141783-63-3Relevant articles and documents
BIOCONJUGATION OF POLYPEPTIDES
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Page/Page column 58; 63; 64, (2019/04/26)
Certain embodiments of the present invention relate to methods of forming and manipulating bioconjugates. Particularly, but not exclusively certain embodiments relate to methods of reversible carbon-carbon bond bioconjugation using aldol based chemical reactions at physiological conditions.
HETEROCYCLE CARBOXAMIDE DERIVATIVES HAVING ADAMANTYL GROUP, PROCESS FOR PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME AS AN ACTIVE INGREDIENT
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, (2017/08/18)
The present invention relates to a heterocyclic carboxamide derivative having an adamantyl group represented by chemical formula 1 which inhibits the activity of 11andbeta;-hydroxysteroid dehydrogenase type 1 (11andbeta;-HSD1), a prodrug of the same, a solvate of the same, a stereoisomer or a pharmaceutically acceptable salt of the same, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. In the chemical formula 1, W, X, R_1, R_2, L, a, and b are as defined in the specification of the present invention.COPYRIGHT KIPO 2017
Synthesis and 11β hydroxysteroid dehydrogenase 1 inhibition of thiazolidine derivatives with an adamantyl group
Kwon, Sung Wook,Kang, Seung Kyu,Lee, Jae Hong,Bok, Joo Hwan,Kim, Chi Hyun,Rhee, Sang Dal,Jung, Won Hoon,Kim, Hee Youn,Bae, Myung Ae,Song, Jin Sook,Ha, Duck Chan,Cheon, Hyae Gyoung,Kim, Ki Young,Ahn, Jin Hee
scheme or table, p. 435 - 439 (2011/02/28)
A new series of thiazolidine derivatives with an adamantyl group was synthesized and evaluated for their ability to inhibit 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1). Our initial compound 5a showed a weak inhibitory activity. Significant improvements in potency were achieved by substituent modification. The potent compound 8g (E) showed good in vitro inhibitory activity toward human 11β-HSD1, selectivity toward 11β-HSD2, metabolic stability, pharmacokinetic, and safety profile. Furthermore, this compound significantly inhibited 11β-HSD1 activity in rat and monkey models, and showed improved glycemic control in KKAy mice.