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제109회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Design and synthesis of triazole-based inhibitors of influenza virus Neuraminidase

등록일
2012년 2월 17일 21시 58분 54초
접수번호
1289
발표코드
MEDI.P-1021 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
4월 25일 (수요일) 18:00~21:00
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
정강연, 김태우, Tasneem Islam1
강릉원주대학교 생명화학공학과, Korea
1Department of Biological, Chemical and Physical Sciences, Roosevelt University, 1400 North Rossevelt Blud, IL, USA, United States
Influenza is a major cause of mortality, particularly in children and the elderly. The global impact of influenza epidemics is estimated to be 3.5 million cases of severe illness and 300,000 to 500,000 deaths annually. Protection through vaccination is limited due to the antigenic variation of the influenza virus. Antiviral agents, thus far remain an important approach to epidemic influenza. Rational drug design has led to the discovery of the two anti-influenza drugs currently being used to treat infected patients (oseltamivir, TamifluTM and zanamivir, RelenzaTM). Reports of the emergence of drug resistance make the development of new anti-influenza molecules a priority. Two sialic acid recognizing proteins, hemagglutinin and sialidase, on the viral surface have been shown to be crucial in invasion and have provided many exciting opportunities for rational structure-based drug discovery of anti-influenza agents. To date the most successful structure-based anti-influenza drug discovery has arisen from targeting the sialidase function. In order to study important recognition features required in the inhibition of sialidase, we synthesized a range of sialyl nucleoside mimetics based on very inexpensive carbohydrate. D-Fructose was used as a substrate for the efficient preparation of 1,2,3-triazole derivatives using the copper-catalyzed azide?alkyne Huisgen cycloaddition (“click chemistry”). As a preliminary study, a small library of 1,2,3-triazole-linked D-fructose derivatives has been synthesized in good yield which will be screened for its influence on influenza neuraminidase inhibitory activity.

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