38675-31-9Relevant articles and documents
Identification of N-arylsulfonylpyrimidones as anticancer agents
Subramanian, Santhosh,Boggu, Pulla Reddy,Yun, Jieun,Jung, Sang-Hun
, p. 251 - 258 (2018/03/09)
For confirming the role of five membered ring of imidazolidinone moiety of N-arylsulfonylimidazolidinones (7) previously reported with highly potent anticancer agent, a series of N-arylsulfonylpyrimidones (10a–g) and N-arylsulfonyltetrahydropyrimidones (11a–e) were prepared and their anti-proliferating activity was measured against human cancer cell lines (renal ACHN, colon HCT-15, breast MDA-MB-231, lung NCI-H23, stomach NUGC-3, and prostate PC-3) using XTT assay. Among them, 1-(1-acetylindolin-5-ylsulfonyl)-4-phenyltetrahydropyrimidin-2(1H)-one (11d, mean GI50?=?3.50?μM) and ethyl 5-(2-oxo-4-phenyltetrahydropyrimidin-1(2H)-ylsulfonyl)-indoline-1-carboxylate (11e, mean GI50?=?0.26?μM) showed best growth inhibitory activity against human cancer cell lines. Considering the activity results, N-arylsulfonyltetrahydropyrimidones (11) exhibited more potent activity compared to N-arylsulfonylpyrimidones (10) and comparable activity to N-arylsulfonylimidazolidinones (7). Especially, tetrahydropyrimidin-2(1H)-one analogs containing acylindolin-5-ylsulfonyl moiety at position 1 demonstrated their strong growth inhibitory activity against human cancer cell lines.
Compounds with cardiac myosin activating function and pharmaceutical composition containing the same for treating or preventing heart failure
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Paragraph 0704-0706, (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
Compounds with cardiac myosin activating function and pharmaceutical composition containing the same for treating or preventing heart failure
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Paragraph 0704-0706, (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
Synthesis and SAR of highly potent and selective dopamine D 3-receptor antagonists: 1H-Pyrimidin-2-one derivatives
Geneste, Herve,Backfisch, Gisela,Braje, Wilfried,Delzer, Juergen,Haupt, Andreas,Hutchins, Charles W.,King, Linda L.,Kling, Andreas,Teschendorf, Hans-Juergen,Unger, Liliane,Wernet, Wolfgang
, p. 490 - 494 (2007/10/03)
The synthesis and SAR of novel highly potent and selective dopamine D 3-receptor antagonists based on a 1H-pyrimidin-2-one scaffold are described. A-690344 antagonized PD 128907-induced huddling deficits in rat (ED50 6.1 mg/kg po), a social interaction paradigm.
SYNTHESIS OF SUBSTITUTED 2- AND 4-HYDROXYAMINOPYRIMIDINES
Moskalenko, G. G.,Sedova, V. F..,Mamaev, V. P.
, p. 1232 - 1236 (2007/10/02)
The reaction of 2- and 4-chlorine-containing alkyl(aryl)pyrimidines with hydroxylamine was studied.It was shown that, depending on the amount of hydroxylamine , N,O-dipyrimidinylhydroxyamides or the corresponding 2- and 4-hydroxyaminopyrimidines are formed together with 2- and 4-oxodihydropyrimidines.
Transformations of 2-Aminopyrimidines and Their N-Oxides under Diazotation Conditions
Sedova, V. F.,Mustafina, T. Yu.,Krivopalov, V. P.,Mamaev, V. P.
, p. 91 - 94 (2007/10/02)
The diazotation of 2-aminopyrimidines and their N-oxides in solutions with various acidities was studied.It is shown that the amino group in pyrimidine N-oxides is not diazotized in strongly acidic media and that bromination in the 5 position of the pyrimidine ring is observed in concentrated hydrobromic acid.When the reaction was carried out in moderately acidic media, it was possible to synthesize the difficult-to-obtain 2-halopyrimidine N-oxides.
REACTIVITY OF 4,7-DIHYDRO-5-PHENYL-1,2,4-OXADIAZEPIN-3(2H)-ONES
Lassalvy, Christiane,Petrus, Clement,Petrus, Francoise
, p. 273 - 278 (2007/10/02)
The reactions of 4,7-dihydro-5-phenyl-1,2,4-oxadiazepin-3(2H)-ones have been studied.The behaviour of this unsaturated, seven-membered heterocyclic series, which possesses an O-NH-CO-NH functionality, depends on the reagents employed, the experimental con