• Bulletin of the Korean Chemical Society
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• v.10 no.1
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• pp.19-22
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• 1989

The suitability of BMPI (2-bromo-N-methyl pyridinium iodide) for solid-phase peptide synthesis was investigated. The coupling rate of BMPI/HOBT procedure. BMPI/HOBT was superior to DCC/HOBT couplings using the solid-phase peptide bond formation proceeded to a greater degree of completion than DCC/HOBT method did. Double couplings with 2 equiv. of Bocamino acids and 1.5 equiv. of BMPI and $NEt_3$ and 2 equiv. of HOBT in DMF/MC (1:1 v/v) gave the best result for the preparation of a model compound. Stepwise solid phase peptide synthesis using BMPI/HOBT procedure was successfully utilized for the preparation of $(D-Ala)^2$-dynorphine A. BMPI/HOBT procedure for the synthesis of $(D-Ala)^2$-dynorphine gave better yield (20%) than DCC/HOBT procedure did.

• YAKHAK HOEJI
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• v.42 no.1
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• pp.12-24
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• 1998

For the development of new cephalosporin antibiotics with aminothiazolcarboxymethylethoxyimino moiety on the C-7 position and tetrazolymethyl moiety on the C-3 position of cephe m ring, 7${\beta}$-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxyimino)acetamido]-3-[5-(substituted)tetrazol-2-yl]methyl-3-cephem-4-carboxylic acids(28-35) were synthesized. These compounds were tested for antimicrobial activity in vitro against Gram(+) and Gram(-) bacteria. They showed remarkable antibacterial activity against Escherichia coli AB 1157, Escherichia coli AB 0111, Escherichia coli BE 1186, Micrococcus luteus ATCC 9341, Salmonella typhimurium TV 119, Salmonella typhimurium SL 1102, Staphylococcus aureus IFO 12732, Staphylococcus aureus R-209, but these compounds were not active against Pseudomonas aeruginosa N-10.

• Journal of the Korean Chemical Society
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• v.42 no.2
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• pp.214-219
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• 1998

Dynorphin B analogues, $[Arg^{11}, D-Ala^{12}]$dynorphin B, $[D-Ala^2, Ala^6, Arg^{11}, D-Ala^{12}]$dynorphin B, and dynorphin B (1-11) were synthesized by solid-phase method. A chloromethylated polystyrene resin cross-linked with 2% divinylbenzene was substituted with Thr in ethanol to contain 1.20 mmol Thr/g of resin. All amino groups of amino acids were protected with t-Boc group and 2,6-dichlorobenzyl and nitro groups were used to protect the side chains of Tyr and Arg, respectively. Stepwise synthetic method was applied for synthesis of the products. Dicyclohexylcarbodiimide (DCC) and 1-hydroxybenzotriazole (HOBT) were used as the coupling reagents. The crude peptides were purified by gel filteration on Sephadex LH-20 column $(2 \times 50 cm)$ using MeOH/MeCN (3/1) and then characterized with HPLC, amino acid analyzer.