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학술발표회초록보기

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  • 09월 01일 18시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제118회 대한화학회 학술발표회, 총회 및 기기전시회 안내 6,7,8,9-tetrahydrobenzo[4,5]thieno[3,2-e][1,2,4]triazolo [4,3-a]pyrimidin-5(4H)-one analogs with Polio, Coxsackie and Rhino Virus Inhibition Activity

등록일
2016년 9월 1일 16시 56분 51초
접수번호
2487
발표코드
MEDI.P-514 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
10월 13일 (목요일) 11:00~12:30
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
BISWAS BISHYAJIT KUMAR, Yashwardhan Malpani1, 이상호2, 한수봉3, 정영식4,*
과학기술연합대학원대학교(UST) 의약 및 약품화학, Korea
1과학기술연합대학원대학교(UST) 의약 약품화학, Korea
2한국화학연구원 신약연구단, Korea
3한국화학연구원 신약연구본부, Korea
4한국화학연구원 신물질연구단, Korea
A series of 6,7,8,9-tetrahydrobenzo[4,5]thieno[3,2-e]triazolo[4,3-a]pyrimidin-5(4H)-one analogs (A), were synthesized and tested for their inhibitory activity against representative picornaviruses. A brief structure activity relationship (SAR) could be established with activities in micro-molar range for the best compounds. The prepared compounds were tested against Coxsackie B1 (Cox B1), Coxsackie B3 (Cox B3), Poliovirus 3 (PV3), Human Rhinovirus 14 (HRV14), Human Rhinovirus 21 (HRV21) and Human Rhinovirus 71 (HRV71). Some of these compounds showed good activity (selective index values >10) against these representative picornaviruses. The presence of tert-butyl side chain on the fused tetrahydrobenzene ring was highly essential for the activity of these analogs against these picornaviruses. Initial time of addition study rules out capsid binding inhibition at entry stages but it is expected to act at later stage/s of picornavirus lifecycle/replication. The present study resulted in discovery of triazolothienopyrimidinones as novel skeleton against picornaviruses.

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