61954-80-1Relevant articles and documents
BENZOXAZINONE COMPOUNDS AS KLK5/7 DUAL INHIBITORS
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Paragraph 0176; 0177-0179, (2021/04/10)
The present invention provides compounds and pharmaceutical compositions including the compounds for the treatment of a skin disease associated with proteolytic activity of one or more KLK proteases, wherein the compounds are according to formula (I): whe
Chemical synthesis, crystal structure, versatile evaluation of their biological activities and molecular simulations of novel pyrithiobac derivatives
Wu, Ren-Jun,Zhou, Kai-Xuan,Yang, Haijin,Song, Guo-Qing,Li, Yong-Hong,Fu, Jia-Xin,Zhang, Xiao,Yu, Shu-Jing,Wang, Li-Zhong,Xiong, Li-Xia,Niu, Cong-Wei,Song, Fu-Hang,Yang, Haitao,Wang, Jian-Guo
supporting information, p. 472 - 484 (2019/02/24)
Since pyrithiobac (PTB) is a successful commercial herbicide with very low toxicity against mammals, it is worth exploring its derivatives for an extensive study. Herein, a total of 35 novel compounds were chemically synthesized and single crystal of 6–6
Synthesis and structure activity relationship studies of benzothieno[3,2-b]furan derivatives as a novel class of IKKβ inhibitors
Sugiyama, Hideyuki,Yoshida, Masato,Mori, Kouji,Kawamoto, Tomohiro,Sogabe, Satoshi,Takagi, Terufumi,Oki, Hideyuki,Tanaka, Toshimasa,Kimura, Hiroyuki,Ikeura, Yoshinori
, p. 613 - 624 (2008/02/13)
As a novel class of IKKβ inhibitors, a series of tricyclic furan derivatives was designed and synthesized based on the structure of known thiophene IKKβ inhibitors. Among the various fused furan derivatives synthesized, a benzothieno[3,2-b]furan derivative 13a displayed potent inhibitory activity towards IKKβ in enzymatic and cellular assays. The potent inhibitory activity originates from an intramolecular non-bonded S...O interaction which was confirmed by the X-ray structure of JNK3 with 16k. The introduction of further substituents on the core structure led to the discovery of the 6-alkoxy derivatives, which possessed a comparable IKKβ inhibitory activity to 13a and an improved metabolic stability. Among these, appropriately lipophilic compounds 16a, h, i, and 13g (logD>2) were found to possess good oral bioavailability.