Thiocyanate and Isothiourea Derivatives of Barbituric Acid

1952 ◽  
Vol 74 (2) ◽  
pp. 498-499 ◽  
Author(s):  
Glenn S. Skinner ◽  
William H. Waitz
Keyword(s):  
Barbituric Acid ◽  
Isothiourea Derivatives ◽  
Derivatives Of

Two polymorphs and the diethylammonium salt of the barbiturate eldoral

2012 ◽  
Vol 68 (2) ◽  
pp. o65-o70 ◽  
Author(s):  
Thomas Gelbrich ◽  
Denise Rossi ◽  
Ulrich J. Griesser
Keyword(s):  
Hydrogen Bond ◽  
Hydrogen Bonds ◽  
Barbituric Acid ◽  
Layer Structure ◽  
Chain Structure ◽  
Hydrogen Bond Acceptor ◽  
Layer Structures ◽  
A Chain ◽  
Derivatives Of ◽  
Hydrogen Bonded

Polymorph (Ia) of eldoral [5-ethyl-5-(piperidin-1-yl)barbituric acid or 5-ethyl-5-(piperidin-1-yl)-1,3-diazinane-2,4,6-trione], C11H17N3O3, displays a hydrogen-bonded layer structure parallel to (100). The piperidine N atom and the barbiturate carbonyl group in the 2-position are utilized in N—H...N and N—H...O=C hydrogen bonds, respectively. The structure of polymorph (Ib) contains pseudosymmetry elements. The two independent molecules of (Ib) are connectedviaN—H...O=C(4/6-position) and N—H...N(piperidine) hydrogen bonds to give a chain structure in the [100] direction. The hydrogen-bonded layers, parallel to (010), formed in the salt diethylammonium 5-ethyl-5-(piperidin-1-yl)barbiturate [or diethylammonium 5-ethyl-2,4,6-trioxo-5-(piperidin-1-yl)-1,3-diazinan-1-ide], C4H12N+·C11H16N3O3−, (II), closely resemble the corresponding hydrogen-bonded structure in polymorph (Ia). Like many other 5,5-disubstituted derivatives of barbituric acid, polymorphs (Ia) and (Ib) contain theR22(8) N—H...O=C hydrogen-bond motif. However, the overall hydrogen-bonded chain and layer structures of (Ia) and (Ib) are unique because of the involvement of the hydrogen-bond acceptor function in the piperidine group.

scholarly journals SOME NEW DERIVATIVES OF BARBITURIC ACID

1925 ◽  
Vol 47 (4) ◽  
pp. 1124-1127 ◽  
Author(s):  
Vanderveer Voorhees ◽  
Glenn S. Skinner
Keyword(s):  
Barbituric Acid ◽  
Derivatives Of

Thermal and 1H NMR studies on some azo derivatives of barbituric acid

1991 ◽  
Vol 189 (1) ◽  
pp. 83-89 ◽  
Author(s):  
Ramesh Chandra ◽  
Narendra N. Ghosh
Keyword(s):  
1H Nmr ◽  
Barbituric Acid ◽  
Nmr Studies ◽  
Azo Derivatives ◽  
Derivatives Of

Imidazole Derivatives of Barbituric Acid

1933 ◽  
Vol 55 (3) ◽  
pp. 1110-1111
Author(s):  
Millard S. Taggart ◽  
G. Holmes Richter
Keyword(s):  
Barbituric Acid ◽  
Imidazole Derivatives ◽  
Derivatives Of

scholarly journals Influence of the type of salt-forming acids on the antiradiation activity of T1023 analogs – salts of N-isobutanoyl-S-isopropylisothiourea

2021 ◽  
Vol 14 (1) ◽  
pp. 68-74
Author(s):  
M. V. Filimonova ◽  
A. S. Saburova ◽  
L. I. Shevchenko ◽  
V. M. Makarchuk ◽  
A. A. Lychagin ◽  
...  
Keyword(s):  
Chemical Synthesis ◽  
Initial Compound ◽  
Radioprotective Activity ◽  
Nos Inhibitors ◽  
Isothiourea Derivatives ◽  
Antiradiation Activity ◽  
Nos Inhibitor ◽  
New Compounds ◽  
Further Development ◽  
Derivatives Of

According to leading experts, the vast arsenal of radioprotective agents available in the world today does not fully meet modern practical needs, both in the field of radiation protection, and in the prevention and treatment of complications of radiotherapy. The purpose of the study was to evaluate the effect of the salt-forming acids type on the radioprotective activity of NOS inhibitor T1023. The chemical part of this study included methods of chemical synthesis, physicochemical and elemental analysis. Pharmacological part – assessment of acute toxicity using V.B. Prozorovsky express method and the study of radioprotective activity using Till and McCulloch method based on the ability of mice hematopoietic cells to form spleen colonies after irradiation. The number of endogenous hematopoietic spleen colonies were assessed on the 8th day after total exposure to gamma-irradiation at a dose of 6 Gy in six independent experiments. As a result of directed chemical synthesis, six new derivatives of T1023 – salts of N-isobutanoyl-S-isopropylisothiourea have been developed, identified and characterized. The results of studying the safety and radioprotective activity of the synthesized compounds showed that changes in the salt-forming acid don’t significantly influence the toxicity: all studied compounds are in the 3rd class of toxicity and hazard. At the same time, it was found that the replacement of the salt-forming acid significantly influenced the severity of the radioprotective effect. For some of these compounds radioprotective efficacy is comparable to or exceeds the efficacy of the initial compound T1023. It is important to note that these new compounds were used in lower, more save doses than T1023. The results suggest promising further development of NOS inhibitors – isothiourea derivatives as radioprotective agents.

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