13249-01-9Relevant academic research and scientific papers
Synthesis and anticancer evaluation of novel triazole linked N-(pyrimidin-2-yl)benzo[d]thiazol-2-amine derivatives as inhibitors of cell survival proteins and inducers of apoptosis in MCF-7 breast cancer cells
Kumbhare, Ravindra M.,Dadmal, Tulshiram L.,Ramaiah, M. Janaki,Kishore,Pushpa Valli,Tiwari, Sudheer Kumar,Appalanaidu,Rao, Y. Khageswar,Bhadra, Manika Pal
, p. 654 - 658 (2015)
A series of novel triazole linked N-(pyrimidin-2yl)benzo[d]thiazol-2-amine 5a-k were synthesized and evaluated for anticancer activity against breast (MCF-7), lung (A549) and skin (A375) cancer cell lines and their cytotoxic effects were compared against
Palladium(II) and platinum(II) complexes of N-phenyl- and N-ethyl-N′-pyrimidin-2-ylthiourea
Kandil, Samir S.
, p. 2455 - 2463 (2010)
Palladium(II) and platinum(II) complexes of N-ethyl-N′-pyrimidin-2- ylthiourea(HL1) and N-phenyl-N′-pyrimidin-2-ylthiourea (HL2) have been prepared, and the complexes [M(HL)Cl2], [Pt(L)2], [Pd(HL1)2]Cl2, and [Pd(L2)2] (where M = PdII or PtII) were charact
Diversity-Oriented Synthesis of Thiazolidine-2-imines via Microwave-Assisted One-Pot, Telescopic Approach and Its Interaction with Biomacromolecules
Saikia, Ananya Anubhav,Rao, Ramdas Nishanth,Maiti, Barnali,Balamurali, Musuvathi Motilal,Chanda, Kaushik
, p. 630 - 640 (2020/12/15)
In this work, a one-pot, telescopic approach is described for the combinatorial library of thiazolidine-2-imines. The synthetic manipulation proceeds smoothly via the reaction of 2-aminopyridine/pyrazine/pyrimidine with substituted isothiocyanates followed by base catalyzed ring closure with 1,2-dibromoethane to obtain thiazolidine-2-imines with broad substrate scope and high functional group tolerance. The synthetic strategy merges well with the thiourea formation followed by base catalyzed ring closure reaction for the thiazolidine-2-imine synthesis in a more modular and straightforward approach. The synthetic procedure reported herein represents a cleaner route toward thiazolidine-2-imines as compared to traditional methodologies. Moreover, the biological significance of combinatorially synthesized thiazolidin-2-imines has been investigated for their use as possible inhibitors for acetyl cholinesterase through molecular docking studies.
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.
Synthesis and antiviral activity of some (3,4-diaryl-3H-thiazol-2-ylidene) pyrimidin-2-yl amine derivatives
Turan-Zitouni, Guelhan,Oezdemir, Ahmet,Kaplancikli, Zafer Asim
experimental part, p. 233 - 239 (2011/04/26)
Chemical Equation Presented Thirteen new (3,4-diaryl-3H-thiazol-2-ylidene) pyrimidin-2-yl amine derivatives were synthesized by reacting 1-aryl-3-pyrimidin-2-yl-thiourea derivatives and phenacyl bromides in absolute ethanol. The solid that separated was f
Hydrogen-bonding networks in heterocyclic thioureas
Saxena, Aakarsh,Pike, Robert D.
, p. 755 - 764 (2008/09/17)
The synthesis of heterocyclic thioureas from heterocyclic amines with phenyl- or methylisothiocyanate or CS2 is described. Seven new X-ray crystal structures are reported: In N-(3-pyridyl)-N'-phenylthiourea (Pna2 1, a = 10.1453(3), b
High-pressure-promoted condensation of isothiocyanates with aminopyridines: Efficient synthesis of pyridine-thiourea conjugates as building blocks for hydrogen-bonding receptors
Kumamoto, Koji,Misawa, Yoshihiro,Tokita, Sumio,Kubo, Yuji,Kotsuki, Hiyoshizo
, p. 1035 - 1038 (2007/10/03)
New N-pyridinothiourea derivatives have been prepared by the high-pressure-promoted condensation of isothiocyanates with aminopyridines under uncatalyzed conditions. Complexation of the prototype 3c with diphenyl hydrogen phosphate was investigated by 1H NMR, and the results suggest that it may be useful as a building block for hydrogen-bonding receptors.
CHARGE-TRANSFER COMPLEXES OF SOME HETEROARYLTHIOUREA DERIVATIVES WITH ?-ACCEPTORS
Hamed, M. M. A.,Salman, H. M. A.,Abd-Alla, E. M.,Mahmoud, M. R.
, p. 127 - 134 (2007/10/02)
Spectral charcteristics and thermodynamic properties of charge-transfer molecular complexes of some heteroarylthioureas with ?-acceptors DDQ, TCNE and CHL are investigated and discussed.It is deduced that the formed CT complexes are of n-? kind.Moreover, 1:1 solid CT complexes are synthesized and characterized.Keywords: Charge-transfer complexes; solvent effects, stability; solid CT complex; heteroarylthioureas.
CHARGE-TRANSFER COMPLEXES OF SOME HETEROARYLTHIOUREA DERIVATIVES WITH ?-ACCEPTORS
Hamed, Maher M. A.,Salman, Hassan M. A.,Abd-Alla, Elham M.,Mahmoud, Mohamed R.
, p. 2846 - 2852 (2007/10/02)
Charge-transfer complexes of some heteroarylthiourea derivatives with ?-acceptors have been studied spectrophotometrically in CH2Cl2.Spectral data, stability constants and enthalpies of complexation are reported.From the enrgies of the CT transition, ionization potentials of the donors have been obtained.Effects of donor molecular structure, ?-acceptor electron affinity and nature of solvent on KCT of complexes are investigated and discussed.It is deduced that the formed CT complexes are of n-? kind and of 1:1 stoichiometry.
Interactions between substituted thioureas and π-acceptors
Mohamed,Hassan,Ibrahim,Semida,Mourad
, p. 592 - 595 (2007/10/02)
Charge-transfer (CT) interactions between some N-aryl-N'-heterocyclic thioureas and both tetracyanoethylene (TCNE) and 2,3-dichloro-5,6-dicyanobenzoquinone (DDQ) were investigated spectroscopically. The formed CT complexes and the solvent effect on CT complexation are discussed. N-Aryl-N'-(2-pyridyl)-thioureas 1 a-d reacted with TCNE to give cyanothiourea derivatives 6, however in case of DDQ, the adducts 7 were obtained.
