와 논피 (Echinochloa crus-galli) 뿌리와 줄기 부위의 protox 저해활성에 대한 3차원적 구조-활성관계(3D-QSAR)에 근거하여(성낙도, 등 (2004) 한국응용생명화학회지 47(3), 351-356) 비교분자 유사성 지수분석(CoMSIA) 방법으로 연구하였다. 두 초종의 부위별 protox 저해활성에 관한 CoMSIA 모델들은 수소결합 주게장이 제외된 입체장, 정전기장, 소수성장, 수소결합 받게장 등으로 조합된 CoMSIA장과 부가적 설명 인자로서 LUMO 분자 궤도장, 몰라 굴절을(MR) 및 쌍극자 능율(DM) 등이 추가된 조건에서 유도되었다. 방제 대상인 논피에 대한 모델이 벼에 대한 모델보다 양호하였으며 논피에 대한 모델은 cross-validated $r^2\;_{cv.}$값$(q^2=0.871{\sim}0.913)$과 non cross-validated $r^2\;_{ncv.}$값$(0.936{\sim}0.920)$ 그리고 PRESS 값$(0.255{\sim}0.273)$에 근거하여 매우 좋은 예측성을 나타내었다. 그리고 protox 저해 활성은 분자의 입체장$(5.4{\sim}15.7%)$ 및 소수성장$(68.0{\sim}84.3%)$과 높은 상관성을 보였다. 이같은 CoMSIA 분석결과, 논피에 대한 선택적인 protox 저해활성은 C-phenyl 고리상 ortho-위치가 steric bulky 할수록 클 것으로 예상되었다.

• 약학회지
• /
• 제41권6호
• /
• pp.829-836
• /
• 1997

Studies on the effect of quinones on cardiac function has been conducted with normal hearts. But not with injured hearts, I.e. ischemia/reperfusion-injured heart. Quinone compounds are known to produce oxygen free radicals during metabolism, and for this reason, quinones are implicated in the aggravation of ischemia/reperfusion injury or cardioprotection, as in the case of ischemic preconditioning depending on the experimental conditions. The present study was carried out to examine the effect of 2-chloro-3-(4-cyanophenylamino)-1.4-naphthoquinone (NQ-Y15) on cardiac function of ischemic/reperfused and normal rat hearts. In isolated perfused hearts, various functional parameters such as left ventricular developed pressure (LVDP), left ventricular end-diastolic pressure (EDP) and maximum positive and negative dP/dt ($[\pm}dP/dt_{max}$), time to contracture, heart rate (HR) and coronary flow rate (CFR) were measured before and 30 min after dosing and following 25 min ischemia/30min reperfusion. NQ-Y15 increased LVDP, +dP/$d_{max}$and -dP/$dt_{min}$ by 18%. 30%, and 40%, respectively. There were no significant changes in other haemodynamic parameters. After ischemia/reperfusion injury, pretreatment with NQ-Y15 induced a significant decrease in LVDP and $[\pm}dP/dt_{max}$, but an increase in EDP. LDH-release was not significantly increased. These results suggested that NQ-Y15 may augment the ventricular contractility but it makes hearts more vulnerable to ischemia/reperfusion injury.

• 대한화학회지
• /
• 제8권2호
• /
• pp.47-56
• /
• 1964

展開한 페이퍼크로마토그램을 韓國 Triga-Mark-Ⅱ 硏究用 原子爐의 뉴마딕튜부施設(中性子線束; 1.5{\times}$10^{12}n/cm^2$, sec)을 利用하여 照射하여 본 結果 크로마토그램上에 展開된 스폿트(spot)를 定性的으로 確認할 수 있었다. 有機하로겐 化合物(크로로酸, 크로로에스테르, 沃化物, 及 弗化物)에 있어서 一般發色法으로서는 明確한 着色스폿트(spot)를 나타내지 못한 것에 있어서도, 이 方法으로서 展開된 스폿트를 明確히 區別할 수 있었다. 濾紙成分의 放射化에 依한 誤差를 減少시키기 爲하여 濾紙두께 補正 及 放射化度 補正을 硏究한 結果, 濾紙두께 補正 及 放射能崩壞 補正法을 究明하였으며, 이 方法으로 스폿트를 放射化하여 定性分析하는데 좋은 結果를 얻을 수 있었다. 有機하로겐化合物의 分析 及 確認에 있어서의 이 方法의 效用性에 關하여 論議하였다. 濾紙相으로는 正常相 及 逆相을 함께 使用하였다.

• Archives of Pharmacal Research
• /
• 제19권1호
• /
• pp.71-73
• /
• 1996

The molecular structure of pirprofen, 3-chloro-4-(2,5-dihydro-1H-pyrrol-1-yl)-.alpha.-methyl-benzeneacetic acid, was determined by single crystal X-ray diffraction analysis. The compound was recrystallized from a mixture of chloroform and toluene in triclinic, space group P over $\bar1,\; with\; a=4.577(1),\; b=11.213(2),\; C=12.485(2){\AA},\alpa.=107.39(1),\;\beta=97.79(1),\;\gamma=92.03(2),\; and Z=2$ The calculated density is $1.384 g/cm^3$. The structure was solved by the direct method and refined by full matrix least-squares procedure to the final R value of 0.034 for 1681 independent reflections. The non-aromatic dihydropyrrol group is found to be coplanar to the central aromatic ring. The molecules are dimerized through the intermolecular hydrogen bonds at the carboxyl group in the crystal.

• Bulletin of the Korean Chemical Society
• /
• 제5권1호
• /
• pp.21-23
• /
• 1984

The addition reactions of thioglycolic acid to ${\omega}$, ${\omega}$-diacetylstyrene derivatives were investigated. ${\omega}$, ${\omega}$-Diacetylstyrene derivatives easily undergo addition reactions with thioglycolic acid to form s-(2, 2-diacetyl-1-phenylethyl)-thiogycolic acid, s-[2,2-diacetyl-1-(methyl) phenylethyl]-thioglycolic acid, s-[2,2-diacetyl-1-(p-methoxy) phenylethyl]-thioglycolic acid and s-[2,2-diacetyl-1-(p-chloro) phenylethyl]-thioglycolic acid, respectively. The structures of these compounds were identified by neutralization equivalent, UV, IR, and NMR spectral data.

• 약학회지
• /
• 제33권5호
• /
• pp.273-279
• /
• 1989

2,3-Dichloro-1,4-naphthoquinone was reacted with o-fluoroaniline, p-sulfadiazine, p-acetoanline, N,N-dimethyl-1,4-phenylenediamine as a nucleophilic substitution to form 2-chloro-3-(N-arylamino)-1,4-naphthoquinones (1.-6.) in good yield. 2,3-Dibromo-1,4-naphthoquinone was also reacted with o-fluoroaniline, m-aminobenzoic acid, m-chloroaniline, morpholine, p-acetoaniline, N,N-dimethyl-1,4-phenylenediamine as a nucleophilic substitution to give 2-bromo-3-(N-arylamino)-1,4-naphthoquinones (7.-12.). These new compounds are expected to have a biological activities such as anticoagulant, cytotoxic.

• Bulletin of the Korean Chemical Society
• /
• 제9권3호
• /
• pp.115-117
• /
• 1988

The addition of L-cysteine without blocking amino and carboxyl groups to${\beta},{\beta}$-dinitrostyrene derivatives(11a-e) were investigated. ${\beta},{\beta}$ -Dinitrostyrene derivatives(11a-e) easily undergo addition reactions with L-cysteine to from s-(2,2-dinitro-1-phenylethyl)-L-cysteine(12a), s-[2,2-dinitro-1-(p-methyl)phenylethyl]-L-cysteine (12b), s-[2,2-dinitro-1-(p-methoxy)phenylethyl]-L-cystein e(12c), s-[2,2-dinitro-1-(p-chloro)phenylethyl]-L-cysteine (12d) and s-[2,2-dinitro-1-(p-nitro)phenylethyl]-L-cysteine( 12a), respectively. The structure of adducts were confirmed by means of spectral data, molecular weight measurement and elemental analysis.