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  • 02월 19일 10시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제121회 대한화학회 학술발표회, 총회 및 기기전시회 안내 In search of a next generation Bedaquiline for the treatment of Tuberculosis

등록일
2018년 1월 15일 16시 12분 53초
접수번호
3202
발표코드
BIO.O-2 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
목 09시 : 20분
발표형식
구두발표
발표분야
Life Chemistry - Oral Presentation in Chemistry of Life
저자 및
공동저자
Peter Choi*, Hamish S. Sutherland, Amy S.T. Tong, Adrian Blaser, Daniel Conole, Christopher B. Cooper1, Scott G. Franzblau2, Anna M. Upton1, William A. Denny, Brian D. Palmer
Auckland Cancer Society Research Centre, University of Auckland, New Zealand
1Global Alliance for TB Drug Development, United States
2Institute for Tuberculosis Research, University of Illinois at Chicago, United States
※ 국외소속으로 등록된 저자의 승인여부는 최소 3일이내 발표자 email로 알려드립니다.
승인 9건

Bedaquiline (1) is the first FDA approved drug for the treatment of tuberculosis (TB) in 40 years and the first of the diarylaminoquinoline class. It has a novel mechanism of action through inhibition of the mycobacterial ATP synthase enzyme.1 It demonstrates excellent efficacy against TB, but induces phospholipidosis at high doses, has a long terminal elimination half-life (due to its high lipophilicity) and exhibits potent hERG channel inhibition, resulting in clinical QTc interval prolongation.2 A range analogues of 1 have been prepared to address these issues and evaluated for their anti- M.tb activity (MIC90) to examine their use as effective and safer second generation analogues of 1. References 1. Koul, A.N.; Dendouga, K.; Vergauwen, B.; Molenberghs, B.; Vranckx, L.; Willebrords, R.; Ristic, Z.; Lill, H.; Dorange, I.; Guillemont, J.; Bald, D;, Andries, K. Diarylquinolines target subunit c of mycobacterial ATP synthase. Nat. Chem. Biol. 2007, 3, 323-324. 2. Kakkar, A.K.; Dahiya, N. Bedaquiline for the treatment of resistant tuberculosis: Promises and pitfalls. Tuberculosis 2014, 94 (4), 357-362.


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