53243-34-8

Upstream product

• 6846-35-1 5-amino-3H-1,2,4-dithiazole-3-thione 
• 106-49-0 p-toluidine 
• 17356-08-0 thiourea 
• 622-59-3 1-isothiocyanato-4-methylbenzene 
• 540-23-8 p-toluidine hydrochloride 
• 622-52-6 p-methylphenylthiourea 
• 1147550-11-5 ammonium thiocyanate 
• 26724-65-2 1-p-tolyl-1H-[1,3,5]triazine-2,4-dithione 

Downstream Products

• 3929-18-8 N³-(p-tolyl)-1H-1,2,4-triazole-3,5-diamine 
• 53243-36-0 (5-amino-[1,2,4]dithiazol-3-ylidene)-p-tolyl-amine 
• 120570-21-0 4-p-tolyl-allophanonitrile 
• 92969-07-8 S-benzyl-N-cyano-N'-p-tolyl-isothiourea 
• 2982-45-8 N-p-tolyl-N'-(4-phenylthiazol-2-yl)thiourea 
• 134700-54-2 C₁₂H₁₅N₃S₂*ClH 
• 134700-55-3 C₁₃H₁₇N₃S₂*ClH 
• 80309-96-2 6-[(Z)-Phenylimino]-1-p-tolyl-1,6-dihydro-[1,3,5]triazine-2,4-dithiol 
• 13911-43-8 1-p-Tolyl-biuret 
• 134700-67-7 6-Isobutyl-6-methyl-1-p-tolyl-[1,3,5]triazinane-2,4-dithione 

Relevant academic research and scientific papers

Microwave induced improved synthesis of monoaryl thiocarbamides, 1,3-diarylthiocarbamides, 1,3-diarylcarbamides and monoaryl-2,4-dithiobiurets

The 1-arylthiocarbamides (3), 1, 3-diarylthiocarbamides (6), 1,3-diarylcarbamides (7) and 1-aryl-2,4-dithiobiurets (11) have been synthesized by the microwave induced heating of respective reactants for about 30-60 s in solvent free condition. Reaction yields are higher with reduced time, period and without the use of any solvent.

Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore

High-throughput screening for inhibitors of the human metalloprotease, methionine aminopeptidase-2 (MetAP2), identified a potent class of 3-anilino-5-benzylthio-1,2,4-triazole compounds. Efficient array and interative synthesis of triazoles led to rapid SAR development around the aniline, benzylthio, and triazole moeities. Evaluation of these analogs in a human MetAP2 enzyme assay led to the identification of several inhibitors with potencies in the 50-100 picomolar range. The deleterious effects on inhibitor potency by methylation of the anilino-triazole nitrogens, as well as the X-ray crystal structure of triazole 102 bound in the active site of MetAP2, confirm the key interactions between the triazole nitrogens, the active site cobalt atoms, and the His-231 side-chain. The structure has also provided a rationale for interpreting SAR within the triazole series. Key aniline (2-isopropylphenyl) and sulfur substituents (furanylmethyl) identified in the SAR studies led to the identification of potent inhibitors (103 and 104) of endothelial cell proliferation. Triazoles 103 and 104 also exhibited dose-dependent activity in an aortic ring tissue model of angiogenesis highlighting the potential utility of MetAP2 inhibitors as anticancer agents.