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  • 05월 20일 18시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제125회 대한화학회 학술발표회 및 총회 Synthesis and biological evaluation of 6-Amino-4-anilinoquinazoline as potential MERS-CoV inhibitors

등록일
2020년 2월 6일 13시 37분 57초
접수번호
0820
발표코드
MEDI.P-703 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
온라인 PDF 제출
발표형식
포스터
발표분야
Medicinal Chemistry
저자 및
공동저자
Jun Young Lee, Chul Min Park, Hyoung Rae Kim*
CEVI, Korea Research Institute of Chemical Technology, Korea
Middle East respiratory syndrome coronavirus (MERS-CoV) has been one of the scariest disease owing to its mortality and possibility of global outbreak. Until July 2019, a total of 2458 laboratory-confirmed cases of MERS, including 848 associated deaths (case-fatality rate: 34.5%) were globally reported from 27 countries. The MERS-CoV is the genus of Betacoronavirus in the family Coronaviridae. Coronaviruses are a group of positive-sense, single-stranded RNA viruses. The transmission of MERS-CoV is suspected through the respiratory secretions, such as coughing of an infected person. There is currently no effective vaccine or therapy available to prevent or treat infection with MERS-CoV. However, several fundamental and clinical studies have been completed or are underway. We screened 200,000 compounds of Korean Chemical Bank (KCB) against MERS-CoV using high content screening (HCS) platform of Institut Pasteur Korea (IPK). We found that 6-amino-4-anilinoquinazoline families were effective for inhibiting MERS-CoV infection. Quinazoline derivatives have previously been effective for inhibiting MERS-CoV infection. Quinazoline derivatives have previously been reported as potent inhibitors of the protein kinase of epidermal growth factor receptor (EGFR). Most of those compounds were approved as anticancer drugs, including Gefitinib, Lapatinib, Erlotinib, and Afatinib. We thought that quinazoline compounds can exhibit good bioavailability and be easily extended to treatment of MERS-CoV infection. This presentation will discuss the synthesis and biological effects of 4-anilino-quinazoline derivatives.

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