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김순옥(Soon Ok Kim),홍사미(Sa Mi Hong),이선화(Seon Hwa Lee) 대한약학회 1992 약학회지 Vol.36 No.5
For the synthesis of tuberin derivatives, N-(disubstituted styryl) carboxamides, the series of cinnamic acids were transformed through chlorides, azides to isocyanates. And then isocyanates were reduced separately by Dibal and Grignard reagent. As a result of antimicrobial susceptibility test, N-(3,4-dichlorostyryl) formamide and N-(3,4-dichlorostyrl) acetamide showed comparatively large activity against some bacteria that is, MIC was respectively 50 ppm, 6.25~50 ppm. MIC of other derivatives was similiar to that of tuberin, about 100.
Β-thiocyanatobenzylidene malonic acid ester 유도체의 합성에 관한 연구
김순옥,홍사미,고정희 성신여자대학교 기초과학연구소 1992 基礎科學硏究誌 Vol.9 No.-
The derivatives of β-thiocyanatobenzylidene malonic acid ester were synthesized by the nucleophillic vinyllic substitution of thiocyanate, were obtained in 30-65% yield. The reactivity and yield were related to the structures of benzylidene malonic acid ester derivatives and the effect of the substituent of the para-substituted benzaldehydes were decresed the order of -NO2> -H, -CI> -OMe and also the reactivity of the malonic acid derivatives were reduced in order of diesters>cyanoacetyl ester>dinitrile. The separation and purification of β-thiocyanatobenzylidene malonic acid esters were carried out by column chromatography and recrystallization. The structure of synthetic compounds were identified by the NMR and IR spectroscopy.
THE SYNTHESIS OF TUBERIN DERIVATIVES
Kim, Soon Ok,Hong, Sa Mi,Park, Jae Kyoung 성신여자대학교 기초과학연구소 1995 基礎科學硏究誌 Vol.13 No.-
결핵균에 대하여 호라성이 있는 새로운 항생물질인 투베린 유도체의 합성을 목적으로, 여러종류의 치환된 신남산을 시작 물질로 그들의 염화물, 아지드 및 이소시아네이트로의 합성단계를 거쳐서 안정한 이소시아네이트 삼합체를 합성하였다. 각 단계 중간물질의 최적 합성조건을 확립하여 적용하고 분리정제 및 구조확인도 실시하였다. 합성한 일련의 N-치환 스티릴 포름아미드의 항균 활성도를 실험한 결과 2, 4-디클로로 스티릴 포름아미드는 S. Aureus 701E와 703E 및 M.Phlei에 대해서는 투베린에 비해서 두배의 활성도가 있었으며 다른 유도체는 항균성이 투베린과 비슷하거나 약하였다. The synthesis of Tuberin detivatives, a natural antibiotic known to be tuberculostatic, were attempted to improve its efficacy. Compounds synthesised were tested for antibacterial activities against Staphylococcus aureus 701E and 703E and My cobacterium phlei. N-(2, 4-dichlorostyryl) formamide showed twice as active as Tuberin itself in vitro.