• Bulletin of the Korean Chemical Society
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• 제18권7호
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• pp.711-714
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• 1997

In an effort to enhance the lipophilicities, thereby, the penetration into the cell membrane and to increase the antitumor activities of modified derivatives of 2',3'-didehydro-3'-deoxythymidine (d4T, 1), derivatives of 1 were designed and synthesized. Starting from thymidine, 1, 2',3'-didehydro-3'-deoxythymidine-5'-phosphate, disodium salt (d4T-p, 7), and two nicotinate esters of 1; 2',3'-didehydro-3'-deoxy-5'-O-(3-pyridinylcarbonyl)thymidine (d4T-NA, 5) and 2',3'-didehydro-3'-deoxy-5'-phosphoryl-O-(3-pyridinylcarbonyl)thymidine (d4T-p-NA, 8) were synthesized. The lipophilicities of the synthesized compounds were measured by P-values and antitumor activities of those were estimated against mouse leukemia P388, murine mammary carcinoma FM3A, and human histiocytic lymphoma U937 tumor cells in vitro. Although the lipophilicities of the nicotinate esters, 5 and 8 were increased 2.75- and 9.71-fold relative to that of 1 and 7, respectively, the synthesized compounds, 1, 5, 7, and 8 were found to be inactive against P388 and FM3A cells except weak antitumor activity against U937 cell.

• 약학회지
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• 제38권3호
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• pp.322-331
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• 1994

For the development new cephalosporin antibiotics with aminothiazolmethoxyimino moiety in the C-7 position and triazolthiomethyl moiety in the C-3 position of cephem ring, $7{\beta}$-[(z)-2-(2-aminothiasol-4-yl)-2-(methoxyimino)acetamido]-3-[5-(aryl or het.)-4-phenyl-4H-1,2,4-triazol-3-yl]thiomethyl-3-cephem-4-carboxylic acids were synthesized. These compounds were tested for antimicrobial activitiy in vitro against ten species of microorganisms. It showed remarkable antibacterial activity against Bacillus subtilis ATCC 6633, Micrococcus luteus ATCC 9341 and Escherichia coli ESS. The antibacterial activity of most new compounds showed more active than cefazoline, but these compounds were lower active than cefotaxime against Pseudomonas aeruginosa IFO 13130.

• 약학회지
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• 제37권3호
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• pp.295-305
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• 1993

In order to develop oral cephalosporin having a new substituent at 3 position, the synthesis of cephalosporins modified at C-3 and the effect of the substituents on the oral absorption is studied. 7-[(Z)-2-(2-Aminothiazole- 4-yl)-2-methoxyiminoacetamidol-3-[4-(2-pyridyl )piperazinyl] thiocarbonylthiomethyl-3-cephem-4-carboxylic acid (CEN1) and 7-[(Z)-2-(2-aminothiazole-4-yl)-2-methoxyiminoacetamido]-3-[4-(2-pyrimid yl)piperazinylthiocarbonylthiomethyl-3-cephem-4-carboxylic acid (CEN2) were synthesized from 4-(2-piridyl)piperazinyl dithiocarbamate potassium salt or 4-(2-pirimidyl)piperazinyl dithiocarbamate potassium salt and cefotaxime. Also pivaloyloxymethyl esters of CEN1 and CEN2, pivaloyloxymethyl 7-[(Z)-2-(2-aminothiazole-4-yl)-2-methoxyiminoacetamido]-3-[4-(2-pyridyl )piperazinyllthiocarbonylthiomethyl-3-cephem-4-carboxylate (CENIP) and pivaloyloxymethyl 7-[(Z)-2-(2-aminothiazole-4-yl)-2-methoxyiminoacetamidol-3- [4-(2-pyrimid yl)piperazinyllthiocarbonylthiomethyl-3-cephem-4-carboxylate (CEN2P) were synthesized. The in vitro activities of two new oral cephalosporins, CEN1 and CEN2, were compared with the in vitro activities of cefaclor and cefotaxime against a variety of bacterial species. CEN2 has a broad antibacterial spectrum covering Gram-positive and Gram-negative bacteria, similar to that exhibited by CEN1 and cefotaxime. CEN1 and CEN2 were more active in vitro than cefaclor against Streptococcus pyogenes, Klebsiella aerogenes and Enterobacter cloacae.

• 생명과학회지
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• 제13권6호
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• pp.943-949
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• 2003

7번 위치에 하롤겐이 치환된 여로종류의 퀴놀론 모핵과 시스 또는 트란스-3-아미노-4-메틸오메틸피롤리딘을 반응시켜 7-(시스 또는 트란스-3-아미노-4-메틸티오메틸피롤리디닐) 퀴롤론-3-카르복실산의 신규 항균제를 합성하였다. 새롭게 합성된 퀴놀론의 약효는 그람양성균에 대해 대조물질인 시프로플로삭신보다 매우 탁월하였고, 녹농균이외의 그람음성균에 대해서도 대조물질과 거의 유사하였다. 그리고 임상에서 문제가 되고 있는 메티실린 내성 포도상구균(MRSA)에 대한 신규 퀴놀론의 약효는 더욱더 향상되어진 것으로 나타났다.

• 대한수의학회지
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• 제26권2호
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• pp.321-327
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• 1986

The anthelmintic efficacy of Albendazo1e and Ivermectin against gastrointestinal nematodes, trematodes and cestode was tested in naturally infected Korean native goats. Albendazole was medicated at a dose rate of 10mg/kg of body weight orally and Ivermectin was injected at a dose rate of 0.2mg/kg of body weight subcutaneously. The efficacy was measured by faecal examinations on the day 7th and the day 14th :after treatment. The results obtained were summarized as follows : 1. The efficacy of Albendazole against trematodes and cestode was shown 91.7% in Fasciola hepatica, 68.8% in Paramphislomum spp., 66.7% in Eurytrema pancreaticum and 100% in Moniezia expansa(cestode). 2. The efficacy of Ivermectin against trematodes and cestode was shown 38.8% in Fasciola hepalica, 26.1% in Paramphistomum spp., 22,2% in Eurytrema pancreaticum and 100% in Moniezia expansa(cestode). 3. The anthelmintic efficacy of Albendazole against gastrointestinal nematodes was shown 97.7% in Haemonchus contorus and 100% in Oesophagostomum spp., Ostertagia spp., Bunostomum trigonocephalum, Trichostrongylus spp., Strongyloides papillosus and Cooperia spp. 4. The efficacy of Ivermectin against gastrointestinal nematodes was shown 96.6% in Haemonchus contortus, 94.1% in Trichostrongylus spp. and 100% in Oesophagostomum spp., Ostertagia spp., Bunostomum trigonocephalum, Strongyloides papillosus and Cooperia spp.

• 한국환경보건학회지
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• 제7권2호
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• pp.107-111
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• 1981

Thirteen Carbanilides, P-chloro, bromo, methyl, ethyl, methoxy and ethoxy carbanilides, 4,4'-dichlorocarbahilide, and 4-bromo, methyl, ethyl, methoxy and ethoxy 4'-chlorocarbanilides have been newly synthesized by reacting P-phenetidime, P-anisidime, anilime, P-chloroanilime, P-bromoanilime, P-methoxy aniline, and P-ethoxy anilime with phenyl and P-chlorophenyl isocyanate, respectively. The compounds generally exhibited antibacterial activity against Escherichia coli, and staphylococcus aureus. The results obtained were as follows 4-chlorocarbanilide and 4,4'-clichlorocarbanilide were active against Eschrichia Coli, and Staphylococcus aureus at the concentration of 50 ug/ml. 4-methyl-4'-chloro carbanilide, and 4-ethoxy-4'-chloro carbanilide were active against Escherichia Coli at the concentration of 100ug/ml. 4-methyl-4'-chloro canbanilide were active against Staphylococcus aureus at the concentration of 50ug/ml.

• 대한수의학회지
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• 제36권2호
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• pp.395-403
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• 1996

Monoclonal antibodies(MAbs) against field isolates of the bovine rotavirus A strain(G6), V strain(G10) and reference I-801 strain(G8) were produced and characterized. Six MAbs(4C2, 4D9, 5E1, 5E7, 5D5, 3E4) against A strain had neutralizing activity and reacted only with the G6 bovine rotaviruses determined by fluorescence focus neutralization (FFN) test. Otherwise, five neutralizing MAbs(1G2, 2G6, 5E2, 5E12, 5H7) against I-801 strain neutralized the G6 and G8 bovine rotaviruses. Five non-neutralizing MAbs(5F12, 7F12, 5E11, 2A11, 2B12) were VP6-specific and cross-reacted with all bovine and porcine rotaviruses examined by fluorescence antibody(FA) test. None of the MAbs reacted with bovie viral diarrhea virus(BVDV) and bovine coronavirus(BCV) determined by FA and FFN test.

• Archives of Pharmacal Research
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• 제29권11호
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• pp.957-962
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• 2006

A novel series of 2-(m-Chlorobenzyl)-4-substituted-1, 1, 3-trioxo-2H, 4H-pyrazolo[4, 5-e][1, 2, 4] thiadiazines (7a-k) were synthesized, and evaluated for their anti-HIV replication in MT-4 cell cultures. Compound (7a) showed activity against HIV-1-induced cytopathicity, with an $EC_{50}$ value of $45.6\;{\mu}M$, but none of the compounds exhibited inhibitory activity against HIV-2.

• 한국식품영양학회지
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• 제19권4호
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• pp.526-531
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• 2006

자몽 종자 추출물의 항균성을 조사하기 위하여 그람 양성균인 Bacillus cereus, Bacillus subtilis, Listeria monocytogenes와 그람 음성균인 Escherichia coli, Salmonella enteritidis, Serratia marcescem를 대상으로 하여 최소 저해 농도, 생육 저해 활성, 콜로니 형성 저해 활성을 실험하였다. 그람 양성균에 대한 자몽 종자 추출물의 최소 저해 농도는 12.5 ppm정도로 상대적으로 낮았으며, 그람음성균의 최소저해 농도는 50ppm 이상으로 상대적으로 높았다. 균주의 증식에 대한 생육 저해 활성을 조사한 결과 Bacillus cereus는 1ppm 이하, Bacillus subtilis는 6.25 ppm, Listeria monocytogenes는 1ppm 이하, Escherichia coli는 6.25 ppm, Salmonella enteritidis는 25 ppm Serratia marcescem는 25pp부터 생육이 저해되었다. 그람 양성균의 콜로니 형성 저해활성은 Bacillus cereus는 93.9%, Bacillus subtilis는 94.0%, Listeria monocytogenes는 99.9%, 그람 음성균의 콜로니 형성 저해 활성은 Escherichia coli는 4.4%, Salmonella enteritidis는 82.7%, Serratia marcesem는 86.4%로, 그람 양성균에 대해서는 높은 저해 활성을 보였으며, 그람 음성균에 대해서는 비교적 낮은 저해 활성을 보였다.

• 한국식품영양과학회지
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• 제37권4호
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• pp.410-415
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• 2008

본 연구는 Ames test와 SRB assay를 통해 SK와 SDK 메탄올 추출물을 이용하여 항돌연변이원성과 세포독성 효과에 대해 살펴보았다. S. Typhimurium TA98과 TA100 균주를 사용하여 돌연변이원성을 실시한 결과 SK와 SDK 메탄올 추출물 자체의 돌연변이원성은 없었으며, MNNG와 4NQO를 유도하여 높은 항돌연변이 효과를 나타내었다. S.Typhimurium TA98에서 4NQO를 유도하여 SDK($200{\mu}g$/plate) 메탄올 추출물 처리 시에 71.4%의 억제효과를 나타내었으며, 반면에 S. Typhimurium TA100에 4NQO와 MNNG의 돌연변이를 유도하였을 때 각각 56.1%와 83.6%의 억제율을 보였다. 암세포 성장 억제효과를 검토한 결과 샘플처리 시 농도 의존적 증가를 보였으며, SDK 메탄올 추출물 1 mg/mL 첨가 시 HeLa, Hep3B, MCF-7, AGS 및 A549에서 각각 61.5%, 61.3%, 51.4%, 57.9% 및 77.7%의 억제효과를 나타내었다. SK 메탄올 추출물 첨가 결과 $51{\sim}58%$ 정도의 억제효과를 보였다. 대조적으로 SDK 메탄올 추출물을 1mg/mL 첨가 시 293에서 $2{\sim}38%$의 세포독성을 나타내었다.