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| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Exhibition Hall 2 |
| Time |
4월 18일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-420 |
| Subject |
Pyrrolo[2,3-D] Pyrimidine derivatives, A Cathepsin K Inhibitor for The Treatment of Osteoporosis
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| Authors |
Jusuk Lee, Ji Hoon Lee*
New Drug Development Center, Daegu Gyeongbuk Medical Innovation Foundation, Korea
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| Abstract |
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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| E-mail |
js001.lee@dgmif.re.kr |
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123rd General Meeting of the KCS