2741-06-2Relevant academic research and scientific papers
Synthesis, spectral, thermal and structural characterization of a hexanuclear copper(I) cluster and a cobalt(III) complex of 1-ethyl-3-phenyl-thiourea
Singh,Bharty,Bharati,Bharti,Singh, Sanjay,Singh
, p. 918 - 925 (2015)
1-Ethyl-3-phenyl-thiourea (Heptu, 1) forms a hexanuclear complex, [Cu6(eptu)6] (2), and a mononuclear complex, [Co(eptu)3] (3), which have been characterized with the aid of elemental analyses, IR, magnetic susceptibility
Square planar Pd(II) complexes derived from 1-ethyl-3-phenylthiourea, 3-mercapto-4-methyl-1,2,4-triazole and 2-mercapto-5-methyl-1,3,4-thiadiazole: Syntheses, spectral, structural characterization and photoluminescence properties
Bharati,Bharti,Nath,Kumari,Singh,Bharty
, p. 160 - 169 (2016)
The reaction of PdCl2 with 1-ethyl-3-phenyl-thiourea (Heptu), 3-mercapto-4-methyl-4H-1,2,4-triazole (Hmmtrz) and 2-mercapto-5-methyl-1,3,4-thiadiazole (Hmthd) respectively, yielded three new complexes [Pd(eptu)2] (1), [Pd(Hmmtrz)sub
Antileishmanial thioureas: Synthesis, biological activity and in Silico evaluations of new promising derivatives
Viana, Gil Mendes,Do Amaral, Lilian Henriques,Meireles, Paloma Wetler,Nunes, Raquel Pinto,Da Silva, Luiz Cláudio Rodrigues Pereira,De Sousa, Valeria Pereira,Sathler, Plínio Cunha,Cabral, Lucio Mendes,Soares, Deivid Costa,Saraiva, Elvira Maria,Santana, Marcos Vinicius,Castro, Helena Carla,De Sequeira Aguiar, Lúcia Cruz,Rodrigues, Carlos Rangel,Abreu, Paula Alvarez
, p. 911 - 919 (2018/10/31)
Leishmaniasis is a neglected tropical disease caused by protozoan parasites belonging to the genus Leishmania. Currently, the drugs available for treatment of this disease present high toxicity, along with development of parasite resistance. In order to overcome these problems, efforts have been made to search for new and more effective leishmanicidal drugs. The aim of this study was to synthesize and investigate the leishmanicidal effect of N,N′-disubstituted thioureas against Leishmania amazonensis, with evaluation of their in silico pharmacokinetics and toxicity profiles. Our results showed that different thioureas could be obtained in high to moderate yields using simple reaction conditions. Nine thiourea derivatives (3e, 3i, 3k, 3l, 3p, 3q, 3v, 3x and 3z) were active against parasite promastigotes (IC50 21.48–189.10μM), with low cytotoxicity on mice peritoneal macrophages (CC50>200μM), except for thiourea 3e (CC50=49.22μM). After that, the most promising thioureas (3k, 3l, 3p, 3q and 3v) showed IC50 ranging from 70 to 150μM against L. amazonensis amastigotes in infected macrophages. Except for thiourea 3p, the leishmanicidal activity of the derivatives were independent of nitric oxide (NO) production. Thioureas 3q and 3v affected promastigotes cell cycle without disturbing the mitochondrial membrane potential. Furthermore, our derivatives showed satisfactory theoretical absorption, distribution, metabolism, excretion, toxicity (ADMET) properties. These data indicate that thiourea derivatives are good candidates as leading compounds for the development of new leishmanicidal drugs.
Anion transport across varying lipid membranes - The effect of lipophilicity
Spooner, Michael J.,Gale, Philip A.
supporting information, p. 4883 - 4886 (2015/03/18)
The anion transport properties of a range of alkyl-substituted phenylthioureas were tested in vesicles of different lipid composition. Although changes in the bilayer affected the rate of transport for all compounds in the series, the 'ideal' log P for pe
Synthesis of thiazolidines via regioselective addition of unsymmetric thioureas to maleic acid derivatives
Pankova, Alena S.,Samartsev, Mikhail A.,Shulgin, Igor A.,Golubev, Pavel R.,Avdontceva, Margarita S.,Kuznetsov, Mikhail A.
, p. 51780 - 51786 (2014/12/10)
A wide range of unsymmetric thioureas has been studied in reaction with N-arylmaleimides and maleic anhydride. The regioselectivity of the addition depends not only on steric factors but on both solvent polarity and type of maleic acid derivative (imide o
A comparative study of glycosyl thioimidates as building blocks for chemical glycosylation
Ranade, Sneha C.,Hasty, Scott J.,Demchenko, Alexei V.
, p. 360 - 379 (2013/10/08)
Our results indicate that the reactivity and the activation profile of thioimidate glycosyl donors vary significantly depending on the endocyclic heteroatom (N,O,S). Reactivity diminishes in accordance with the following sequence: O > S > N; and this tren
Microwave-assisted synthesis of symmetrical and unsymmetrical N,N 0-disubstituted thioureas and ureas over MgO in dry media
Valizadeh, Hassan,Dinparast, Leila
experimental part, p. 251 - 254 (2012/07/01)
Under mild microwave irradiation conditions a variety of symmetrical and unsymmetrical A,N′-disubsti-tuted thioureas and ureas were prepared via the reaction of Af-monosubstituted hydroxylamines with isocyanate and isothiocyanate derivatives over MgO under solvent-free conditions. This new method afforded satisfactory results with good yields, short reaction time, and simplicity in the experimental procedure.
COMPOUNDS AND METHODS FOR MODULATING G PROTEIN-COUPLED RECEPTORS
-
Page/Page column 48, (2010/04/03)
The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with or mediated by G protein-coupled receptors, in particular G protein-coupl
COMPOUNDS WHICH POTENTIATE AMPA RECEPTOR AND USES THEREOF IN MEDICINE
-
Page/Page column 50, (2008/06/13)
Compounds of formula (I), and salts and solvates thereof for use as a medicament are provided: (I) wherein R1, R2, R4, R10, X and Z are defined in the specification. Processes for preparation, pharmaceutical com
