• 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)

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.211.1-211.1
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• 2003

On the purpose of develcpement of antioxidative compound from natural sources, medicinal plants known to have antioxidant actuvity have been examined concening DPPH radical scavenging activity and SOD-liked activities. Among 8 plants exhibiting the activity, Houttuynia cordata THUNB was selected as resources to search for active compounds due to rareness of study. The antioxidative compounds from Houttuynia cordata THUNB,quercitrin was assayed using a DPPH free radical. The DPPH radical scavenging activity of quercitrin was similar to that of BHA and Ascorbic acid

• Archives of Pharmacal Research
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• v.17 no.5
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• pp.298-303
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• 1994

4-Arylazo-1H-pyrazol-3, 5-idimines 1a-c reacted with bromomalononitrile (2) to yield the corresponding imidazo[1, 2-b]pyrazoles 3a-c. The latter reacted with some active methylene compounds and with .alpha.-cinnamonitriles to afford the corresponding pyrazoloimidazopyridines 6, 8, 9 and 15, respectively. Compounds 3 reacted with each of formic acid, formamide, trichlo-roacetonitrile and with guanidine to yield the corresponding pyrazoloimidazopyrimidines 16-19 respectively.

• YAKHAK HOEJI
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• v.15 no.3_4
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• pp.87-92
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• 1971

Fourteen novel N,N'-disubstitued thiourea derivatives were synthesized by Hugershof reaction. Antitubercular activities of ten compounds against Mycobacterium tuberculosis H$_{37}$ Rv were tested and was found tat 1-cyclohexyl-3-(4-benzenesulfonepiperidide)-2-thiourea was considerably active at 1mg/ml and 1-$\alpha$-naphthyl-3-(4-benzenesulfonepiperidide)-2-thiourea was slightly active at 1mg/ml. Antibacterial activity of the newly synthesized compounds against E. coli, Sta. aureus and Streptococcus hemolyticus were also tested. 1-cyclohexyl-3-(4-benzenesulfonepiperidide)-2-thiourea was makedly active against E. coli, Sta, aureus and Streptococcus hemolyticus; Phenol coefficients against E. coli, Sta, aureus and Streptococcus hemolyticus were 30,17.5 and 21.3, respectively. 1,1'-p-phenylene-3,3'bis[N-(2-thiazolyl)-sulfamylphenyl]-2,2'-dithiourea and 1-$\alpha$-naphthyl-3-(4-benzenesulfonepiperidide)-2-thiourea were considerably active against E. coli: phenol coefficients, 18.8 and 37.5 respectively. 1-(4-ethoxyphenyl)3-(4-sulfamylphenyl)-2-thiourea was active against Streptococcus hemolyticus: phenol coefficients, 22.5. 1-$\alpha$-naphthyl-3-(4-sulfamylphenyl)-2-thiourea, 1-$\betha$-naphthyl-3-[4-N-(2-thiazolyl)-sulfamylphenyl]-2-thiourea and 1-$\alpha$-naphthyl-3-(4-benzenesulfonepiperidide)-2-thiourea were active against Sta. aureus: phenol coefficients, 17.5, 20.0 and 18.8 respectively.

• Archives of Pharmacal Research
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• v.26 no.3
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• pp.197-201
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• 2003

Novel $\beta$-hydroxy propenamides as analogues of the active metabolite of leflunomide (A 771726) were synthesized and evaluated for their inhibitory activity on dihydroorotate dehydrogenase (DHODH) in an investigation into their immunosuppressive activity. Compounds 2a, 3a, and 3h were approximately 4-40 times more potent than leflunomide in their activity while they were-less active than A 771726.

• Bulletin of the Korean Chemical Society
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• v.32 no.2
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• pp.576-582
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• 2011

Various 2-amino-6-[3-(substituted phenyl)-5-phenyl-4,5-dihydropyrazol-1-yl]-4-(substituted phenyl)nicotinonitriles (3a-t) were designed and synthesized by clubbing two active anticonvulsant pharmacophores pyrazole and pyridine. All the synthesized compounds possessed the pharmacophoric elements essential for good anticonvulsant activity. The anticonvulsant screening was performed by maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) tests. Two compounds 3i and 3s showed significant anticonvulsant activity in both the screens with $ED_{50}$ values 17.5 mg/kg and 22.6 mg/kg respectively in MES screen and 154.1 mg/kg and 242.6 mg/kg respectively in scPTZ screen. They were also found to have no acute toxic effects in mice when tested at elevated doses.

• Journal of Microbiology and Biotechnology
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• v.30 no.1
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• pp.146-154
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• 2020

With the advantages of biocatalytic method, enzymes have been excavated for the synthesis of chiral amino acids by the reductive amination of ketones, offering a promising way of producing pharmaceutical intermediates. In this work, a robust phenylalanine dehydrogenase (PheDH) with wide substrate spectrum and high catalytic efficiency was constructed through rational design and active-site-targeted, site-specific mutagenesis by using the parent enzyme from Bacillus halodurans. Active sites with bonding substrate and amino acid residues surrounding the substrate binding pocket, 49L-50G-51G, 74M,77K, 122G-123T-124D-125M, 275N, 305L and 308V of the PheDH, were identified. Noticeably, the new mutant PheDH (E113D-N276L) showed approximately 6.06-fold increment of k_cat/Km in the oxidative deamination and more than 1.58-fold in the reductive amination compared to that of the wide type. Meanwhile, the PheDHs exhibit high capacity of accepting benzylic and aliphatic ketone substrates. The broad specificity, high catalytic efficiency and selectivity, along with excellent thermal stability, render these broad-spectrum enzymes ideal targets for further development with potential diagnostic reagent and pharmaceutical compounds applications.

• Natural Product Sciences
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• v.24 no.2
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• pp.88-92
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• 2018

The present study was undertaken to investigate the isolated compounds from the stem bark of Garcinia atroviridis as potential cholinesterase inhibitors and the ligand-enzyme interactions of selected bioactive compounds in silico. The in vitro cholinesterase results showed that quercetin (3) was the most active AChE inhibitor ($12.65{\pm}1.57{\mu}g/ml$) while garcinexanthone G (6) was the most active BChE inhibitor ($18.86{\pm}2.41{\mu}g/ml$). It is noteworthy to note that compound 6 was a selective inhibitor with the selectivity index of 11.82. Molecular insight from docking interaction further substantiate that orientation of compound 6 in the catalytic site which enhanced its binding affinity as compared to other xanthones. The nature of protein-ligand interactions of compound 6 is mainly hydrogen bonding, and the hydroxyl group of compound 6 at C-10 is vital in BChE inhibition activity. Therefore, compound 6 is a notable lead for further drug design and development of BChE selective inhibitor.

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.256.3-257
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• 2003

The bioactivity-guided fractionation of an active methylene chloride extract of the sclerotium of Poria cocos led to the isolation of compounds 1-5. These compounds were tested in the human colon carcinoma and human breast carcinoma cell lines, compounds 3, 4, and 5 exhibited IC50 values of 10.8, 15.4, and 5.1 $\mu\textrm{g}$/$m\ell$ against human colon carcinoma cell line. In addition, compounds 3, 4 and 5 showed moderate activities as inhibitors of Topoisomerase I and all compounds were inactive in the Topoisomerase II inhibition.

• Journal of Korean Society of Water and Wastewater
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• v.28 no.2
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• pp.235-248
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• 2014

The widespread occurrence of dissolved endocrine disrupting compounds(EDCs) and pharmaceutical active compounds(PhACs) in water sources is of concern due to their adverse effects. To remove these chemicals, adsorption of EDCs/PhACs on granular activated carbon(GAC) was investigated, and bisphenol A, carbamazepine, diclofenac, ibuprofen, and sulfamethoxazole were selected as commonly occurring EDCs/PhACs in the aquatic environment. Various adsorption isotherms were applied to evaluate compatability with each adsorption in the condition of single-solute. Removal difference between individual and competitive adsorption were investigated from the physicochemical properties of each adsorbate. Hydrophobicity interaction was the main adsorption mechanism in the single-solute adsorption with order of maximum adsorption capacity as bisphenol A > carbamazepine > sulfamethoxazole > diclofenac > ibuprofen, while both hydrophobicity and molecular size play significant roles in competitive adsorption. Adsorption kinetic was also controled by hydrophobicity of each adsorbate resulting in higher hydrophobicity allowed faster adsorption on available adsorption site on GAC. EDCs/PhACs adsorption on GAC was determined as an endothermic reaction resulting in better adsorption at higher temperature ($40^{\circ}C$) than lower temperature ($10^{\circ}C$).