• 약학회지
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• 제37권2호
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• pp.136-142
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• 1993

To a suspension of 1-cyclopropyl-6,8-difluoro-1,4-dihydro-7-{3,7-diazabicyclo[3.3.0]oct-1(5)-en-3-yl}-4-oxo-3-quinoline carboxylic acid(C1) in sodium hydroxide solution and water is added dropwise with stirring carbon disulfide. [6R-[6$\alpha$, 7$\beta$(Z)]]-7-[[[2-Amino-4-thiazoly)methoxyimino]-acetyl]amino]-3-[[[[7-( 3-carboxy-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-7-guinolonyl)-3,7-diazabicyclo[3.3.0]oct-1(5)-en-3-yl]thioxomethyl]thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-2-carboxylic acid (DACD) was synthesized from 1-cyclopropyl-6,8-difluoro-1,4-dihydro-7-[7-(mercapto) thioxomethyl-[3,7-dia zabicyclo[3.3.0]oct-1(5)-en-3-yl}]-4-oxo-3-quinoline carboxylic acid disodium salt(C2) and cefotaxime. The invitro activity of novel dual-action cephalosporin, DACD, was compared with the in vitro activities of CENO(cefotaxime 3'-norfloxacin dithiocarbamate), cefotaxime, and norfloxacin against a variety of bacterial species. In vitro activity of DACD was superior to that of norfloxacin against Streptococcus pyogenes. Against Gram-positive and Gram-negative bacteria, its activity was almost equal to that of CENO.

• Bulletin of the Korean Chemical Society
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• 제31권7호
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• pp.2003-2010
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• 2010

A new class of halobenzyloxy or alkoxy 1,2,4-triazoles and their hydrochlorides were synthesized through cyclization starting from commercially available phenylhydrazine. The structures were characterized by MS, IR and $^1H$ NMR spectra as well as elemental analyses. All the synthesized compounds were screened for their antibacterial activities in vitro against Staphylococcus aureus (ATCC29213), methicillin-resistant Staphylococcus aureus (N315), Bacillus subtilis, Escherichia coli (ATCC25922), Pseudomonas aeruginosa, Shigella dysenteriae, Eberthella typhosa, and antifungal activities against Candida albicans (ATCC76615), Aspergillus fumigatus by broth microdilution assay method. The results of preliminary bioassay indicated that 3-(2,4-difluorobenzyloxy)-1-phenyl-1H-1,2,4-triazole hydrochloride exhibited the best inhibitory activity with an MIC value of 56.25 ${\mu}M$ against P. aeruginosa superior to Chloramphenicol, and showed comparable activity with Chloramphenicol against E. coli (ATCC25922).

• International Journal of Industrial Entomology and Biomaterials
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• 제38권1호
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• pp.6-13
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• 2019

In the present study, we investigated the antifungal activity of methanol and ethanol extracts of different parts (leaves, twigs, and root bark) of mulberry plant against Alternaria alternata and Fusarium sp. Among them, the methanol and ethanol extracts of mulberry root bark exerted the highest inhibitory activity against the mycelial growth of A. alternata ($70.6{\pm}1.6$ to $80.8{\pm}6.7%$ and $58.7{\pm}0.0$ to $80.8{\pm}6.7%$, respectively) and Fusarium sp. ($15.5{\pm}2.7$ to $39.3{\pm}3.4%$ and $26.4{\pm}2.7$ to $47.6{\pm}4.8%$, respectively). In contrast, the methanol and ethanol extracts from mulberry leaves and twigs did not suppress the mycelial growth of these fungal species. Importantly, the methanol and ethanol extracts of mulberry leaves tended to even accelerate the mycelial growth of A. alternata and Fusarium sp. Therefore, the results of this study indicate that methanol and ethanol extracts of mulberry root bark can be used as control agents against A. alternata and Fusarium sp.

• 약학회지
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• 제44권4호
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• pp.318-324
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• 2000

9 New cephalosporin derivatives were synthesized and screened for antibacterial activities against various bacteria. (6R,7R) -7$\beta$-[(Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-(fluoromethoxyimino)acetamido]-3-[(2-hydroxycarbamoyl)-s-triazolo[1,5-a]-pyrimidin-7-yl]thiomethyl]-3-cephem-4-carboxylic acid sodium salt (compound 3) showed 2 fold enhanced in vitro activity against P. aerurginosa, compared to ceftazidime.

• Natural Product Sciences
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• 제25권1호
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• pp.23-27
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• 2019

From the pericarps of Litsea japonica (Thunb.) Jussieu, eighteen butanolide derivatives (1 - 18) were evaluated for their cytotoxic activity against HeLa, HL-60, and MCF-7 cells. Compounds 1-9 with 2-alkylidene-3-hydroxy-4-methylbutanolides structure exhibited cytotoxic activities against cancer-cell lines. Among them, compound 8 (litsenolide $D_2$) exhibited the most potent cytotoxicity against the tested cell lines, including HeLa, HL-60, and MCF-7, with $IC_{50}$ values of $17.6{\pm}1.3$, $4.2{\pm}0.2$, and $12.8{\pm}0.0{\mu}M$, respectively. Compound 8 induced apoptosis in a dose-dependent manner. Annexin V/Propidium Iodide (PI) double staining confirmed that 8 effectively induced apoptosis in MCF-7 cells. To the best of our knowledge, we have reported cytotoxic activity of butanolides from L. japonica against these cancer-cell lines for the first time.

• 약학회지
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• 제34권2호
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• pp.117-121
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• 1990

$7{\beta}$-[4-Phenyl-5-(3.4.5-trimethoxyphenyl)-4H-1.2.4-triazol-3-yl]thioacetoamidocepharosporanic acid was synthesized by condensation of 7-Aminocephalosporanic acid (7-ACA) with [4-Phenyl-5-(3.4.5-trimethoxyphenyl)-4H-1.2.4-triazol-3-yl] thioacetylchloride. This compound was tested for antimicrobial activity in vitro against nine species of microorganisms. It showed remakable antibacterial activity against Bacillus subtilis, Micrococcus luteus, and Staphylococcus aureus.

• International Journal of Industrial Entomology and Biomaterials
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• 제14권2호
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• pp.81-85
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• 2007

White Muscardine is the most common fungal disease of silkworm, Bombyx mori L. caused by the pathogenic fungus, Beauveria bassiana (Balsamo) Vuillemin. In the present investigation, an attempt has been made to screen locally available medicinal/ weed plants against Beauveria bassiana. Among the plant extracts (PE) tested, 5% aqueous crude extract of the bulb of Allium sativum (Garlic) has been found to be most effective against Beauveria bassiana. The radial growth of Beauveria bassiana in vitro was inhibited to the tune of 54.9% in aqueous extract and 54.4% in ethanolic extract of Allium sativum and correspondingly mycelial dry weight gave rise to 110.7 mg and 108.7 mg against 201.7 mg in control 15 days post treatment. Similarly, silkworm larvae topically inoculated with the Beauveria bassiana conidia ($1.8{\times}10^6/ml$) registered survival up to 53.0% against 0.0% in control after treatment with aqueous extract of Allium sativum. Simultaneously, as a preventive measure, silkworm larvae were put to rear in conidia contaminated seat paper instantly treated with aqueous extract of Allium sativum that also increased survival up to 61.0% against 4.6% in control. It is also observed that the plant extract is absolutely innocuous to silkworm.

• 미생물학회지
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• 제39권1호
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• pp.51-55
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• 2003

환경친화적인 미생물인산비료를 개발하기 위하여 불용성 인산을 가용화 시킬 수 있는 세균을 콩의 근권 토양으로부터 분리하였다. 분리균주의 분류학적 위치를 검토한 결과, Pantoea agglomerans로 동정되었다. 불용성 인산인 $Ca_{3}(PO_{4})_{2}$)로부터 가용성 인산을 생성하기 위한 최적 배지 및 배양조건은 glucose 3%, $NH_{4}NO_{3}$ 0.1%, $MgSO_{4}\cdot\7H_{2}O$ 0.02%, $CaCl_{2}\cdot\2H_{2}O$, 0.06%,초기 pH 7.5, 배양온도 $30^{\circ}C$이었으며, 최적조건에서 배양 5 일 후,898 mg/L의 인산이 생성되었다. 불용성 인산 가용화 기작은 유기산 생성에 의한 배양액의 pH감소와 밀접한 관계가 있었다. 분리균주는 $CaHPO_{4}$, hydroxyapatite로부터 각각 698,912 mg/L의 가용성 인산을 생성하였으나 $FePO_{4}\cdot\4H_{2}O$, $AIPO_{4}$로부터는 각각 28,19 mg/L.의 가용성 인산을 생성하였다.

• 미생물학회지
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• 제42권3호
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• pp.223-229
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• 2006

다기능성 농업용 미생물 제제를 개발하기 위하여 항진균능을 가진 불용성 인산 가용화 세균을 식물의 근권 토양으로부터 분리하였다. 분리균주의 분류학적 위치를 검토한 결과, Pseudomonas fluorescens RAF15로 동정되었다. P. fluorescens RAF15는 농작물의 잿빛곰팡이병균 Botrytis cinerea와 줄기썩음병균 Rhizoctonia solani의 생육을 억제할 수 있었다. 불용성 인산인 $Ca_3(PO_4){_2}$로부터 가용성 인산을 생성하기 위한 최적 배지 및 배양조건은 glucose 1.5%, urea 0.005%, $MgCl_2{\cdot}6H_2\;0.3%,\;MgSO_4{\cdot}7H_2O\;0.01%,\;CaCl_2{\cdot}2H_2O$ 0.01%, NaCl 0.05%, 배양온도 $30^{\circ}C$ 및 초기 pH 7.0이었으며, 최적조건에서 배양 5일 후 863 mg/L의 가용성 인산이 생성되었다. 불용성 인산 가용화는 유기산 생성에 의한 배양액의 pH 감소와 밀접한 관계가 있었다. P. fluorescens RAF15는 $10-35^{\circ}C$, 1-4% 염 농도 및 pH 2.0-11.0의 범위에서도 가용성 인산을 생성할 수 있었다. 본 균주는 $CaHPO_4,\;Ca_3(PO_4){_2}$ 및 hydroxyapatite에서 각각 971-1121 mg/L, 791-908 mg/L 및 844 mg/L의 가용성 인산을 생성하였다. 그러나 $FePO_2$ 및 $AlPO_4$의 경우, 생성된 가용성 인산의 농도는 각각 18 mg/L, 5 mg/L이었다.

• 약학회지
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• 제41권2호
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• pp.225-232
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• 1997

The in vitro antibacterial activity of DWP20367 (1-Cyclopropyl-6-fluoro-8-chloro-7-(2,7-diazabicyclo[3,3,0]oct-4-ene-7-yl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid), a new broad-spectrum fluoroquinolone, was compared with those of ciprofloxacin (CPFX), sparfloxacin (SPFX) and ofloxacin (OFLX). DWP20367 was showed antibacterial activity much higher than CPFX, SPFX and OFLK against gram-positive bacteria, while it was slightly more superior to quinolones against gram-negative bacteria. DWP20367 was particularly effective against MRSA, and its $MlC_{90}$ against clinical isolates of methicillin-susceptible S. aureus, low methicillin-resistant S. aureus and high methicillin-resistant S. aureus were 0.098, 0.781 and 1.563 micro g/ml, respectively. Against S. pneumoniae, MIC90 of DWP20367 was 2- to 8-fold higher than those of CPFX. With a view of MIC90, DWP20367 showed slightly more potent activity against P. aeruginosa and E. coli isolates than the control quinolones. DWP20367 activity was not affected by inoculum size and medium pH. But addition of $Mg^{2+}, \;Ca^{2+} $Mg2+, Ca2+ or horse serum (25%) decreased its antibacterial activity. DWP20367 was showed rapidly bactericidal activity within 2 to 4 h, and regrowth was not observed even after 24 h incubation at concentrations near the 4-fold of MIC.