87120-73-8Relevant articles and documents
Synthesis and antimicrobial activity of some new of 2-(furan-2-yl)-1-(piperidin-4-yl)-1H-benzo[d]imidazole derivatives
Parmar, Tejasvi H.,Sangani, Chetan B.,Parmar, Nilesh D.,Bhalodiya, Pradip C.
, p. 471 - 481 (2018)
We report a series of new heterocyclic compounds containing the imidazole scaffold were synthesized such as 2-(furan-2-yl)-1-(piperidine-4-yl)-1H-benzo[d]imidazole derivative. Due to the biological activities of imidazole as antimicrobial agents, in the p
Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening
Wellaway, Christopher R.,Amans, Dominique,Bamborough, Paul,Barnett, Heather,Bit, Rino A.,Brown, Jack A.,Carlson, Neil R.,Chung, Chun-Wa,Cooper, Anthony W. J.,Craggs, Peter D.,Davis, Robert P.,Dean, Tony W.,Evans, John P.,Gordon, Laurie,Harada, Isobel L.,Hirst, David J.,Humphreys, Philip G.,Jones, Katherine L.,Lewis, Antonia J.,Lindon, Matthew J.,Lugo, Dave,Mahmood, Mahnoor,McCleary, Scott,Medeiros, Patricia,Mitchell, Darren J.,O'Sullivan, Michael,Le Gall, Armelle,Patel, Vipulkumar K.,Patten, Chris,Poole, Darren L.,Shah, Rishi R.,Smith, Jane E.,Stafford, Kayleigh A. J.,Thomas, Pamela J.,Vimal, Mythily,Wall, Ian D.,Watson, Robert J.,Wellaway, Natalie,Yao, Gang,Prinjha, Rab K.
, p. 714 - 746 (2020/02/04)
The bromodomain and extraterminal (BET) family of bromodomain-containing proteins are important regulators of the epigenome through their ability to recognize N-acetyl lysine (KAc) post-translational modifications on histone tails. These interactions have been implicated in various disease states and, consequently, disruption of BET-KAc binding has emerged as an attractive therapeutic strategy with a number of small molecule inhibitors now under investigation in the clinic. However, until the utility of these advanced candidates is fully assessed by these trials, there remains scope for the discovery of inhibitors from new chemotypes with alternative physicochemical, pharmacokinetic, and pharmacodynamic profiles. Herein, we describe the discovery of a candidate-quality dimethylpyridone benzimidazole compound which originated from the hybridization of a dimethylphenol benzimidazole series, identified using encoded library technology, with an N-methyl pyridone series identified through fragment screening. Optimization via structure- and property-based design led to I-BET469, which possesses favorable oral pharmacokinetic properties, displays activity in vivo, and is projected to have a low human efficacious dose.
The preparation method of the deuterium generation of Mauzy is special
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Paragraph 0028; 0036-0037, (2017/07/01)
The invention discloses a preparation method of deuterated pimozide. The pimozide-d4 is synthesized from 4-bromopentafluorobenzene-d4 through eight steps. The provided preparation method has the advantages of reasonable technological design, simple operation, easy product separation and purification, easily-available raw materials, high yield, and high purity. The isotope abundance of the obtained target product is high. The prepared stable isotope-labeled pimozide-d4 can be well applied to clinical pharmacokinetics researches, so people can acknowledge the metabolism process and action mechanism of pimozide in human body more precisely and conveniently, and thus the deuterated pimozide has an important application value.
