111452-72-3Relevant academic research and scientific papers
DIPHENYLMETHYL PIPERAZINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION USING SAME
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Paragraph 0073; 0095, (2014/10/16)
The present invention provides: a novel compound which has a useful pharmacological action for treating heart failure or shock without increasing heart rate; and a pharmaceutical composition using the same. The present invention relates to a diphenylmethy
Al(OTf)3-mediated epoxide ring-opening reactions: Toward piperazine-derived physiologically active products
Williams, D. Bradley G.,Cullen, Adam
supporting information; experimental part, p. 9509 - 9512 (2010/03/04)
(Chemical Equation Presented) Al(OTf)3 is a good catalyst for the ring opening of epoxides, forming β-amino alcohols bearing the piperazine motif. Two different strategies were examined, where the glycidyl ether resided on one-half of the molec
Anticancer agents
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Page/Page column 6, (2008/06/13)
Disclosed herein is a method for suppressing the growth of cancer cells in a mammal in need of such treatment comprising administering to said mammal a cancer cell suppressing amount of a diphenylmethylpiperazine represented by the following general formu
Synthesis and structure-activity relationships of 6-heterocyclic- substituted purines as inactivation modifiers of cardiac sodium channels
Estep,Josef,Bacon,Carabateas,Rumney IV,Pilling,Krafte,Volberg,Dillon,Dugrenier,Briggs,Canniff,Gorczyca,Stankus,Ezrin
, p. 2582 - 2595 (2007/10/02)
Purine-based analogs of SDZ 211-500 (5) were prepared and evaluated as inactivation modifiers of guinea pig or human cardiac sodium (Na) channels expressed in Xenopus oocytes. Substances which remove or slow the Na channel inactivation process in cardiac tissue are anticipated to prolong the effective refractory period and increase inotropy and thus have potential utility as antiarrhythmic agents. Heterocyclic substitution at the 6-position of the purine ring resulted in compounds with increased Na activity and potency, with 5-membered heterocycles being optimal. Only minor modifications to the benzhydrylpiperazine side chain were tolerated. Selected compounds which delayed the inactivation of Na channels were found to increase refractoriness and contractility in a rabbit Langendorff heart model, consistent with the cellular mechanism. Activity in both the oocyte and rabbit heart assays was specific to the S enantiomers. Preliminary in vivo activity has been demonstrated following intravenous infusion. The most promising compound on the basis of in vitro data is the formylpyrrole (S)74, which is 25-fold more potent than DPI 201-106 (1) in the human heart Na channel assay.
Diphenylmethyl piperazine derivatives
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, (2008/06/13)
Novel diphenylmethyl piperazine derivatives of this invention have a chemical structure represented by the following Formula [I]: STR1 wherein R represents STR2 The compounds have an effect of inhibiting the overcontraction and overextension of the myocar
Synthesis and Biological Activity of 4-(Diphenylmethyl)-α--1-piperazineethanol and Related Compounds
Sircar, Ila,Haleen, Steve J.,Burke, Sandra E.,Barth, Hubert
, p. 4442 - 4449 (2007/10/02)
A series of 4-(diphenylmethyl)-α--1-piperazineethanol and closely related compounds was synthesised and evaluated for cardiac and vascular activity in isolated perfused rat and guinea pig hearts.Compound 1 produced greater inotropic effects in rat hearts than in guinea pig hearts, a phenomenon which was also observed with the prototype agent DPI 201-106.Compound 15 produced an inotropic effect with one-tenth the potency of compound 1.Both compounds 1 and 15 demonstrated direct inotropic and vasodilatory effects when administered iv in anesthetized dogs, although the vasodilatory activity was more pronounced with compound 15 than 1 and DPI compound.Compound 1 lacks the CN moiety which is a key structural requirement in DPI for positive inotropic activity.The synthesis, in vitro, and in vivo evaluations of these agents, and comparative data with DPI-201-106 (compound 17) are reported.
Purine derivatives, medicaments containing them and methods of treating cardiac insufficiencies and irregularities with them.
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, (2008/06/13)
The compounds of formula I, STR1 in free form or in salt form have cardiotonic and antiarrhythmic activity. They may be used as medicaments. They are obtained by means of appropriate 3-amino-2-hydroxy-propylation of purines.
