14294-11-2Relevant academic research and scientific papers
Gravimetric, electrochemical and surface studies on the anticorrosive properties of 1-(2-pyridyl)-2-thiourea and 2-(imidazol-2-yl)-pyridine for mild steel in hydrochloric acid
Zhang, Weiwei,Li, Hui-Jing,Wang, Yiwei,Liu, Ying,Gu, Qing-Ze,Wu, Yan-Chao
, p. 12649 - 12665 (2018)
1-(2-Pyridyl)-2-thiourea (TP) and 2-(imidazol-2-yl)-pyridine (IP) are described here for the first time as inhibitors of mild steel corrosion in acidic medium based on investigations such as weight loss tests, potentiodynamic polarization measurements and
SO2F2-Mediated N-Alkylation of Imino-Thiazolidinones
Santos, Laura,Donnard, Morgan,Panossian, Armen,Vors, Jean-Pierre,Jeschke, Peter,Bernier, David,Pazenok, Sergii,Leroux, Frédéric R.
, p. 2012 - 2021 (2021/09/02)
The N-alkylation of ambident and weakly nucleophilic imino-thiazolidinones has been developed via substitution with alkyl fluorosulfonates. These reactive electrophiles are obtained through the transformation of nontoxic, economic, and commercially availa
COMPOUNDS AND METHODS FOR MODULATING INTERLEUKIN-2-INDUCIBLE T-CELL KINASE
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Paragraph 0893; 0896; 0897, (2018/05/27)
Provided herein, inter alia, are methods and compounds for modulating Interleukin-2-inducible T-cell kinase.
Synthesis and antitumor evaluation of 5-(benzo[: D] [1,3]dioxol-5-ylmethyl)-4-(tert -butyl)- N -arylthiazol-2-amines
Wu,Fang,Tang,Xiao,Ye,Li,Hu
, p. 1768 - 1774 (2016/09/28)
A series of novel N-aryl-5-(benzo[d][1,3]dioxol-5-ylmethyl)-4-(tert-butyl)thiazol-2-amines (C1-C31) were synthesized and evaluated for their antitumor activities against HeLa, A549 and MCF-7 cell lines. Some tested compounds showed potent growth inhibition properties with IC50 values generally below 5 μM against the three human cancer cells lines. Compound C27 showed potent activities against HeLa and A549 cell lines with IC50 values of 2.07 ± 0.88 μM and 3.52 ± 0.49 μM, respectively. Compound C7 (IC50 = 2.06 ± 0.09 μM) was the most active compound against A549 cell line, while compound C16 (IC50 = 2.55 ± 0.34 μM) showed the best inhibitory activity against the MCF-7 cell line. The preliminary mechanism of the inhibitory effect was investigated via further experiments, such as morphological analysis by dual AO/EB staining and Hoechst 33342 staining, and cell apoptosis and cycle assessment by FACS analysis. The results illustrated that compound C27 could induce apoptosis and cause both S-phase and G2/M-phase arrests in HeLa cell line. Therefore, compound C27 could be developed as a potential antitumor agent.
COMPOUNDS AND METHODS FOR INDUCING BROWNING OF WHITE ADIPOSE TISSUE
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Page/Page column 15, (2016/09/15)
The present invention provides a compound for inducing browning of white adipose tissue in vitro and in vivo of formula I, the preparation method thereof, as well as a composition comprising the same. Further, the present invention also relates to the use of the compound and the method to treat metabolic disorders, such as obesity and diabetes.
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.
NOVEL ANTIPRION COMPOUNDS
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Paragraph 0648; 0649; 0708, (2013/03/28)
Described herein are novel compositions and methods of treatment addressing diseases such as neurodegenerative diseases, including prion diseases and Alzheimer's disease.
Structure-activity relationships of 2-aminothiazoles effective against Mycobacterium tuberculosis
Meissner, Anja,Boshoff, Helena I.,Vasan, Mahalakshmi,Duckworth, Benjamin P.,Barry III, Clifton E.,Aldrich, Courtney C.
, p. 6385 - 6397 (2013/10/22)
A series of 2-aminothiazoles was synthesized based on a HTS scaffold from a whole-cell screen against Mycobacterium tuberculosis (Mtb). The SAR shows the central thiazole moiety and the 2-pyridyl moiety at C-4 of the thiazole are intolerant to modification. However, the N-2 position of the aminothiazole exhibits high flexibility and we successfully improved the antitubercular activity of the initial hit by more than 128-fold through introduction of substituted benzoyl groups at this position. N-(3-Chlorobenzoyl)-4-(2-pyridinyl) -1,3-thiazol-2-amine (55) emerged as one of the most promising analogues with a MIC of 0.024 μM or 0.008 μg/mL in 7H9 media and therapeutic index of nearly ~300. However, 55 is rapidly metabolized by human liver microsomes (t1/2 = 28 min) with metabolism occurring at the invariant aminothiazole moiety and Mtb develops spontaneous low-level resistance with a frequency of ~10-5.
Dental material with color indicator and metods of using same
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, (2012/05/20)
A dental material is provided that exhibits a color change upon or after mixing or contacting components of the composition. The composition includes an acidic component in one part, and a basic component in another part that upon contact with the acidic component initiates a chemical reaction thereof that alters the pH of the composition. An acid or base sensitive color change agent is present in the composition that registers the change in pH by changing color as the pH changes.
2-aminothiazoles as therapeutic leads for prion diseases
Gallardo-Godoy, Alejandra,Gever, Joel,Fife, Kimberly L.,Silber, B. Michael,Prusiner, Stanley B.,Renslo, Adam R.
experimental part, p. 1010 - 1021 (2011/04/25)
2-Aminothiazoles are a new class of small molecules with antiprion activity in prion-infected neuroblastoma cell lines (J. Virol. 2010, 84, 3408). We report here structure-activity studies undertaken to improve the potency and physiochemical properties of 2-aminothiazoles, with a particular emphasis on achieving and sustaining high drug concentrations in the brain. The results of this effort include the generation of informative structure-activity relationships (SAR) and the identification of lead compounds that are orally absorbed and achieve high brain concentrations in animals. The new aminothiazole analogue (5-methylpyridin-2-yl)-[4-(3-phenylisoxazol-5-yl)-thiazol-2-yl]-amine (27), for example, exhibited an EC50 of 0.94 μM in prion-infected neuroblastoma cells (ScN2a-cl3) and reached a concentration of ~25 μM in the brains of mice following three days of oral administration in a rodent liquid diet. The studies described herein suggest 2-aminothiazoles as promising new leads in the search for effective therapeutics for prion diseases.
