• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.154.2-155
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• 2003

Recently, we developed a new anti-osteoporotic agent, DW-1350, which not only inhibited osteoclast formation but also induced osteoblast differentiation through the in vitro randomized screening studies. We identified inhibitory activities of DW-1350 for each step of osteoclast differentiation, fusion and pit formation process in co-culture system with mouse bone marrow and primary osteoblasts. (omitted)

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.155.1-155.1
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• 2003

In the present study, the effect of DW-1350, a newly synthesized anti-osteoporotic agent, was evaluated in ovariectomized Rat. Female SD Rat mice underwent bilateral ovariectomy for prevention study that test article was administered from 2 days after ovariectomy for 6 weeks, for therapeutic study it was conducted from 6 weeks after ovariectomy for three months. (omitted)

• Biomolecules & Therapeutics
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• 제6권4호
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• pp.395-399
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• 1998

DW2282, (S)- (+)-4-phenyl -1-[N-(4-am mob enzoyl) -indolin-5- sulfonyl]-4,5- dihydro-2-imidazolone hydrochloride, is a novel anticancer agent thought to have an unique mechanism of action on the inhibition of tumor growth. In this study, we estimated in vivo antitumor activities and pharmacokinetics of Dw2282 depending on various vehicles. The inhibition rate of tumor growth was increased by 50, 100 and 200 mg/kg of Dw2282 in a dose-dependent manner. When Dw2282 dissolved in 4 sorts of vehicles was orally single dosed to rats at 50 mg/kg, Cmax of Dw2282 in 0.5% CMC.Na was a half as high as those in PG, PG+CP and PG+CP+DW. When Dw2282 was orally administered to mice for 5 days, antitumor activity of 130 mg/kg suspended in 0.5% CMC.Na was as effective as that of 65 mg/kg dissolved in the rest of vehicles. Taken together, it is thought that antitumor activities of Dw2282 are resulted from the absorption extent of it and related to the vehicle used.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1997년도 춘계학술대회
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• pp.73-73
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• 1997

A series of 4-phenyl-1-(indoline-5-sulfonyl)-2-imidazolone derivatives has been synthesized starting from 2-bromoacetophenone. Reaction of 2-aminoacetophenone obtained from 2-bromoacetophenon by Delepin synthesis and potassium cyanate affords 1,3-dihydro-4-phenyl-2-imidazolone. This key intermediate was treated with sodium hydride and N-trifluoroacetyl-indoline-5-sulfonylchloride, and trifluoroacetyl group was deprotected to give 4-Phenyl-1-(indoline-5-sulfonyl)-2-imidazolone. Various substituents were introduced on the nitrogen of indoline. Antitumor activity of this series of compound was evaluated by MTT method. Nearly all of the compounds showed broad-spectrum activity.

• Archives of Pharmacal Research
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• 제27권5호
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• pp.478-484
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• 2004

The novel 1-(1-benzoylindoline-5-sulfonyl)-4-phenyl-4,5-dihydroimidazolones 2 shows highly potent and broad cytotoxicities. Their cytotoxicities against human lung carcinoma A549, human chronic myelogenous leukemia K562, and human ovarian adenocarcinoma SK-OV-3 are compatible with doxorubicin. Compound 2p (1-[(4-aminobenzoyl)indoline-5-sulfonyl])-4-phenyl-4,5-dihydroimidazolone) exhibits a cytotoxicity that is far more potent than doxorubicin and also exhibits highly effective antitumour activities against murine (3LL, Colon 26) and human xenograft (NCI-H23, SW620) tumor models.

• Biomolecules & Therapeutics
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• 제5권2호
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• pp.187-193
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• 1997

The in vivo and in vivo antibacterial activity of DW-116, a newly synthesized fluoroquinolone, were compared with those of other quinolones. DW-116 exhibited more potent antibacterial activity than rufloxacin and lower activity than ofloxacin and ciprofloxacin in in vivo assay But, DW-116 particularly showed strong activity against the family of staphylococci including methicillin-sensitive staphylococcus and its activity was more active than that of ciprofloxacin. The time-kill curve studies showed rapid bactericidal activity for DW-116. The post-antibiotic effect of DW-116 was observed between 0.66 and 5 hours. The therapeutic efficacy of DW-116 against respiratory infection with P. aeruginosa was as strong as that of ciprofloxacin and its effect against urinary tract in(traction with E. coli was more effective than rufloxacin. The excellent therapeutic efficacy of DW-116 against these local infections is due to its good pharmacokinetic profiles.

• Biomolecules & Therapeutics
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• 제4권3호
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• pp.239-243
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• 1996

DW-116 {(1-(5-fluoro-2-pyridyl)-6-fluoro-7-(4-methyl-1-piperazinyl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid hydrochloride) is a new quinolone antibiotic with a broad antibacterial spectrum against G(+) and G(-) bacteria. DW-116 was evaluated for the appearance of micronucleus in polychromatic erythrocytes (PCEs) of mouse bone marrow cells after intraperitoneal and oral single administration. We prepared the bone marrow cells at 30hr after drug administration and they were used for measuring PCE with micronucleus. The results showed there was no statistically significant increase in the numbers of PCEs with micronucleus in all DW-116 administered groups compared with a negative control group. The results also showed that the ratio of normochromatic erythrocytes(NCEs) to PCEs of all DW-116 administered groups was not significantly different from that of a negative control group. These results suggested that DW-116 may not cause any chromosomal damage and it has no in vivo mutagenic potential under these experimental conditions.

• Archives of Pharmacal Research
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• 제21권5호
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• pp.610-614
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• 1998

DW-116, [1-(5-fluoro-2-pyridyl)-6-fluoro-7-(4-methyl-1-piperazinyl)-1,4-dihydro-4-oxoquino-line-3-carboxylic acid hydrochloride}, is a new quinolone antibiotic with a broad antibacterial spectrum against G(+) and G(-) bacteria. DW-116 was evaluated for the immunomodulating activities, which is one of the efforts to investigate the mechanism of action related to the good in vivo antibacterial efficacy. The results of in vitro studies revealed there was no statistically significant increase in B and T lymphocyte proliferation. But the results of in vivo studies showed that the number of plaque forming cells (PFC), the amount of polyclonal antibodies and delayed-type hypersensitivity (DTH) were significantly increased after the repeat administration with 12 and 60 mg/kg of DW-116. Taken together, these results proposed that immunostimulting effect of DW-116 could be one of the action mechanisms for demonstrating in vivo antibacterial activities under these experimental conditions.

• Journal of Pharmaceutical Investigation
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• 제27권2호
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• pp.133-137
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• 1997

Buccal absorption test of omeprazole in human was performed to determine the permeability of the drug molecule through oral mucous membrane. Oral mucosal adhesive tablets of omeprazole were prepared by compressing the omeprazole with a mixture of sodium alginate and hydroxypropylmethyl cellulose (HPMC) as bioadhesive polymers, magnesium oxide (MgO) as a stabilizer and sodium carboxymethyl cellulose (Na CMC) or cros-carmellose sodium (Ac-Di-Sol) as disintegrants. The bioadhesive force, stability in saliva and release characteristics of the tablets were evaluated. Omeprazole was absorbed about 23% in 15 min through human buccal mucous membrane. Furthermore, omeprazole was stable in saliva for more than 8 hrs when MgO was added to the tablet as the amount of 2.5 fold of omeprazole. The release rate of omeprazole was increased with increasing the amount of sodium alginate in the tablet. From these results, it is suggested that tablets composed of [omeprazole/HPMC/sodium alginate/MgO/Ac-Di-Sol and/or Na CMC (20/6/24/50/10) (mg/tablet)] are potential candidate for buccal drug delivery system.

• Biomolecules & Therapeutics
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• 제10권4호
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• pp.236-239
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• 2002

The goal of this study was to evaluate the antidiarrheal efficacy of $Lacteol^{TM}$-loperamide combination against the mouse model of secretory diarrhea. Secretory dirrhea was induced in mice by p.o. administration of castor oil (0.3 ml). Antidirrheal effects of $Lacteol^{TM}$-loperamide combination were compared with each individual component. $Lacteol^{TM}$-loperamide combination was the most potent among these agents, eliminating diarrhea in 100% of mice at a dose 1360/4 mg/kg (Lacteol/loperamide, respectively). In this study, we also measured changes of bodyweight as another indicator of the dirrhea, based on the assumption that lower bodyweight loss represented reduced fecal passage. The bodyweight loss of $Lacteol^{TM}$-loperamide combination administered group was 4 times lower than that of vehicle control. These findings indicate that $Lacteol^{TM}$-loperamide combination may be more potent than individual component in its antidiarrheal action, so we are going to challenge this combination for further study and clinical evaluation.