13140-69-7

Upstream product

• 462-08-8 pyridin-3-ylamine 
• 103-72-0 phenyl isothiocyanate 

Downstream Products

• 69437-86-1 2-phenylimino-3-pyridin-3-yl-thiazolidin-4-one 
• 854392-31-7 2-methyl-1-phenyl-3-pyridin-3-yl-isothiourea 
• 781566-78-7 N-phenyl-N'-(3-pyridyl)-1-pyrrolidinocarboxamidine 
• 30162-37-9 3-pyridylthiourea 
• 709000-28-2 [4-(3,4-dimethoxyphenyl)-thiazol-2-yl]-pyridin-3-yl-amine 
• 1205532-79-1 CuI(N-(3-pyridyl)-N'-phenylthiourea) 

Relevant academic research and scientific papers

Hydrogen-bonding networks in heterocyclic thioureas

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

Synthesis and in vitro urease inhibitory activity of N,N′- disubstituted thioureas

Thiourea derivatives (1-38) were synthesized and evaluated for their urease inhibition potential. The synthetic compounds showed a varying degree of in vitro urease inhibition with IC50 values 5.53 ± 0.02-91.50 ± 0.08 μM, most of which are superior to the standard thiourea (IC50 = 21.00 ± 0.11 μM). In order to ensure the mode of inhibition of these compounds, the kinetic study of the most active compounds has been carried out. Most of these inhibitors were found to be mixed-type of inhibitors, except compounds 13 and 30 which were competitive, while compound 19 was identified as non-competitive inhibitor with Ki values between 8.6 and 19.29 μM.

2-aminothiazoles as therapeutic leads for prion diseases

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.

Microwave-assisted synthesis of N,N′-diaryl cyanoguanidines

(Chemical Equation Presented) A mild, efficient, and high-yielding method for the synthesis of N,N′-diaryl cyanoguanidines from their corresponding thioureas under microwave-assisted conditions is described. A series of cyanoguanidines were synthesized containing both electron-donating and electron-withdrawing substituents. The reactions were facilitated by the use of polar solvents along with moderate temperatures.