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  • 02월 28일 17시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제123회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Pyrrolo[2,3-D] Pyrimidine derivatives, A Cathepsin K Inhibitor for The Treatment of Osteoporosis

등록일
2019년 2월 14일 15시 27분 03초
접수번호
4510
발표코드
MEDI.P-420 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
4월 18일 (목요일) 11:00~12:30
발표형식
포스터
발표분야
Medicinal Chemistry
저자 및
공동저자
Jusuk Lee, Ji Hoon Lee*
New Drug Development Center, Daegu Gyeongbuk Medical Innovation Foundation, Korea
Osteoporosis is a disease where increased bone weakness increases the risk of a broken bone. When bone resorption exceeds bone formation, pathologic processes, such as osteoporosis, can result. Cathepsin K, a lysosomal cysteine protease that is expressed by osteoclasts during the process of bone resorption, acts as the major collagenase responsible for the degradation of the organic bone matrix during the bone remodeling process. Because excessive bone remodeling is a key element in the pathogenesis of postmenopausal osteoporosis and other skeletal disorders, cathepsin K is a potential target for therapeutic intervention. In order to develop new inhibitors of Cathepsin K, we synthesized a series of prrolo [2,3-D] pyrimidine derivatives and evaluated their in vitro cathepsin K inhibitory activity. The screenig results show that the potency of most compounds were equal to or greater than that of the reference compound. Finally, we found prrolo [2,3-D] pyrimidine structure as highly potent Cathepsin K inhibitor.

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