598-52-7Relevant academic research and scientific papers
Liquid chromatographic determination of noxytiolin and 1-methyl-2-thiourea in serum: Application to pharmacokinetic studies in rabbits and humans
Debruyne,Moulin,Bricard,Bigot
, p. 224 - 226 (1985)
A high-performance liquid chromatographic method is described which determines noxytiolin and 1-methyl-2-thiourea concentrations in serum. Valid determination requires immediate ultracentrifugation of blood samples, rapid serum freezing, and injection into the chromatograph within 6 h. A number of pharmacokinetic parameters were calculated from serum concentration data in rabbits and humans. An unknown metabolite was detected in both species but its structure was not identified.
Pyrimidone compound and application thereof
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Paragraph 0888-0891, (2019/07/08)
The invention discloses a pyrimidone compound, pharmaceutically acceptable salt and solvate thereof, and provides a method for preparing the compounds, a composition containing the compounds and medicinal application of the compounds in preparation of medicines for treating diseases or disorders related to EED protein and/or PRC2 protein complex action mechanisms.
CuBr2 mediated synthesis of 2-Aminothiazoles from dithiocarbamic acid salts and ketones
Zhang, Baohua,Shi, Lanxiang
, p. 1134 - 1139 (2019/07/15)
In a one-pot procedure, CuBr2 has been used as a efficient desulfurizing agent in the synthesis of 2-aminothiazoles by the condensation of in situ-generated 1-substituted thioureas from their dithiocarbamic acid salts, with in situ-generated α-bromoketones from ketones. All reactions were carried out under optimized reaction conditions and gave the target products in 61–95% yield.
Methyl thiosemicarbazide synthesis process
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Paragraph 0013; 0014; 0015; 0016; 0017; 0018; 0019; 0020, (2017/08/25)
The invention discloses a methylthiosemicarbazide synthesis process comprising the following steps: thiourea is dissolved in a solvent; a catalyst is added, and the temperature is increased to 10-200 DEG C under stirring; methyl chloride gas is delivered and a reaction is allowed; when the reaction is finished, nitrogen gas is delivered for purging residual hydrogen chloride gas; hydrazine hydrate is dropped in under a temperature of 30-90 DEG C, and a reaction is carried out; when the reaction is finished, the solvent is distillated; the temperature is reduced to -10 DEG C to 50 DEG C, and a solid material is obtained by filtration; and drying is carried out, such that methylthiosemicarbazide is obtained.
Design, synthesis and biological evaluation of novel HSP70 inhibitors: N, N′-disubstituted thiourea derivatives
Zeng, Yan-Qun,Cao, Rui-Yuan,Yang, Jian-Ling,Li, Xing-Zhou,Li, Song,Zhong, Wu
, p. 83 - 95 (2016/05/24)
As novel heat shock protein 70 (HSP70) inhibitors, N, N′-disubstituted thiourea derivatives were designed and synthesized based on the X-ray structure of the ATPase domain (nucleotide binding domain, NBD). An ATPase activity inhibition assay revealed that these compounds effectively inhibited HSP70 ATPase activity. The results revealed that the compounds 370/371/374/379/380//392/394/397/404/405 and 407 can inhibit the HSP70 ATPase turnover with high percentages of inhibition: 50.42, 38.46, 50.45, 44.12, 47.13, 50.50, 40.95, 65.36, 46.23, 35.78, and 58.37 in 200 μM, respectively. Significant synergies with lapatinib were observed for compound 379 and compound 405 in the BT474 breast cancer cell line. A structure-function analysis revealed that most of the thiourea derivatives exhibited cooperative action with lapatinib in the BT474 cancer cell line and the BT/LapR1.0 lapatinib-resistant cell line. HSP70 inhibitors may be developed as synergetic drugs in drug-resistant cancer therapy.
Synthesis and evaluation of compounds that induce readthrough of premature termination codons
Jung, Michael E.,Ku, Jin-Mo,Du, Liutao,Hu, Hailiang,Gatti, Richard A.
scheme or table, p. 5842 - 5848 (2011/10/18)
A structure-activity relationship (SAR) study was carried out to identify novel, small molecular weight compounds which induce readthrough of premature termination codons. In particular, analogs of RTC13, 1, were evaluated. In addition, hypothesizing that these compounds exhibit their activity by binding to the ribosome, we prepared the hybrid analogs 13 containing pyrimidine bases and these also showed good readthrough activity.
Bismuth chloride mediated synthesis, antimicrobial, and anti-inflammatory activities of new 4-aryl-2-amino thiazoles
Giridhar,Reddy, R. Buchi,Kumar, A. Sunil,Chandra Mouli
scheme or table, p. 2058 - 2072 (2009/07/18)
Synthesis of 4-aryl-2-Amino thiazoles (3a-u), (4a-c), and (5a-c) was achieved from the reaction of 4-butyl phenacyl chlorides (2a-c) with N-substituted thioureas, in the presence of Bismuth Chloride. The antimicrobial and anti-inflammatory activities of the final products were also studied. Copyright Taylor & Francis Group, LLC.
Hydrolysis of N- and S-monomethyl derivatives of 2-thiophenobarbital
Tarsa, Monika,Zuchowski, Grzegorz,Bojarski, Jacek
, p. 247 - 252 (2007/10/03)
Kinetics of hydrolysis of S-methyl-2-thiophenobarbital in aqueous solutions was investigated using the UV spectroscopic method within the pH range 1.5-12.9 at 60°C. Chromatography was used to separate and isolate the products of hydrolysis of this compound and its N-methyl isomer. The products were identified by spectroscopic methods and the course of hydrolysis of both isomers were compared.
Methods for the solid phase synthesis of 2-amino-4(H)-quinazolinone derivatives
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, (2008/06/13)
The present invention relates to solid phase synthesis of substituted 2-amino-4(H)-quinazolinone compounds of formula (I): having pharmacological activity, to processes for their preparation, to a combinatorial library and solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, and to pharmaceutical compositions thereof.
6-amino-2,4-dioxo-3,4-dihydro-1,3,5-triazine derivatives and methods for the solid phase synthesis thereof
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, (2008/06/13)
The present invention relates to substituted 6-amino-2,4-dioxo-3,4-dihydro-1,3,5-triazine compounds of formula (I) having pharmacological activity, to solid phase synthesis methods for their preparation, to combinatorial libraries thereof, utilizing libraries of the compounds for drug discovery, and to pharmaceutical compositions thereof.
