• Bulletin of the Korean Chemical Society
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• 제10권1호
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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.

• 약학회지
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• 제42권1호
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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.

• 대한화학회지
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• 제42권2호
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• pp.214-219
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• 1998

Dynorphin B유도체들인 $[Arg^{11},\;D-Ala^{12}]$ dynorphin B, $[D-Ala^2,\;Ala^6,\;Arg^{11},\;D-Ala^{12}]$ dynorphin B 및 dynorphin B (1-11)를 고상법으로 합성하였다.에탄올 용액에서 2%의 디비닐벤젠으로 교차결합된 파라-염화메틸폴리스티렌 수지와 Thr을 반응시켜 수지 1g당 1.20 mmol의 Thr을 치환시켰다. 모든 아미노산의 아미노기는 t-Boc기로 보호하였으며 Tyr과Arg의 곁사슬은 2,6-디클로로벤질기와 니트로기로 각각 보호하였다. 각 유도체는 DCC와HOBT를 짝지음 시약으로 사용하여 단계적 합성법으로 합성하였으며 생성물은 MeOH/MeCN (3/1)을 전개용매로 하여 Sephadex LH-20 column (2${\times}$50 cm)으로 정제하였으며 HPLC와 아미노산 분석기로 확인하였다.