• Archives of Pharmacal Research
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• v.28 no.5
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• pp.509-517
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• 2005

A series of structurally diverse amide derivatives of [6-(3,5-dimethyl-4- chloro-pyrazole-1-yl)-3(2H)-pyridazinone-2-yl]acetic acid were prepared and tested for their in vivo analgesic and anti-inflammatory activity by using p-benzoquinone-induced writhing test and carrageenan induced hind paw edema model, respectively. The analgesic and anti-inflammatory activity of the compounds, 7c, 7d and 7k were found to be equipotent to aspirin (as an analygesic) and indometacin (as an anti-inflammatory drug), respectively. The other amide derivatives generally resulted in lower activity on comparision with reference compounds.

• Bulletin of the Korean Chemical Society
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• v.34 no.8
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• pp.2480-2486
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• 2013

A new series of diarylamides and diarylureas having 2,3-dihydropyrrolo[3,2-b]quinoline scaffold was synthesized. Their in vitro antiproliferative activities were tested over NCI-60 cancer cell lines of nine different cancer types. Some target compounds showed good inhibition percentages over different cell lines. Among all the target compounds, compound 1f possessing 6,7-dimethoxy-2,3-dihydropyrrolo[3,2-b]quinoline nucleus, amide linker, and 4-chloro-3-(trifluoromethyl)phenyl terminal ring showed high selectivity against MCF7 and MDA-MB-468 breast cancer cell lines more than the other tested cell lines. Its inhibition percentages at $10{\mu}M$ concentration over those two cell lines were 84.97% and 87.13%, respectively.

• Bulletin of the Korean Chemical Society
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• v.28 no.10
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• pp.1641-1642
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• 2007

• Archives of Pharmacal Research
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• v.14 no.1
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• pp.48-51
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• 1991

Amides from amino acid ester and nalidixic acid were synthesized. The solubility characteristics and partition coefficient of the compounds were studied. The hydrolysis of the compounds was studied in the simulated gastric fluid and simulated intestinal fluid. Some compounds showed better antibacterial activity than nalidixic acid.

• Journal of the Korean Applied Science and Technology
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• v.35 no.1
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• pp.173-185
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• 2018

Effects of three different types of dispersions and flow improving additives composed with fatty acid esters, fatty acid metal salts and amide compound on the vulcanization and the mechanical properties properties of rubber compounds of EPDM and carbon black as fillers. were investigated using Mooney viscometer, moving die rheometer, hardness tester, and universal test machine. The aging characteristics of vulcanized EPDM compounds were also investigated. The Mooney viscosity measured at $125^{\circ}C$ showed a tendency to decrease in the order of amide type> metal salt type > ester type additive. Scorch time showed little or no difference with the addition of ester or metal salt type additives, but the amide type additive shortened a scorch time more than one minute. Rheological measurement data obtained at $160^{\circ}C$ showed that the vulcanization time was faster for metal salt type and amide type additive systems. Delta torque values of EPDM compound increased with metal salt type and amide type additives, but slightly decreased with ester type additive. The tensile strength of the EPDM compound was greatly improved when an ester type additive was added, but the amide type or metal salt type additive had no significant effect. The elongation was significantly improved for metal salt type additive, while the rest were not significantly affected. The tear strength of the EPDM compounds increased with the addition of all kinds of additives, and it increased remarkably in the case of metal salt type additive. Hardness of the EPDM compounds was nearly same value regardless of additive types. The thermal aging of the EPDM blend at $100^{\circ}C$ for 24 h showed little change in the case of metal salt type or amide type additive, but the elongation tends to decrease by 10-20% for all EPDM compounds containing additives.

• Bulletin of the Korean Chemical Society
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• v.27 no.9
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• pp.1353-1358
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• 2006

We investigated in vitro T-cell inhibitory activity and bioavailability of small chemical inhibitors for Lck SH2 domain, which had a different scaffold such as an amide bond, reduced amide bond, N-methyl amide bond, thioamide bond, and urethane bond. Each of these compounds, with its particular scaffold, showed a different logP value, stability against serum enzyme, stability in buffer solution, and in vitro T-cell inhibitory activity. Overall results indicated that the SH2 inhibitor containing urethane bond can be a new lead compound because of its superior bioavailability, potent in vitro T-cell inhibitory activity, and facile synthesis.

• Bulletin of the Korean Chemical Society
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• v.32 no.3
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• pp.1022-1026
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• 2011

The syntheses of DTPA-bis(amide) conjugates of phosphonated cyclohexane moieties (5a-d) and their Gd(III) complexes of the type $[Gd(L)(H_2O)]{\cdot}nH_2O$ (6a-d; L = 5a-d) are described. All new compounds have been characterized by microanalysis and spectroscopic techniques. High $r_1$ relaxivities of aqueous solutions of 6a-d are observed to be in the range of $10.7-18.3\;mM^{-1}sec^{-1}$, which compare much better than that of $Omniscan^{(R)}$ ($r_1=3.90\;mM^{-1}sec^{-1}$).

• Korean Membrane Journal
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• v.3 no.1
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• pp.9-16
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• 2001

The diamide-diamine having carboxylic acid was prepared by direct condensation of 1,2,4-benzenetricarboxylic acid with bits[4- (3-aminophenoxy ) phenyl] sulfone and bits(4-aminouhenyl)-1,4- diisopropylbenzene in medium consisting of triphenylphosphite, LiCl, and N-methyl-2-pyrrolidone. Copoly (amide-imide) derivatives with high molecular weight could be synthesized by one-step polycondensation of prepared diamide-diamine having carboxylic acid and various dianhydride compounds. Depending on the chemical structure and composition of polymer backbones, the viscosities of polymers were found to range between 0.87∼ 1.57 dL/B. All the polymers showed good thermal stability up to 320$\^{C}$ and the 10% weight loss temperature was observed in the range of 450∼540$\^{C}$ in a thermogravimetric traces. The glass transition was recorded in the temperature range of 200 ∼ 270$\^{C}$. All the polymers showed an amorphous nature on a differential scanning calorimetric thermograms. These polymers generally had good mechanical properties and readily soluble in various polar solvents. Further, it was proved that their properties could be determined from the composition.

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.186.1-186.1
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• 2003

Bradykinin is an autocoid related to acute and chronic pain and inflammation. The non-peptide bradykinin antagonists are of interest as novel anti-inflammatory therapeutics. Some active compounds such as FR 173657, LF 160687, and bradyzide were reported very recently. In our search for the new bradykinin antagonists, we designed and synthesized the iminodiacetic acid derivatives having two or three amide bonds and lipophilic ring system in each molecule. Liquid phase combinatorial synthesis using the iminodiacetic acid template gave diverse individual compounds rapidly and efficiently on a 10-50 mg scale. (omitted)

• Bulletin of the Korean Chemical Society
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• v.32 no.7
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• pp.2497-2500
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• 2011