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Synthesis and biological evaluation of α-sulfonamido-N-adamantanecarboxamide derivatives as 11β-HSD1 inhibitors
- Kim, Young Hoon;
- Kang, Seung Kyu;
- Lee, Gwi Bin;
- Lee, Kyu Myung;
- Kumar, Jaladi Ashok;
- ... Lee, Won Koo;
- 외 5명
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0초록
A series of alpha-sulfonamido-N-adamantanecarboxamide derivatives as 11 beta-HSD1 inhibitors was identified. Among them, compound 7j was the most active with an IC50 value of 8 nM in humans 11 beta-HSD1. Compound 7j exhibited reasonable stability, permeability and safety profiles (CYP and hERG). Compound 7j showed good ex vivo 11 beta-HSD1 inhibition with similar to 80% inhibition after 20 MPK oral dosing.
키워드
11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE-1; VISCERAL OBESITY; DISCOVERY; GLUCOSE
- 제목
- Synthesis and biological evaluation of α-sulfonamido-N-adamantanecarboxamide derivatives as 11β-HSD1 inhibitors
- 저자
- Kim, Young Hoon; Kang, Seung Kyu; Lee, Gwi Bin; Lee, Kyu Myung; Kumar, Jaladi Ashok; Kim, Ki Young; Dal Rhee, Sang; Joo, Jeongmin; Bae, Myung Ae; Lee, Won Koo; Ahn, Jin Hee
- 발행일
- 2015-07-01
- 유형
- Article
- 저널명
- MedChemComm
- 권
- 6
- 호
- 7
- 페이지
- 1360 ~ 1369