18226-07-8Relevant academic research and scientific papers
Design and synthesis of histamine H3/H4 receptor ligands with a cyclopropane scaffold
Watanabe, Mizuki,Kobayashi, Takaaki,Ito, Yoshihiko,Fukuda, Hayato,Yamada, Shizuo,Arisawa, Mitsuhiro,Shuto, Satoshi
, p. 3630 - 3633 (2018)
We previously designed and synthesized a series of histamine analogues with an imidazolylcyclopropane scaffold and identified potent non-selective antagonists for histamine H3 and H4 receptor subtypes. In this study, to develop H4 selective ligands, we newly designed and synthesized cyclopropane-based derivatives having an indole, benzimidazole, or piperazine structure, which are components of representative H4 selective antagonists such as JNJ7777120 and JNJ10191584. Among the synthesized derivatives, imidazolylcyclopropanes 12 and 13 conjugated with a benzimidazole showed binding affinity to the H3 and H4 receptors comparable to that of a well-known non-selective H3/H4 antagonist, thioperamide. These results suggest that the binding modes of the cyclopropane-based H3/H4 ligands in the H4 receptor can be different from those of the indole/benzimidazole-piperazine derivatives.
Method for preparing 1,4,7,10-tetraaza-2,6-pyridinophane
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Paragraph 0038, (2017/08/28)
The invention relates to a novel method for preparing 1,4,7,10-tetraaza-2,6-pyridinophane. 2,6-dimethylamino pyridine serving as a raw material is subjected to amino protection through o-/p-nitrobenzenesulfonyl and reacts with N,N-di(2-chloroethyl)-o-/p-n
Ras oncoprotein inhibitors: The discovery of potent, ras nucleotide exchange inhibitors and the structural determination of a drug-protein complex
Taveras,Remiszewski,Doll,Cesarz,Huang,Kirschmeier,Pramanik,Snow,Wang,Del Rosario,Vibulbhan,Bauer,Brown,Carr,Catino,Evans,Girijavallabhan,Heimark,James,Liberles,Nash,Perkins,Senior,Tsarbopoulos,Ganguly,Aust,Brown,Delisle,Fuhrman,Hendrickson,Kissinger,Love,Sisson,Villafranca,Webber
, p. 125 - 133 (2007/10/03)
The nucleotide exchange process is one of the key activation steps regulating the ras protein. This report describes the development of potent, non-nucleotide, small organic inhibitors of the ras nucleotide exchange process. These inhibitors bind to the r
