• Korean Journal of Weed Science
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• v.4 no.2
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• pp.169-178
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• 1984

This experiment was conducted to find out selective herbicides which are safe to the rice seedlings and to provide effective weed control method in protected semi-irrigated rice seedbed. There was no crop injury in rice with benzophenap [2-(4-2, 4-dichloro-3-methylbenzoyl)-1, 3-dimethyl-pyrazol-5-yl-oxy)-4'-methyl acetophenone] (240g), pyrazoxyfene [1,3-dimethyl-4-(2,4-dichlorobenzoyl)-Sphenacyloxy pyrazole] (200g), chlormethoxynil [2,4-dichlorophenyl-4-nitro-3-methoxyphenyl ether] (180g), dimepiperate [S-(1-methyl-1-phenethyl)-piperidine-l-carbathioate] (210g), dimepiperate + probenazol [3-allyloxy-1,2-benzisothiazol-1,1-dioxide] (210 + 120g) mixture and dimepiperate + probenazol + molinate [S-ethyl-N,N-hexamethylene-thiol-carbamate] (120 + 120 + 120g) mixture at times of application studied. Butachlor [2-chloro-2',6'-diethyl-N-buthoxymethyl acetanilide] + pyrazolate [4-(2,4-dichlorbenzoyl)-1,3dimethyl-pyrazol-5-yl-p-toluene-sulfonate] (70 + 120g) mixture and butachlor + chlormethoxynil (60 + 120g) mixture caused root length to shorten and root viability to decrease. However, the crop injury was recovered at 25 days after seeding. Benzophenap, pyraxoxyfene and butachlor + pyrazolate mixture were effective for weed control when applied at 2 days before seeding. Chlormethoxynil and butachlor + chlormethoxynil mixture was very effective for controlling annual weed. Dimepiperate, dimepiperate + probenazol mixture and dimepiperate + probenazol + molinate mixture did not control most weeds except for Echinochloa crus-galli (L.) Beauv.

• Journal of the Korean Chemical Society
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• v.56 no.2
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• pp.246-250
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• 2012

An efficient access, single step and environmentally benign synthesis of a new series of pyrazole containing isoxazolines derivatives were prepared by the condensation of chalcones bearing pyrazole moiety with hydroxyl amine hydrochloride in basic condition by using polyethylene glycol-400 (PEG) as a greener reaction solvent. The advantages of the present methodology are mild reaction condition and avoidance of volatile organic solvent. Furthermore, these newly synthesized compounds were screened for their antimicrobial activity against various pathogens like Escherichia coli (MTCC 2939), Salmonella typhi (MTCC 98), Staphylococcus aureus (MTCC 96), Bacillus subtilis (MTCC 441), Aspergillus niger (MTCC 281), Aspergillus flavus (MTCC 2501), Penicillium chrsogenum (MTCC 160) and Fusarium moniliformae (MTCC 156). Especially compound containing the hydroxyl group in C2-position and presence of halo (I, Br and Cl) groups as substituents at $C_3$ and $C_5$ position on the benzene nucleus showed the higher activity. Furthermore, compounds bearing methyl groups in combination with I and Br which enhanced the activity.

• Journal of the Korean Institute of Electrical and Electronic Material Engineers
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• v.19 no.9
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• pp.878-882
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• 2006

We have fabricated single organic layer devices of the organolanthanide complex, terbium tris-(1-phenyl-3-methyl-4-(tertiarybutyry)pyrazol-5-one)triphenylphosphine oxide [$(tb-PMP)_{3}Tb-(Ph_{3}PO)$] for the investigation of its light emission and electrical conduction properties. The thickness of ($(tb-PMP)_{3}Tb-(Ph_{3}PO)$) layer was varied to 60, 75, 95 nm. Mg and Ca layers were used for the cathode contact. The electrical conduction in the $(tb-PMP)_{3}Tb-(Ph_{3}PO)$ single layer devices was dominated by the injection of electrons into the organic layer from the cathode. A higher current density at much lower voltages can be attained with Ca cathode because of the enhanced electron injection. The device shows very sharp emission at 548 nm. The FWHM of the strongest emission peak was 12 nm.

• Bulletin of the Korean Chemical Society
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• v.35 no.10
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• pp.2922-2928
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• 2014

To investigate the possible isosteric replacement of imidazolidinone moiety in 4-phenyl-1-arylsulfonylimidazolidinones (2) for broad and potent anti-cancer agents, a series of 5-phenyl-1H-pyrazol-3-yl 1-(acyl)indoline-5-sulfonates (4) and 1-(1-(acyl)indolin-5-ylsulfonyl)-5-phenylpyrazolidin-3-ones (5) were prepared and evaluated for their cytotoxicity against six human cancer cell lines. Although the pyrazoles 4 or pyrazolidinones 5 showed relatively good activity, still they showed lesser activity in comparison to imidazolidinones 2. These activity decreases could be interpreted with the effect of change of the hydrogen bonding characteristics and the substitution pattern on structural variations of five membered rings from imidazolidinones 2 to pyrazoles 4 and pyrazolidinones 5, respectively. Therefore, it can be concluded that 4-phenyl-1-arylsulfonylimidazolidinone is a basic pharmacophore of imidazolidinones 2.

• Journal of the Korean Chemical Society
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• v.62 no.5
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• pp.352-357
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• 2018

Celecoxib (4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide) is a cyclooxygenase-2 inhibitor used in the treatment of arthritis, acute pain, and dysmenorrhoea. Celecoxib is a Biopharmaceutics Classification System (BCS) class II compound whose oral bioavailability is highly limited owing to its poor aqueous solubility. Several polymorphs of celecoxib have been identified as Form I, Form II, and Form III with melting points of about $162.8^{\circ}C$, $161.5^{\circ}C$, and $160.8^{\circ}C$, respectively. Form IV was generated from the precipitated suspension in the presence of HPMC (Hydroxypropyl methylcellulose) and Polysorbate 80. A rapid rate of dissolution is useful because the rate of dissolution of a drug typically increases its bioavailability. The aim of this study was to investigate the possibility of production of new crystal form of celecoxib that has higher solubility than Form III. New crystal form of celecoxib (Form A) has been isolated by recrystallization and characterized by differential scanning calorimetry (DSC), thermogravimetric (TG) analysis and powder X-ray diffractometry (PXRD). Form A was dissolved faster than Form III. At 30 minutes, the dissolution of Form A was 97.3%, whereas the dissolution of Form III was 82.2% (p < 0.1). After storage of three months at $20^{\circ}C$, in 24% RH (Relative Humidity), the crystal form was not transformed.

• Korean Journal of Weed Science
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• v.2 no.1
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• pp.31-40
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• 1982

For the effective control of weeds in mechanically transplanted paddy field weeding effects of naproanide ${\alpha}$-(${\beta}$-naphthoxy) propion anilide], pyrazolate [4-2, 4-dichlorobenzoyl)-1, 3-dimethyl pyrazol-5-yl-p-tolune sulphanate], chlormethoxynil (2, 4-dichloro-phenyl-4-nitro-3-methoxy phenyl ether), SL-49 [1-3dimethyl-4(2, 4dichlorobenzoyl)-5-phenacyloxy pyrazole], ACN (3-chloro-2-amino-l, 4-naphthoquinone) either alone or in combination with butachlor (2-chlor-2, 6-diethyl-N-buthoxymethyl acetanilide) were compared. Pyrazolate and SL-49 were most effective for the control of Sagittaria pygmaea MIQ. and Potomogeton distinctus A. BENN. including most annual weeds. Weeding effect of butachlor alone was very high for annuals, good for Cyperus serotinus ROTTB. and poor for S. pygmaea and P. distinctus. But the weeding effect of the combination of butachlor and pyrazolate was stronger than that of butachlor alone and therefore this mixture was effective for S. pygmaea, P. distinctus and C. serotinus including all the annual weeds. The combination of butachlor and SL-49 showed the same tendency as the combination of butachlor and pyrazolate. Naproanilide was not effective for the control of Echinochlor crusgalli P. BEAUV and less effective for Monochoria vaginalis PRESL, but excellent for S. pygmaea. By mixing butachlor with naproanilide weeding, spectrum for annuals and S. pygmaea was much increased by that for P. distinctus and C. serotinus was not satisfactory. ACN was not satisfactory for the control of all the tested weeds but the weeding effect was increased in general by mixing with butachlor. Chlormethoxynil was excellent for the control of annual weeds but it has no effect on C. serotinus, S. pygmaea and P. distinctus showing some initial controling effect but these weeds regrew afterwards. The weeding activity of ACN increased in combination with butachlor and the residual activity was stronger than that of ACN alone. A light crop injury was found at the initial period after treatments in all treated plots. The yield from all treated plots except those from plots treated with ACN, butachlor and naproanilide were not significantly different from the band weeded plot.

• The Korea Journal of Herbology
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• v.22 no.1
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• pp.53-61
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• 2007

Objectives: Our previous studies have clearly demonstrated that the scavenging activity of reactive oxygen species (ROS), protective effect of lipid peroxidation (LPO), and inhibition of cytochrome P450 isozymes (CYPs) from the Circium japonicum aqua-acupuncture solution (CJAS). But, Circium japonicum water extracted solution (CJWS) was weakly reported in cardiovascular diseases such as oxidative stress-mediated atherosclerosis or its value evaluated. Methods: CJWS was assessed to determine the mechanism of its scavenging activity of ROS and inhibitory effect of CYP 2E1. Results: CJWS exhibited a concentration-dependent scavenger of DPPH and superoxide anions radicals using different assay systems. In addition, CJWS showed dose-dependent free radical scavenging activity, including hydroxyl radicals, peroxynitrite, and nitric oxide. The CJWS was also found to be effective in protecting rat liver homogenate against LPO. Futhermore, the CJWS showed significant inhibition of CYP 2E1 induced by pyrazol in a rat liver microsome. Conclusion : ROS and CYPs may play a role in several diseases, such as cardiovascular disease and heart failure. Our study demonstrated that the CJWS has excellent scavenging activity of ROS. Hence, it is worthwhile to investigate the potential effectiveness of CJWS in preventing oxidative stress-mediated cardiovascular diseases.

• Korean Journal of Weed Science
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• v.10 no.4
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• pp.255-260
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• 1990

Seventeen different herbicides were screened to select promising ones for the control of weeds, which may be used in paddy fields transplanted with 8 days old young rice seedlings. Four classes of herbicides were chosen and tested with seedlings grown under different cultivating conditions. Contact herbicides such as diphenyl-ether and oxadiazol showed severe growth retardation of rice seedlings. Carbamate class(dimepiperate), quinoline class (quinclorac), pyrazol class(pyrazolate), acid amide class(mefenacet and pretilachlor), addition of safener (pretilachlor+fenclorim and mefenacet+bensulfuron+dymuron) and unknown class (KC-7079) exhibited normal growth of seedlings. Sulfonyl urea herbicide class(cimosulfuron, bensulfuron, pyrazosulfuron), and oxarane class(tridiphane) showed the slight growth inhibition but recovered shortly.

• Korean Journal of Weed Science
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• v.14 no.2
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• pp.112-119
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• 1994

The experiment was conducted to investigate the cause of the continous increase of Sagittaria trifolia dominance and it's effective control methods in the paddy rice fields. Early physilogical response of S. trifolia caused by sulfonylurea three herbicides resulted in growth cessation. However, the growth-ceased plant regrew after the certain period of time. Pyrazolate{4-[2, 4-dichloro benzoyl]-1, 3-dimethylpyrazol-5-yl-ptoluene sulphonate} could control S. trifolia until 6-7 leaf stages. The herbicidal activity of S. trifolia by pyrazolate was not related to the size of tuber and the amount of carbohydrate consumption in the tuber. The production of S. trifolia tubers inhibited more than 95% by the systematic treatment of pyrazosulfuron-ethyl{Ethyl-5-(4, 6-dimethoxy pyrimidin-2-yl carbomoyl sulfamoyl)-2-chloro-2', 6'-diethyl acetanilide}, cinosulfuron and pyrazolate after the first treatment of pyrazosulfuron-ethyl and pyrazolate.

• Biomolecules & Therapeutics
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• v.30 no.6
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• pp.520-528
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• 2022

Mast cells are an effector cell that plays a pivotal role in type I hypersensitive immune responses. Mast cells exist in connective tissues, such as skin and mucosal tissue, and contain granules which contain bioactive substances such as histamine and heparin in cells. The granules of mast cells are secreted by antigen stimulation to cause the type I allergic hypersensitivity. In addition, stimulated by antigen, mast cells synthesize and secrete various eicosanoids and cytokines. While AT9283 is known to have anticancer effects, the therapeutic effect of AT9283 on allergic disorders is completely unknown. In this study, it was found that AT9283 reversibly inhibited antigen-IgE binding-induced degranulation in mast cells (IC₅₀, approx. 0.58 μM) and suppressed the secretion of the inflammatory cytokines IL-4 (IC₅₀, approx. 0.09 μM) and TNF-α (IC₅₀, approx. 0.19 μM). For a mechanism of mast cell inhibition, while not inhibiting Syk phosphorylation, AT9283 suppressed the activation of LAT, a downstream substrate protein of Syk, in a dose-dependent manner. As expected, AT9283 also inhibited the activation of PLCγ1 and Akt, downstream signaling molecules of Syk/LAT, and MAP kinases such as JNK, Erk1/2, and P38. In an in vitro protein tyrosine kinase assay, AT9283 directly inhibited Syk activity. Next, AT9283 dose-dependently inhibited passive cutaneous anaphylaxis (PCA), an IgE-mediated allergic acute response, in mice (ED50, approx. 34 mg/kg, p.o.). These findings suggest that AT9283 has potential to use as a new drug for alleviating the symptoms of IgE-mediated allergic disorders.