5909-45-5Relevant academic research and scientific papers
BARBITURIC ACID DERIVATIVES AS SELF-TANNING SUBSTANCES
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Paragraph 0226-0227, (2020/02/20)
The present invention relates to the use of barbituric acid derivatives of the formula I as self-tanning substance, for increasing melanin synthesis, for improving melanin transport and/or improving the distribution of melanin in superbasal layers, to preparations comprising these barbituric acid derivatives, and to specific barbituric acid derivatives.
2-Phenyl-2,3-dihydrobenzo[ d ]thiazole: A Mild, Efficient, and Highly Active in situ Generated Chemoselective Reducing Agent for the One-Pot Synthesis of 5-Monoalkylbarbiturates in Water
Kalita, Subarna Jyoti,Deka, Dibakar Chandra
, p. 477 - 482 (2017/12/06)
A metal- and catalyst-free reductive alkylation protocol for the one-pot synthesis of 5-monoalkylbarbiturates from barbituric acids and aldehydes using the in situ generated chemoselective reducing agent 2-phenyl-2,3-dihydrobenzo[ d ]thiazole from 2-aminothiophenol and benzaldehyde is described. The notable advantages of the protocol are operational simplicity, mild reaction conditions, high yield, short reaction time, and simple workup and purification process which make it highly attractive.
Ruthenium-catalyzed selective synthesis of monoalkylated barbituric acids through “borrowing hydrogen” methodology
Putra, Anggi Eka,Oe, Yohei,Ohta, Tetsuo
supporting information, p. 1098 - 1101 (2017/03/02)
An environmentally benign alkylation of barbituric acids via “borrowing hydrogen” process with ruthenium catalysis has been established. The corresponding 5-(alkyl)barubituric acids were obtained in good to excellent yields with low catalyst loading. Vari
Pd/C-catalyzed alkylation of heterocyclic nucleophiles with alcohols through the "borrowing hydrogen" process
Putra, Anggi Eka,Oe, Yohei,Ohta, Tetsuo
, p. 7799 - 7805 (2015/12/31)
The alkylation of heterocyclic compounds is important for the synthesis of various biologically active compounds. In this paper, we present the development of a Pd/C-catalyzed alkylation of heterocyclic compounds using alcohols as the alkylating agents. T
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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Page/Page column 142-145, (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.
Nuclear magnetic resonance and molecular modeling study of exocyclic carbon-carbon double bond polarization in benzylidene barbiturates
Figueroa-Villar, J. Daniel,Vieira, Andreia A.
, p. 310 - 317 (2013/03/13)
Benzylidene barbiturates are important materials for the synthesis of heterocyclic compounds with potential for the development of new drugs. The reactivity of benzylidene barbiturates is mainly controlled by their exocyclic carbon-carbon double bond. In this work, the exocyclic double bond polarization was estimated experimentally by NMR and correlated with the Hammett σ values of the aromatic ring substituents and the molecular modeling calculated atomic charge difference. It is demonstrated that carbon chemical shift differences and NBO charge differences can be used to predict their reactivity.
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.
Exploring new inhibitors of Plasmodium falciparum purine nucleoside phosphorylase
Cui, Huaqing,Ruda, Gian Filippo,Carrero-Lérida, Juana,Ruiz-Pérez, Luis M.,Gilbert, Ian H.,González-Pacanowska, Dolores
experimental part, p. 5140 - 5149 (2010/11/19)
Plasmodium falciparum purine nucleoside phosphorylase (PfPNP) has a central role in purine salvage and inhibitors of the enzyme have been shown to have antiplasmodial activity. The enzyme preferentially uses inosine as substrate (Km = 5 μM, ks
Multi-catalysis cascade reactions based on the methoxycarbonylketene platform: Diversity-oriented synthesis of functionalized non-symmetrical malonates for agrochemicals and pharmaceuticals
Ramachary, Dhevalapally B.,Venkaiah, Chintalapudi,Reddy, Y. Vijayendar,Kishor, Mamillapalli
scheme or table, p. 2053 - 2062 (2009/09/05)
In this paper we describe new multi-catalysis cascade (MCC) reactions for the one-pot synthesis of highly functionalized non-symmetrical malonates. These metal-free reactions are either five-step (olefination/hydrogenation/alkylation/ ketenization/esterif
