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GIST Repository College of Natural Sciences Department of Chemistry 1. Journal Articles

Synthesis and biological evaluation of alpha-sulfonamido-N-adamantanecarboxamide derivatives as 11 beta-HSD1 inhibitors

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Author(s)
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
Type
Article
Citation
MedChemComm, v.6, no.7, pp.1360 - 1369
Issued Date
2015-07
Abstract
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.
Publisher
Royal Society of Chemistry
ISSN
2040-2503
DOI
10.1039/c5md00096c
URI
https://scholar.gist.ac.kr/handle/local/31625
Appears in Collections:
Department of Chemistry > 1. Journal Articles
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