198554-64-2Relevant academic research and scientific papers
Design, synthesis and decoration of molecular scaffolds for exploitation in the production of alkaloid-like libraries
Craven, Philip,Aimon, Anthony,Dow, Mark,Fleury-Bregeot, Nicolas,Guilleux, Rachel,Morgentin, Remy,Roche, Didier,Kalliokoski, Tuomo,Foster, Richard,Marsden, Stephen P.,Nelson, Adam
supporting information, p. 2629 - 2635 (2015/01/30)
The design, synthesis and decoration of six small molecule libraries is described. Each library was inspired by structures embedded in the framework of specific alkaloid natural products. The development of optimised syntheses of the required molecular scaffolds is described, in which reactions including Pd-catalysed aminoarylation and diplolar cycloadditions have been exploited as key steps. The synthesis of selected exemplar screening compounds is also described. In five cases, libraries were subsequently nominated for production on the basis of the scope and limitations of the validation work, as well as predicted molecular properties. In total, the research has led to the successful synthesis of >2500 novel alkaloid-like compounds for addition to the screening collection (the Joint European Compound Library, JECL) of the European Lead Factory.
Novel piperidinylpyrimidine derivatives as inhibitors of HIV-1 LTR activation
Fujiwara, Norio,Nakajima, Takashi,Ueda, Yutaka,Fujita, Hitoshi,Kawakami, Hajime
experimental part, p. 9804 - 9816 (2009/04/06)
Piperidinylpyrimidine derivatives, previously prepared as inhibitors of TNF-α production, were evaluated for their inhibitory activity against HIV-1 LTR activation. Some of these derivatives inhibited activation of HIV-1 LTR-directed CAT gene expression i
Synthesis and bioactivities of novel piperidylpyrimidine derivatives: Inhibitors of tumor necrosis factor-alpha production
Fujiwara, Norio,Fujita, Hitoshi,Iwai, Kiyotaka,Kurimoto, Ayumu,Murata, Shinobu,Kawakami, Hajime
, p. 1317 - 1320 (2007/10/03)
New piperidylpyrimidine derivatives, including quinazolines, were prepared, and their abilities to inhibit TNF-α production evaluated. Some compounds showed potent inhibitory activity in mouse macrophages stimulated with LPS. The synthesis and structure-activity relationships of these compounds are described. (C) 2000 Elsevier Science Ltd. All rights reserved.
Triazine angiogenesis inhibitors
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, (2008/06/13)
Compounds having Formula I STR1 or pharmaceutically acceptable salts or prodrugs thereof, are useful for treating pathological states which arise from or are exacerbated by angiogenesis. The invention also relates to pharmaceutical compositions comprising these compounds and to methods of inhibiting anglogenesis in a mammal.
Piperidinylpyrimidine derivatives
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, (2008/06/13)
A compound of formula (1) STR1 wherein X1 is amino or hydroxyl, X2 is carbonyl and the like R1 is an alkyl, an aryl and the like, R2 is hydrogen and the like, and R3 is an alkyl and the like, or a pharmaceutical acceptable salt thereof is effective for inibiting the production and/or secretion of tumor necrosis factor in a patient in need of such inhibition.
