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  • 09월 10일 16시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제124회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Synthesis of siderophore equipped antibiotic to penetrate cell wall of Gram negative bacteria.

2019년 8월 29일 13시 32분 12초
MEDI.P-279 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
10월 17일 (목요일) 11:00~12:30
Medicinal Chemistry
저자 및
Byung soo Lee, Jeungsoon Choi*
Legochem Biosciences, Inc., Korea

Nowadays, the Gram-negative bacteria research re-gained its interest due to the growing concern of the lack of treatment against drug-resistant bacteria. The mutations in outer membrane and porin channel are the main causes of this resistance, prohibiting the drug from penetrating into bacteria. To overcome these resistance, many research groups have mimicked “siderophore”, high-affinity iron-chealating compound that bacteria produces to transport iron ion across cell membrane for its essential ingredient. Thus, siderophore was incorporated into the antibiotic via a specific linker to penetrate cell wall of bacteria, then its active ingredient would show antibacterial activity in the cell. LCB10-0200, was patented by LegoChemBioscience (US2012/264727) which represnts a typical example of this strategy in which cepha unit was connected to the dihydroxypyridinone siderophore via disubstituted pyrimidine linker. Here in this poster, we will show the total synthesis of LCB10-0200 in the original medicinal chemistry (mg scale) as well as the synthesis in view of process chemistry for larger scale (kg scale), specifically focused on the linker-siderophore unit.