70622-91-2Relevant academic research and scientific papers
Exploration of flexible phenylpropylurea scaffold as novel cardiac myosin activators for the treatment of systolic heart failure
Manickam, Manoj,Jalani, Hitesh B.,Pillaiyar, Thanigaimalai,Sharma, Niti,Boggu, Pulla Reddy,Venkateswararao, Eeda,Lee, You-Jung,Jeon, Eun-Seok,Jung, Sang-Hun
, p. 379 - 391 (2017/04/24)
A series of flexible urea derivatives have been synthesized and demonstrated as selective cardiac myosin ATPase activator. Among them 1-phenethyl-3-(3-phenylpropyl)urea (1, cardiac myosin ATPase activation at 10?μM?=?51.1%; FS?=?18.90; EF?=?12.15) and 1-benzyl-3-(3-phenylpropyl)urea (9, cardiac myosin ATPase activation?=?53.3%; FS?=?30.04; EF?=?18.27) showed significant activity in?vitro and in?vivo. The change of phenyl ring with tetrahydropyran-4-yl moiety viz., 1-(3-phenylpropyl)-3-((tetrahydro-2H-pyran-4-yl)methyl)urea (14, cardiac myosin ATPase activation?=?81.4%; FS?=?20.50; EF?=?13.10), and morpholine moiety viz., 1-(2-morpholinoethyl)-3-(3-phenylpropyl)urea (21, cardiac myosin ATPase activation?=?44.0%; FS?=?24.79; EF?=?15.65), proved to be efficient to activate the cardiac myosin. The potent compounds 1, 9, 14 and 21 were found to be selective for cardiac myosin over skeletal and smooth myosins. Thus, these urea derivatives are potent scaffold to develop as a newer cardiac myosin activator for the treatment of systolic heart failure.
Preparation method for alkyl/benzyl/aryl urea compounds through heterogeneous-phase catalysis
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Paragraph 0063-0071; 0072; 0073; 0074; 0075; 0078; 0079, (2016/10/09)
The invention discloses a preparation method for formula (I) compounds, and the compounds are obtained by reacting a formula (II) compound with a formula (III) compound in a solvent in carbon monoxide atmosphere under catalysis of a heterogeneous-phase pa
Compounds with cardiac myosin activating function and pharmaceutical composition containing the same for treating or preventing heart failure
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Paragraph 0415; 0683-0686, (2017/02/02)
The present invention relates to a compound having a cardiotonic activating function and a pharmaceutical composition containing the same. The composition comprising the compound according to the present invention is effective in preventing or treating heart failure. In addition, the compound is represented by chemical formula 2 or is pharmaceutically acceptable salt thereof.COPYRIGHT KIPO 2016
Pd/C Catalyzed Carbonylation of Azides in the Presence of Amines
Zhao, Jin,Li, Zongyang,Yan, Shuaihu,Xu, Shiyang,Wang, Ming-An,Fu, Bin,Zhang, Zhenhua
, p. 1736 - 1739 (2016/05/19)
A facile and efficient Pd/C-catalyzed carbonylation of both aliphatic and aromatic azides in the presence of amines is reported. Serving as the widely existed fragments in an array of biological pharmaceuticals, functionalized unsymmetrical ureas were str
Compounds with cardiac myosin activating function and pharmaceutical composition containing the same for treating or preventing heart failure
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Paragraph 0413-0416; 0683-0686, (2016/10/07)
Disclosed are a compound having cardiotonic activity and a pharmaceutical composition containing the same, and the composition containing the compound, according to the present invention, is useful for preventing and treating heart failure.COPYRIGHT KIPO 2016
An efficient two-step synthesis of mono-, di- and triureas from resin- bound amides
Nefzi, Adel,Ong, Nhi A.,Houghten, Richard A.
, p. 5441 - 5446 (2007/10/03)
An efficient method for the solid-phase synthesis of mono-, di- and triureas from resin-bound mono-amines, diamines and triamines is described. The exhaustive reduction of solid support-bound amides generated the requisite amines, which, following treatme
Ureylene anticonvulsants and related compounds
Dimmock,Vashishtha,Stables
, p. 490 - 494 (2007/10/03)
The results from a previous study led to the postulate that a number of aryl semicarbazones displaying anticonvulsant activity in the maximal electroshock (MES) screen interacted at both a hydrophobic and a hydrogen bonding areas on a specific binding site. These two parts of the binding site may be referred to as areas A and B, respectively. In order to circumvent the possible problems of the carbimino group in semicarbazones, such as toxicity and acid lability, some related ureylenes were considered. Initial evidence suggested that a second lipophilic group in the molecule was advantageous; this group may interact at area C on the proposed binding site. Most of the compounds prepared with a view to interacting at areas A, B and C showed protection in mice against MES induced siezures. Of particular interest were the compounds 1d, j which contained an α-methylbenzyl group attached to the N1 atom of the ureylenes which afforded good protection in the MES screen. The areas A and C at which lipophilic moieties were considered to interact were capable of accommodating groups of different sizes as measured by their solvent accessible surface areas. A number of compounds were active when given orally to rats and devoid of neurotoxicity at the doses utilized. Several compounds including 1d, f, j, 2d are useful prototypic molecules for subsequent development of further novel anticonvulsants.
