85103-39-5

Upstream product

• 87-24-1 ethyl 2-methylbenzoate 
• 89-71-4 2-Methyl-benzoic acid methyl ester 
• 118-90-1 ortho-methylbenzoic acid 
• 75-15-0 carbon disulfide 
• 7658-80-2 2-methylbenzohydrazide 
• 933-88-0 ortho-toluoyl chloride 

Downstream Products

• 87239-95-0 4-amino-5-(2-methylphenyl)-4H-1,2,4-triazole-3-thiol 
• 87239-95-0 4-amino-2,4-dihydro-5-(2-methylphenyl)-3H-1,2,4-triazole-3-thione 
• 2503-66-4 5-(2-methylphenyl)-1,3,4-oxadiazole-2-thiol 
• 591734-70-2 N'-(2-methylbenzoyl)-hydrazinecarbodithioic acid methyl ester 
• 76779-96-9 5-(2-methylphenyl)-1,3,4-thiadiazole-2-thiol 

Relevant academic research and scientific papers

5-substituent-1, 2, 4-triazole-thioketone Schiff base compound as well as preparation method and application thereof

The invention belongs to the technical field of chemical medicines, and relates to a 5-substituent 1, 2, 4-triazole thioketone Schiff base compound as well as a preparation method and application thereof. An intermediate (I) or an intermediate (II) is subjected to reflux reaction with 3, 5-dimethyl 4-hydroxy benzaldehyde in glacial acetic acid respectively, filtering and drying are performed to obtain the 5-substituent -1, 2, 4-triazole thioketone Schiff base compound. According to the 5-substituent-1, 2, 4-triazole-thioketone Schiff base compound as well as the preparation method and application thereof of the invention, an active group-- imino is introduced into a triazole ring matrix to prepare and synthesize a series of triazole Schiff base compounds with multiple active sites, and thetriazole Schiff base compounds have the advantages of good activity, small dosage, small toxic and side effects, safety and environmental protection; meanwhile, the compounds can be used as crop antifungal agents and can influence the synthesis of fungal cell walls, so that the growth and proliferation of fungi are inhibited, and finally, an antibacterial or bactericidal effect is achieved.

Synthesis and Biological Evaluation of Kojic Acid Derivatives Containing 1,2,4-triazole as Potent Tyrosinase Inhibitors

A series of 5-substituted-3-[5-hydroxy-4-pyrone-2-yl-methymercapto]-4-amino-1,2,4-triazole derivatives were synthesized by nucleophilic substitution reaction of 5-hydroxy-2-chloromethyl -4H-pyran-4-one with 5-substituted-3-mercapto-4-amino-1,2,4-triazole,

Ultrasound-assisted, one-pot, three-component synthesis and antibacterial activities of novel indole derivatives containing 1,3,4-oxadiazole and 1,2,4-triazole moieties

Thirteen novel indole derivatives were efficiently synthesized through ultrasound irradiation by using 4-amino-5-(1H-indol-3-yl)-4H-[1,2,4]triazole-3-thiol (8) and 2-mercapto-5-substituted-1,3,4-oxadiazoles (5a-m). Compared with conventional and microwave methods, yields increased to 82-93%, and reaction times decreased to 15-35 min. The structures of these novel compounds were characterized by spectral data and elemental analysis. Two out of the synthesized compounds (10f and 10l) exhibited excellent activity against Staphylococcus aureus and Escherichia coli, and thus warrant further research.

Synthesis and evaluation of novel azoles as potent antifungal agents

Using a rational approach to the design of antifungal agents, a series of azole agents with 1,3,4-oxadiazole side chains were designed and synthesized. The results of preliminary in vitro antifungal tests with eight human pathogenic compounds showed that all of the title compounds exhibited excellent activities against all of the tested fungi except Aspergillus fumigatus. Compounds 11e and 11f were found to be the most effective, with a minimum inhibitory concentration of 0.0039 μg/mL, followed by voriconazole, which has a MIC of 0.0625 μg/mL. The 1,3,4-oxadiazole side chain is not the major contributor but plays a role in eliciting the observed antifungal activity.

Synthesis and evaluation of antioxidant properties of novel 1,2,4-triazole-based schiff base heterocycles

A series of 1,2,4-triazole-based Schiff base heterocyclic compounds (5a-f and 8a-i) and phenethylamines (7a-h) were synthesized and evaluated for antioxidant properties by free-radical scavenging, anti-hemolytic activity, lipid peroxidation, and their protective effects against DNA oxidative damage. Compounds 7c, 7d, 7h, 8b, and 8i showed promising DPPH? radical scavenging activity with the level of inhibition between 86.8% and 94%. Compounds 8a, 8b, 8d, 8g, and 8i were effective against the oxidative hemolysis of human erythrocytes and lipid peroxidation, in a dose-dependent manner, with IC50 values in the range of 55.7-80.7 and 53.2-81.2 μg/mL, respectively. Compounds 8a and 8b were effective against oxidative damage on erythrocyte ghost membrane proteins, and 8g and 8i were able to protect against DNA oxidative damage. 1,2,4-Triazole based Schiff base heterocycles (5a-f, 8a-i) and phenethylamines (7a-h) were synthesized and evaluated for their antioxidant properties by free-radical scavenging, anti-hemolytic activity, lipid peroxidation, and their protective effects against DNA oxidative damage.

Synthesis and antihyperlipidemic activity of some novel 4-(substitutedamino)-5-substituted-3-mercapto-(4H)-1,2,4-triazoles

Hyperlipidemia is considered one of the key factors for cardiovascular diseases. Based on earlier work on a series of 5-alkyl-4-aryl-3-mercapto-(4H)-1, 2,4-triazoles, for further lead modification, a series of 4-(substituted)amino- 5-substituted-3-mercapto-(4H)-1,2,4-triazoles was designed. Target compounds were synthesized by the well known Hoggarth synthesis of substituted 1,2,4-triazoles. Synthesized compounds were screened for lipid lowering activity using the "Poloxamer 407 induced hyperlipidemia in rats" model at a dose of 100 mg/kg p. o. Compounds were found to alter serum lipid levels significantly. Most of the compounds significantly reduced serum cholesterol and triglyceride levels. Some of the compounds were found to reduce triglycerides and elevate high density lipoprotein (HDL) levels more than the standard drug atorvastatin (CAS 134523-03-8). Compounds with chloro substitution on aryl rings were found more active in reducing serum lipid levels than other substitutions. ECV ? Editio Cantor Verlag.

Green synthesis of 5-substituted-1,3,4-thiadiazole-2-thiols as new potent nitrification inhibitors [1]

(Chemical Equation Presented) A fast, efficient synthesis of 5-substituted-1,3,4-thiadiazole-2-thiols was successfully developed, assessed using green chemistry matrices, and compounds were screened for their in vitro nitrification inhibitory activity. The greener method was superior with higher energy efficiency, E(nvironmental) factor, atom economy, atom efficiency, carbon efficiency, and reaction mass efficiency.

Identification of a potent new chemotype for the selective inhibition of PDE4

A series of substituted 3,6-diphenyl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines were prepared and analyzed as inhibitors of phosphodiesterase 4 (PDE4). Synthesis, structure-activity relationships, and the selectivity of a highly potent analogue against related phosphodiesterase isoforms are presented.