23282-96-4

Upstream product

• 120811-69-0 2-benzoyl-N-benzylhydrazinecarbothioamide 
• 613-94-5 benzoic acid hydrazide 
• 96133-99-2 C₁₀H₁₃N₃OS 
• 100-46-9 benzylamine 
• 622-78-6 Benzyl isothiocyanate 
• 5333-86-8 ethyl benzimidate hydrochloride 

Downstream Products

• 108222-96-4 3-Phenyl-4-benzyl-4H-1,2,4-triazole 

Relevant academic research and scientific papers

Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β- d -ribofuranose 2′-Oxidase

We report herein the discovery of 3,5-dinitrophenyl 1,2,4-triazoles with excellent and selective antimycobacterial activities against Mycobacterium tuberculosis strains, including clinically isolated multidrug-resistant strains. Thorough structure-activity relationship studies of 3,5-dinitrophenyl-containing 1,2,4-triazoles and their trifluoromethyl analogues revealed the key role of the position of the 3,5-dinitrophenyl fragment in the antitubercular efficiency. Among the prepared compounds, the highest in vitro antimycobacterial activities against M. tuberculosis H37Rv and against seven clinically isolated multidrug-resistant strains of M. tuberculosis were found with S-substituted 4-alkyl-5-(3,5-dinitrophenyl)-4H-1,2,4-triazole-3-thiols and their 3-nitro-5-(trifluoromethyl)phenyl analogues. The minimum inhibitory concentrations of these compounds reached 0.03 μM, which is superior to all the current first-line anti-tuberculosis drugs. Furthermore, almost all compounds with excellent antimycobacterial activities exhibited very low in vitro cytotoxicities against two proliferating mammalian cell lines. The docking study indicated that these compounds acted as the inhibitors of decaprenylphosphoryl-β-d-ribofuranose 2′-oxidase enzyme, which was experimentally confirmed by two independent radiolabeling experiments.

Small molecule inhibitors of HIV RT Ribonuclease H

Two classes of compounds, thiocarbamates 1 and triazoles 2, have been identified as HIV RT RNase H inhibitors using a novel FRET-based HTS assay. The potent analogs in each series exhibited selectivity and were active in cell-based assays. In addition, sa

Triazole derivatives as non-nucleoside inhibitors of HIV-1 reverse transcriptase-Structure-activity relationships and crystallographic analysis

A series of 3,4,5-trisubstituted 1,2,4-4H triazole derivatives was synthesized and investigated for HIV-1 reverse transcriptase inhibition. An X-ray structure with HIV-1 RT secured the binding mode and allowed the key interactions with the enzyme to be identified.

Photochemical synthesis of triazolo[3,4-b]-1,3(4H)-benzothiazines: A detailed mechanistic study on photocyclization/photodesulfurisation of triazole-3-thiones

Irradiation of 4-(2-halobenzyl)-5-substituted-1,2,4-triazole-3-thiones under base mediated (CH3CN/2 M NaOH) condition afforded triazolo[3,4-b]-1,3(4H)-benzothiazines and desulfurized triazoles. Benzophenone sensitized photolysis of triazole-3-thiones gave desulfurized triazoles exclusively. The mechanism of the photocyclization/photodesulfurization and the involvement of singlet and triplet energy levels are discussed.

Photodesulfurization of 2,4-diaryl-1,2, 4-triazole-3-thiones

The photodesulfurization of 2,4-diaryl-1,2,4-triazole-3-thiones was discussed in the article. The triazole thiones were synthesized from the respective acid hydrazide and isothiocyanate. The structure of the compounds were confirmed by spectral and analytical data. It was concluded that thioenolization may facilitate the desulfurization.

4-Aralkyl-5-substituted-1,2,4-triazole-5-thiols

Compounds of formula (I) and pharmaceutically acceptable salts thereof are described in which, n is 0 to 5; X1 to X5 are any accessible combination of hydrogen, halogen, C1 6alkyl, C1 6alkoxy, cyano, nitro, SONH2, SO2NH2, SO2CH3, SO2CH2F, SO2CHF2, SO2CF3, CF3, CHO, OH, CH2OH, CO2H, or CO2CpH2p+1wherein p is 1 to 4; R1 is phenyl substituted by X1 to X5, C1 4alkyl, C3 6cycloalkyl, or an arylC1 4alkyl group substituted by X1 to X5; R2 is hydrogen, C1 4alkyl or (CH2)m-CO2R3; m is 0 to 5; and R3 is H or C1 4alkyl. These compounds are dopamine-β-hydroxylase inhibitors. Pharmaceutical compositions are described as are methods of use. Processes for the preparation of these compounds are described.

Derives de la dihydro-2,4 triazole-1,2,4 thione-3 et de l'amino-2 thiadiazole-1,3,4 a partir de nouvelles thiosemicarbazones d'esters

A new general synthesis of 4,5-disubstituted 2,4-dihydro-1,2,3-triazole-3-thiones is proposed.These heterocycles are obtained by the action of primary amines, aralhydrazines or aroylhydrazines on the thiosemicarbazones of esters.These last compounds are prepared by action of chlorhydrates of iminoesters on thiosemicarbazide in dimethylformamide.These thiosemicarbazones react also with strong acids, acid anhydrides and chlorides; by thermolysis and they give 2-amino-1,3,4-thiadiazole derivatives.Also, two derivatives of 1,2,4-triazolo-1,3,4-thiadiazole have been prepared.