56406-20-3Relevant academic research and scientific papers
Discovery of decamidine as a new and potent PRMT1 inhibitor
Zhang, Jing,Qian, Kun,Yan, Chunli,He, Maomao,Jassim, Brenson A.,Ivanov, Ivaylo,Zheng, Yujun George
supporting information, p. 440 - 444 (2017/03/08)
Protein arginine methyltransferase 1 (PRMT1) is a key player for the dynamic regulation of arginine methylation. Its dysregulation and aberrant expression are implicated in various pathological conditions, and a plethora of evidence suggests that PRMT1 inhibition is of significant therapeutic value. Herein, we reported the modification of a series of diamidine compounds with varied lengths in the middle alkyl linker for PRMT1 inhibition. Decamidine (2j), which possesses the longest linker in the series, displayed 2- and 4-fold increase in PRMT1 inhibition (IC50 = 13 μM), compared with furamidine and stilbamidine. The inhibitory activity toward PRMT1 was validated by secondary orthogonal assays. Docking studies showed that the increased activity is due to the extra interaction of the amidine group with the SAM binding pocket, which is absent when the linker is not long enough. These results provide structural insights into developing the amidine type of PRMT1 inhibitors.
Molecular tectonics: Generation of 1-D interdigitated and 2-D interwoven helical silver coordination networks by oligoethylene glycol based tectons bearing two benzonitrile moieties
Bourlier, Julien,Hosseini, Mir Wais,Planeix, Jean-Marc,Kyritsakas, Nathalie
, p. 25 - 32 (2007/10/03)
Ligands based on oligoethylene glycol units bearing at their extremities benzonitrile groups behave in the crystalline phase as tectons and lead in the presence of silver cation to different coordination networks. Depending on the number of glycol units, 1-D stair type or 1-D interdigitated and 2-D interwoven architectures composed of helical strands are obtained. The Royal Society of Chemistry and the Centre National de la Recherche Scientifique.
Sulfonamide bridging compounds that inhibit tryptase activity
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, (2008/06/13)
The present invention is directed to compounds which are capable of inhibiting the activity of tryptase. Such compounds are useful in the treatment or prevention of inflammatory disease, particularly those disease states which are mediated by mast cell activation. Also encompassed by the invention are formulations comprising the noted compounds, processes for preparing such compounds and methods for treating or preventing an inflammatory disease.
Analogues of 1,5-bis(4-amidinophenoxy)pentane (pentamidine) in the treatment of experimental Pneumocystis carinii pneumonia
Tidwell,Jones,Geratz,Ohemeng,Cory,Hall
, p. 1252 - 1257 (2007/10/02)
A series of 33 analogues of the anti-Pneumocystis carinii drug 1,5-bis(4-amidinophenoxy)pentane (pentamidine) was synthesized for screening against a rat model of P. carinii pneumonia (PCP). Twenty-five of the compounds showed efficacy against PCP when compared to a saline-treated control group. Two compounds, 1,4-bis(4-amidinophenoxy)butane (butamidine, 6) and 1,3-bis(4-amidino-2-methoxyphenoxy)propane (DAMP, 16), were statistically more effective than the parent drug in treating PCP in the rat model of infection. In addition to their activity against PCP, the compounds were also evaluated for antitrypsin activity, ability to inhibit thymidylate synthetase, affinity for DNA, and toxicity. No correlation was observed between the tested molecular interactions of the diamidines and their effectiveness against PCP.
Bis(4-[4'-hydroxy-5'-carboxy-2'-pyrimidinyl]phenoxy)alkanes
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, (2008/06/13)
5-Carboxypyrimidine derivatives and their pharmaceutically acceptable basic salts, and their use as antiallergy agents.
