37556-14-2Relevant academic research and scientific papers
Design, synthesis and in vivo evaluation of sodium 2-benzyl-chloromalonates as new central nervous system depressants
Vieira, Andreia Aguiar,Marinho, Bruno Guimar?es,De Souza, Luana Gon?alves,Fernandes, Patricia Dias,Figueroa-Villar, José D.
, p. 1427 - 1437 (2015/08/18)
This work describes the design, synthesis and in vivo evaluation of new central nervous system depressing agents that show low levels of acute toxicity as well as high solubility in water and exhibit anxiolytic and hypnotic effects. These new compounds are sodium 2-benzyl-2-chloromalonates, which were designed using molecular modelling techniques and synthesized in four steps, with an overall yield between 41% and 65%. In vivo tests with mice, including pentobarbital-induced sleep, rotarod, open field and elevated plus maze tests, were carried out, and the results indicated that some of these agents induce activities similar to those induced by diazepam but with lower hypnotic potency and greater anxiolytic potency. These compounds were also orally administered to mice in doses of 2 g kg-1, and their effects were evaluated for 14 days. The mice did not show signs of intoxication, confirming that sodium 2-benzyl-2-chloromalonates exhibit low levels of acute toxicity. These observations indicate that sodium 2-benzyl-2-chloromalonates and their analogues are efficient and safer central nervous system depressing drugs relative to existing standards of care.
N-HYDROXYLAMINO-BARBITURIC ACID DERIVATIVES AS NITROXYL DONORS
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, (2015/12/17)
The present disclosure provides N-hydroxylamino-barbituric acid compounds of formulae (1)- (4), pharmaceutical compositions and kits comprising them, and methods of using such compounds or pharmaceutical compositions. The present disclosure provides methods of using such compounds or pharmaceutical compositions for treating heart failure.
Synthesis of novel bis(pyrimido[5,4-c]quinoline-2,4(1H,3H)-dione) and its derivatives: Evaluation of their antioxidant properties
Parameswaran, Kandasamy,Sivaguru, Paramasivam,Lalitha, Appaswami
, p. 3873 - 3878 (2013/07/27)
One pot cyclocondensation reaction of barbituric/thiobarbituric acid with aromatic aldehydes and p-phenylenediamine/2,6-diaminopyridine by refluxing in glacial acetic acid afforded novel bis(pyrimido[5,4-c]quinoline-2,4(1H,3H)- diones)/pyrido bis(pyrimido
Synthesis and in vivo evaluation of 5-chloro-5-benzobarbiturates as new central nervous system depressants
Vieira, Andreia A.,Gomes, Niele M.,Matheus, Maria E.,Fernandes, Patricia D.,Figueroa-Villar, Jose? D.
experimental part, p. 364 - 371 (2011/10/01)
A new family of barbiturates, 5-chloro-5-benzylbarbituric acids, was prepared using a simple efficient synthetic method from aromatic aldehydes and barbituric acid, followed by reduction and chlorination with trichloro-isocyanuric acid, affording overall yields of 53 to 70percent. The in vivo evaluation with mice showed that these compounds present tranquilizing activity.
Synthesis and antimicrobial activities of novel 5-substituted pyrimidin-2,4,6-triones
Goudgaon,Patil,Rahaman,Upendar Reddy
experimental part, p. 743 - 748 (2011/08/09)
5-Benzylpyrimidin-2,4,6-triones (3a-c), 5-((furan-2-yl)methyl)pyrimidin-2, 4,6-trione (3g) and 5-((3-aryl-1-phe-nyl-1H-pyrazol-4-yl)methyl)pyrimidin-2,4,6- triones (3h-j) were obtained in two steps. Reaction of barbituric acid (1) with various substituted aromatic aldehydes, furfuraldehyde and 3-aryl-1-phenyl-1H- pyrazole-4-carbaldehydes in methanol yielded the corresponding chalcones 2a-m in 48-85% yield. These chalcones on reduction with sodium borohydride in isopropyl alcohol furnished desired novel compounds 3a-c and 3g-j in 55-85% yield. The structure of all the synthesized compounds have been established by various spectral studies and elemental analysis. All the synthesized compounds have been screened for antimicrobial activity.
Modified pyrimidine glucocorticoid receptor modulators
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Page/Page column 17, (2008/06/13)
The present invention provides a novel class of modified pyrimidine compounds and compositions and methods of using the compounds as glucocorticoid receptor modulators.
