• 제목/요약/키워드: lactonization

검색결과 14건 처리시간 0.021초

새로운 사이클로프로필 뉴크레오사이드 유도체의 합성과 생리활성 (Synthesis of Novel Cyclopropyl Nucleoside Derivatives as Potential Antiherpetic Agent)

  • 강진아;천부순;문형룡
    • 약학회지
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    • 제56권4호
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    • pp.230-235
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    • 2012
  • Synthesis of novel cyclopropyl pyrimidine and purine nucleoside derivatives 2~8 with ${\alpha}$-configuration was successfully accomplished using an epoxide-ring opening reaction, lactonization, a hydroboration-oxidation reaction and a Mitsunobu reaction as the key steps. Antiviral activities against HSV-1 and -2, HIV-1 and -2, coxsackie B1and B3 viruses and poliovirus were assayed. Three compounds 4, 7 and 8 exhibit cytotoxicity-derived antiviral activity only in HIV-1 and -2.

항암작용 가능성이 있는 10-Membered Enediyne의 선구물질인 14-Membered Phenylthio Enediyne Lactone의 합성 (Synthesis of 14-Membered Phenylthio Enediyne Lactone : A Precursor of the Potential Enediyne Antitumor Antibiotics)

  • 김기동
    • 대한화학회지
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    • 제39권2호
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    • pp.103-110
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    • 1995
  • 본 연구에서는 항암제로서의 가능성이 있는 10-membered enediyne(6)의 선구물질로 사용될 수 있는 14-membered phenylthio enediyne lactone을 성공적으로 합성할 수 있었다. 14-membered lactone은 Ireland-Clasisen rearrangement에 의해 10-membered enediyne(11)으로 변환되며 이물질(11)은 최종물질(8)로 전환될 수 있을 것으로 예상된다. 이 14-membered enediyned lactone(23)은 DCC/PTSA/Pyridine 하에 enediyne hydroxyl acid(22)의 락톤화 반응에 의해 합성되었다. Enediyne hydroxyl acid는 Pd(0) 촉매하에 methyl pentynoate(19)와 enyne alcohol(17)을 cis-1,2-dichloroethylene과 연속적으로 coupling 반응을 하여 좋은 수득율로 얻을 수 있었다. 그 때 필요한 enyne alcohol(17)은 vinyltin(12)을 출발물질로 하여 성공적으로 얻을 수 있었다.

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불소 이온 감지용 형광 센서의 개발 (Development of Highly Selective Fluorescent Chemosensors for Fluoride Ion)

  • 김태현;김인자;유민지
    • 대한화학회지
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    • 제51권3호
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    • pp.258-264
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    • 2007
  • 새로운 불소 이온 감지용 화학 센서를 합성하였다. 탈실리콘화 과정에서 만들어지는 페녹사이드를 친핵체로 사용하여 형광 물질로 락톤화되는 기존의 방법에 대한 추가적인 설명과 함께 탈실리콘화에 의한 방향족 화합물의 평면 화를 통한 형광의 변화 방법이 새로이 제시되었다. 개발된 센서들은 불소에 대해 선택적인 친화력을 갖는 실리콘을 이 용하므로 불소 이온에 대해 높은 선택성을 보였다. 또한, 합성된 센서에 공액 고분자를 연결하여 그 감도를 성공적으로 증대시켰다.

Analysis of Trans-Acting Elements for Regulation of moc Operons of pTi15955 in Agrobacterium tumefaciens

  • Jung, Won-Hee;Baek, Chang-Ho;Lee, Jeong-Kug;Kim, Kun-Soo
    • Journal of Microbiology and Biotechnology
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    • 제9권5호
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    • pp.637-645
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    • 1999
  • Two putative regulator genes, mocR and mocS, of the moc (mannityl opine catabolism) operons in pTi15955 of the octopine-/mannityl opine-type Agrobacterium tumefaciens strain 15955, were tested for their possible roles as repressors in the moc operons. The regions upstream of macC and mocD, the first structural genes in the two divergently oriented moc operons, were transcriptionally fused into the promoterless lacZ reporter gene. Each of the lacZ-fusions was introduced into Agrobacterium strain UIA5, a Ti plasmid-cured derivative, harboring either a mocR or a mocS clone. The resulting strains were grown in media containing various sugar sources, and the $\beta$-galactosidase activities were quantitatively measured. The results suggested that MocR repressed the expression of macC and macD. The expression of the fused $\beta$-galactosidase was not induced by mannopine (MOP) or possible catabolic intermediates of the opine, e.g. santhopine (SOP), glucose, mannose, or glutamine. However, the repression was significantly relieved by the supplementation of MOP and the concomitant introduction of the agcA gene encoding MOP cyclase that catalyzes the lactonization of MOP to agropine (AGR). These results suggested that AGR, rather than MOP or the other catabolic intermediates, is the inducer for the expression of the operon. On the contrary to previous report showing that the induction levels of macC and macD were lowered by the supplementation of inorganic nitrogen in media, the expression of these genes was not affected by the level of nitrogen in our reporter system. MocS did not strongly repress the expressions of macC and mocD. It is possible that MocS may be involved in the regulation of the operons present downstream of the moc operon, which are responsible for the utilization of mannopinic acid and agropinic acid.

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